| Year |
Citation |
Score |
| 2022 |
Dwomoh L, Rossi M, Scarpa M, Khajehali E, Molloy C, Herzyk P, Mistry SN, Bottrill AR, Sexton PM, Christopoulos A, Conn J, Lindsley CW, Bradley SJ, Tobin AB. M muscarinic receptor activation reduces the molecular pathology and slows the progression of prion-mediated neurodegenerative disease. Science Signaling. 15: eabm3720. PMID 36378750 DOI: 10.1126/scisignal.abm3720 |
0.791 |
|
| 2022 |
Luessen DJ, Gallinger IM, Ferranti AS, Foster DJ, Melancon BJ, Lindsley CW, Niswender CM, Conn J. mGlu-mediated restoration of prefrontal cortex inhibitory signaling reverses social and cognitive deficits in an NMDA hypofunction model in mice. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 35643819 DOI: 10.1038/s41386-022-01350-0 |
0.778 |
|
| 2022 |
Garrison AT, Orsi DL, Capstick RA, Whomble D, Li J, Carter TR, Felts AS, Vinson PN, Rodriguez AL, Han A, Hajari K, Cho HP, Teal LB, Ragland MG, Ghamari-Langroudi M, ... ... Lindsley CW, et al. Development of : A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder. Journal of Medicinal Chemistry. PMID 35417155 DOI: 10.1021/acs.jmedchem.2c00192 |
0.751 |
|
| 2022 |
McClenahan SJ, Kent C, Kharade S, Isaeva E, Williams J, Han C, Terker A, Gresham R, Lazarenko R, Days E, Romaine I, Bauer J, Boutaud O, Sulikowski G, Harris R, ... ... Lindsley C, et al. . Molecular Pharmacology. PMID 35246480 DOI: 10.1124/molpharm.121.000464 |
0.79 |
|
| 2021 |
Bertron JL, Duvernay MT, Mitchell SG, Smith ST, Maeng JG, Blobaum AL, Davis DC, Meiler J, Hamm HE, Lindsley CW. Discovery and Optimization of a Novel Series of Competitive and Central Nervous System-Penetrant Protease-Activated Receptor 4 (PAR4) Inhibitors. Acs Chemical Neuroscience. PMID 34855359 DOI: 10.1021/acschemneuro.1c00557 |
0.8 |
|
| 2021 |
Long MF, Capstick RA, Spearing PK, Engers JL, Gregro AR, Bollinger SR, Chang S, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Jeffrey Conn P, Lindsley CW, Engers DW, et al. Development of structurally distinct tricyclic M positive allosteric modulator (PAM) chemotypes - Part 2. Bioorganic & Medicinal Chemistry Letters. 128416. PMID 34710625 DOI: 10.1016/j.bmcl.2021.128416 |
0.68 |
|
| 2021 |
Yamada Y, Gilliland K, Xiang Z, Haymer D, Crocker KE, Loch MT, Schulte ML, Rodriguez AL, Niswender CM, Jeffrey Conn P, Lindsley CW, Melancon BJ. Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds. Bioorganic & Medicinal Chemistry Letters. 128342. PMID 34461178 DOI: 10.1016/j.bmcl.2021.128342 |
0.634 |
|
| 2021 |
Kent CN, Fulton MG, Stillwell KJ, Dickerson JW, Loch MT, Rodriguez AL, Blobaum AL, Boutaud O, Rook JL, Niswender CM, Jeffrey Conn P, Lindsley CW. Discovery and optimization of a novel CNS penetrant series of mGlu PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian model. Bioorganic & Medicinal Chemistry Letters. 127838. PMID 33556572 DOI: 10.1016/j.bmcl.2021.127838 |
0.791 |
|
| 2020 |
Reed CW, Kalbfleisch JJ, Wong MJ, Washecheck JP, Hunter A, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu Positive Allosteric Modulator Tool Compound. Acs Medicinal Chemistry Letters. 11: 1773-1779. PMID 32944146 DOI: 10.1021/Acsmedchemlett.0C00432 |
0.305 |
|
| 2020 |
Kalbfleisch JJ, Reed CW, Park C, Spearing PK, Quitalig MC, Jenkins MT, Rodriguez AL, Blobaum AL, Jeffrey Conn P, Niswender CM, Lindsley CW. Synthesis and SAR of a series of mGlu NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core. Bioorganic & Medicinal Chemistry Letters. 127529. PMID 32890686 DOI: 10.1016/J.Bmcl.2020.127529 |
0.368 |
|
| 2020 |
Kent CN, Park C, Lindsley CW. Classics in Chemical Neuroscience: Baclofen. Acs Chemical Neuroscience. PMID 32436697 DOI: 10.1021/Acschemneuro.0C00254 |
0.78 |
|
| 2020 |
Fulton MG, Loch MT, Rodriguez AL, Lin X, Javitch JA, Conn PJ, Niswender CM, Lindsley CW. Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu heterodimeric receptor results in a compound with mGlu homodimer selectivity. Bioorganic & Medicinal Chemistry Letters. 127212. PMID 32371100 DOI: 10.1016/J.Bmcl.2020.127212 |
0.368 |
|
| 2020 |
Turkett JA, Ringuette AE, Lindsley CW, Bender AM. Synthesis of Substituted 6,7-Dihydro-5H-pyrrolo[2,3-c]pyridazines/pyrazines via Catalyst-Free, Tandem Hydroamination-Aromatic Substitution. The Journal of Organic Chemistry. PMID 32227869 DOI: 10.1021/Acs.Joc.9B03463 |
0.313 |
|
| 2020 |
Jeffries DE, Borza CM, Blobaum AL, Pozzi A, Lindsley CW. Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy. Acs Medicinal Chemistry Letters. 11: 29-33. PMID 31938459 DOI: 10.1021/Acsmedchemlett.9B00382 |
0.346 |
|
| 2020 |
Norman CL, Gould RW, Bragg C, Lindsley CW, Jones CK, Nader MA. The Effects of the M 1 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0486846 on Cognitive Performance in Aged Nonhuman Primates The Faseb Journal. 34: 1-1. DOI: 10.1096/Fasebj.2020.34.S1.08654 |
0.32 |
|
| 2020 |
Conley A, Key A, Blackford J, Rook J, Conn J, Lindsley C, Jones C, Newhouse P. FUNCTIONAL ACTIVITY OF THE MUSCARINIC POSITIVE ALLOSTERIC MODULATOR VU319 DURING A PHASE 1 SINGLE ASCENDING DOSE STUDY The American Journal of Geriatric Psychiatry. 28: S114-S115. DOI: 10.1016/J.Jagp.2020.01.142 |
0.772 |
|
| 2019 |
Moran SP, Xiang Z, Doyle CA, Maksymetz J, Lv X, Faltin S, Fisher NM, Niswender CM, Rook JM, Lindsley CW, Conn PJ. Biased M receptor-positive allosteric modulators reveal role of phospholipase D in M-dependent rodent cortical plasticity. Science Signaling. 12. PMID 31796631 DOI: 10.1126/Scisignal.Aax2057 |
0.383 |
|
| 2019 |
Temple KJ, Long MF, Engers JL, Watson KJ, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Jeffrey Conn P, Engers DW, Lindsley CW. Discovery of structurally distinct tricyclic M positive allosteric modulator (PAM) chemotypes. Bioorganic & Medicinal Chemistry Letters. 126811. PMID 31787491 DOI: 10.1016/J.Bmcl.2019.126811 |
0.67 |
|
| 2019 |
Temple KJ, Engers JL, Long MF, Watson KJ, Chang S, Luscombe VB, Jenkins MT, Rodriguez AL, Niswender CM, Bridges TM, Jeffrey Conn P, Engers DW, Lindsley CW. Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M positive allosteric modulator (PAM) chemotype. Bioorganic & Medicinal Chemistry Letters. 126812. PMID 31784320 DOI: 10.1016/J.Bmcl.2019.126812 |
0.692 |
|
| 2019 |
Vuckovic Z, Gentry PR, Berizzi AE, Hirata K, Varghese S, Thompson G, van der Westhuizen ET, Burger WAC, Rahmani R, Valant C, Langmead CJ, Lindsley CW, Baell JB, Tobin AB, Sexton PM, et al. Crystal structure of the M muscarinic acetylcholine receptor. Proceedings of the National Academy of Sciences of the United States of America. PMID 31772027 DOI: 10.2210/Pdb6Ol9/Pdb |
0.35 |
|
| 2019 |
Joffe ME, Santiago CI, Oliver KH, Maksymetz J, Harris NA, Engers JL, Lindsley CW, Winder DG, Conn PJ. mGlu and mGlu Negative Allosteric Modulators Divergently Enhance Thalamocortical Transmission and Exert Rapid Antidepressant-like Effects. Neuron. PMID 31735403 DOI: 10.1016/J.Neuron.2019.09.044 |
0.318 |
|
| 2019 |
Temple KJ, Engers JL, Long MF, Gregro AR, Watson KJ, Chang S, Jenkins MT, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW. Discovery of a novel 3,4-dimethylcinnoline carboxamide M positive allosteric modulator (PAM) chemotype via scaffold hopping. Bioorganic & Medicinal Chemistry Letters. 126678. PMID 31537424 DOI: 10.1016/j.bmcl.2019.126678 |
0.658 |
|
| 2019 |
Fulton MG, Bertron JL, Reed CW, Lindsley CW. Formal Total Synthesis of Pericoannosin A. The Journal of Organic Chemistry. PMID 31436090 DOI: 10.1021/Acs.Joc.9B01846 |
0.791 |
|
| 2019 |
Yamada Y, Yohn SE, Gilliland K, Loch MT, Schulte ML, Rodriguez AL, Blobaum AL, Niswender CM, Jeffrey Conn P, Lindsley CW. Further exploration of an N-aryl phenoxyethoxy pyridinone-based series of mGlu NAMs: Challenging SAR, enantiospecific activity and in vivo efficacy. Bioorganic & Medicinal Chemistry Letters. PMID 31358468 DOI: 10.1016/J.Bmcl.2019.07.030 |
0.654 |
|
| 2019 |
Gould RW, Gunter BW, Bubser M, Matthews RT, Teal LB, Ragland MG, Bridges TM, Garrison AT, Winder DG, Lindsley CW, Jones CK. Acute Negative Allosteric Modulation of M Muscarinic Acetylcholine Receptors Inhibits Oxycodone Self-Administration and Cue-Induced Reactivity with no effect on Antinociception. Acs Chemical Neuroscience. PMID 31268669 DOI: 10.1021/Acschemneuro.9B00274 |
0.738 |
|
| 2019 |
Chopko TC, Han C, Gregro AR, Engers DW, Felts AS, Poslusney MS, Bollinger KA, Morrison RD, Bubser M, Lamsal A, Luscombe VB, Cho HP, Schnetz-Boutaud NC, Rodriguez AL, Chang S, ... ... Lindsley CW, et al. SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M PAMs. Bioorganic & Medicinal Chemistry Letters. PMID 31248774 DOI: 10.1016/J.Bmcl.2019.06.032 |
0.377 |
|
| 2019 |
Butkiewicz M, Rodriguez AL, Rainey SE, Wieting JM, Luscombe VB, Stauffer SR, Lindsley CW, Conn PJ, Meiler J. Identification of novel allosteric modulators of mGlu5 acting at site distinct from MPEP binding. Acs Chemical Neuroscience. PMID 31132237 DOI: 10.1021/Acschemneuro.8B00227 |
0.358 |
|
| 2019 |
Engers DW, Melancon BJ, Gregro AR, Bertron JL, Bollinger SR, Felts AS, Konkol LC, Wood MR, Bollinger KA, Luscombe VB, Rodriguez AL, Jones CK, Bubser M, Yohn SE, Wood MW, ... ... Lindsley CW, et al. VU6005806/AZN-00016130, an advanced M positive allosteric modulator (PAM) profiled as a potential preclinical development candidate. Bioorganic & Medicinal Chemistry Letters. PMID 31113706 DOI: 10.1016/J.Bmcl.2019.05.026 |
0.807 |
|
| 2019 |
Childress ES, Garrison AT, Sheldon JR, Skaar EP, Lindsley CW. Total synthesis of hinduchelins A-D, stereochemical revision of hinduchelin A, and biological evaluation of natural and unnatural analogs. The Journal of Organic Chemistry. PMID 31039303 DOI: 10.1021/Acs.Joc.9B00391 |
0.741 |
|
| 2019 |
Maksymetz J, Joffe ME, Moran SP, Stansley BJ, Li B, Temple K, Engers DW, Lawrence JJ, Lindsley CW, Conn PJ. M Muscarinic Receptors Modulate Fear-Related Inputs to the Prefrontal Cortex: Implications for Novel Treatments of Posttraumatic Stress Disorder. Biological Psychiatry. PMID 31003787 DOI: 10.1016/J.Biopsych.2019.02.020 |
0.642 |
|
| 2019 |
Jeffries DE, Lindsley CW. Asymmetric synthesis of natural and unnatural dibenzylbutane lignans from a common intermediate. The Journal of Organic Chemistry. PMID 31002498 DOI: 10.1021/Acs.Joc.9B00633 |
0.338 |
|
| 2019 |
Panarese JD, Engers DW, Wu YJ, Bronson JJ, Macor JE, Chun A, Rodriguez AL, Felts AS, Engers JL, Loch MT, Emmitte KA, Castelhano AL, Kates MJ, Nader MA, Jones CK, ... ... Lindsley CW, et al. Discovery of VU2957 (Valiglurax): An mGlu Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease. Acs Medicinal Chemistry Letters. 10: 255-260. PMID 30891122 DOI: 10.1021/Acsmedchemlett.8B00426 |
0.316 |
|
| 2019 |
Garrison AT, Childress ES, Davis DC, Lindsley CW. Preparation of 1,5-Dihydropyrazolo[3',4':5,6]pyrano[3,4- b]pyridines via a Microwave-Assisted, Palladium-Catalyzed Regioselective C-H Heteroarylation of Electron-Rich Pyrazoles. The Journal of Organic Chemistry. PMID 30807155 DOI: 10.1021/Acs.Joc.9B00144 |
0.749 |
|
| 2019 |
Reed CW, Yohn S, Washecheck JP, Roenfanz HF, Quitalig MC, Luscombe VB, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Discovery of an orally bioavailable and Central Nervous System (CNS) penetrant mGlu7 Negative Allosteric Modulator (NAM) in vivo tool compound: N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962). Journal of Medicinal Chemistry. PMID 30608678 DOI: 10.1021/Acs.Jmedchem.8B01810 |
0.313 |
|
| 2019 |
Reed CW, Lindsley CW. A general, enantioselective synthesis of 2-substituted thiomorpholines and thiomorpholine 1,1-dioxides Tetrahedron Letters. 60: 151104. DOI: 10.1016/J.Tetlet.2019.151104 |
0.312 |
|
| 2019 |
Perry CK, Fulton MG, Lindsley CW. Total synthesis of violaceimides A–E and consideration of the reported stereochemistry Tetrahedron Letters. 60: 151103. DOI: 10.1016/J.Tetlet.2019.151103 |
0.303 |
|
| 2019 |
Perry CK, Lindsley CW. Total synthesis of Punicagranine Tetrahedron Letters. 60: 150989. DOI: 10.1016/J.Tetlet.2019.150989 |
0.317 |
|
| 2019 |
Reed CW, Fulton MG, Nance KD, Lindsley CW. Total synthesis of natural (−)- and unnatural (+)-Melearoride A Tetrahedron Letters. 60: 743-745. DOI: 10.1016/J.Tetlet.2019.02.006 |
0.745 |
|
| 2019 |
Rook JM, Newhouse PA, Lindsley CW, Conn PJ. OPTIMIZATION OF NOVEL M1 PAMS FOR CLINICAL DEVELOPMENT WITH ENHANCED EFFICACY WHILE AVOIDING ADVERSE EFFECT LIABILITY FOR THE TREATMENT OF ALZHEIMER’S DISEASE Alzheimer's & Dementia. 15: P1592-P1593. DOI: 10.1016/J.Jalz.2019.09.046 |
0.313 |
|
| 2019 |
Russell JK, Gould RW, Bubser M, Fu RJ, Norman N, Nader MA, Newhouse PA, Lindsley CW, Conn J, Jones CK. P2-068: Circadian Rhythm-Dependent Effects Of M1 Muscarinic Acetylcholine Receptor Positive Allosteric Modulators On Arousal And Cognition Alzheimers & Dementia. 15. DOI: 10.1016/J.Jalz.2019.06.2475 |
0.791 |
|
| 2019 |
Newhouse PA, Conley AC, Key AP, Blackford JU, Lindsley CW, Conn J, Jones CK. P2-009: DEVELOPMENT OF THE MUSCARINIC CHOLINERGIC PAM VU319 FOR COGNITIVE ENHANCEMENT: PHASE 1 TESTS OF SAFETY AND TARGET ENGAGEMENT Alzheimer's & Dementia. 15: P574-P574. DOI: 10.1016/J.Jalz.2019.06.1231 |
0.767 |
|
| 2019 |
Conley AC, Key AP, Blackford JU, Conn J, Lindsley CW, Jones CK, Newhouse PA. P1-053: COGNITIVE AND ELECTROPHYSIOLOGICAL MEASURES OF A PHASE 1 SINGLE ASCENDING DOSE STUDY OF THE MUSCARINIC POSITIVE ALLOSTERIC MODULATOR VU319 Alzheimer's & Dementia. 15: P253-P253. DOI: 10.1016/J.Jalz.2019.06.078 |
0.767 |
|
| 2019 |
Conley A, Key A, Conn PJ, Lindsley C, Jones C, Newhouse P. THE USE OF COGNITIVE AND ERP BIOMARKERS OF CHOLINERGIC FUNCTION IN NOVEL TESTS OF MUSCARINIC POSITIVE ALLOSTERIC MODULATORS The American Journal of Geriatric Psychiatry. 27: S132. DOI: 10.1016/J.Jagp.2019.01.038 |
0.32 |
|
| 2018 |
Prael FJ, Chen R, Li Z, Reed CW, Lindsley CW, Weaver CD, Swale DR. Use of chemical probes to explore the toxicological potential of the K/Cl cotransporter (KCC) as a novel insecticide target to control the primary vector of dengue and Zika virus, Aedes aegypti. Pesticide Biochemistry and Physiology. 151: 10-17. PMID 30704707 DOI: 10.1016/J.Pestbp.2018.03.019 |
0.301 |
|
| 2018 |
Poslusney MS, Salovich JM, Wood MR, Melancon BJ, Bollinger KA, Luscombe VB, Rodriguez AL, Engers DW, Bridges TM, Niswender CM, Jeffrey Conn P, Lindsley CW. Novel M positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands. Bioorganic & Medicinal Chemistry Letters. PMID 30580918 DOI: 10.1016/J.Bmcl.2018.12.039 |
0.318 |
|
| 2018 |
Rigg RA, Healy LD, Chu TT, Ngo ATP, Mitrugno A, Zilberman-Rudenko J, Aslan JE, Hinds MT, Vecchiarelli LD, Morgan TK, Gruber A, Temple KJ, Lindsley CW, Duvernay MT, Hamm HE, et al. Protease-activated receptor 4 activity promotes platelet granule release and platelet-leukocyte interactions. Platelets. 1-10. PMID 30560697 DOI: 10.1080/09537104.2017.1406076 |
0.64 |
|
| 2018 |
Waterson AG, Scott SA, Kett NR, Blobaum AL, Alex Brown H, Lindsley CW. Isoform selective PLD inhibition by novel, chiral 2,8-diazaspiro[4.5]decan-1-one derivatives. Bioorganic & Medicinal Chemistry Letters. PMID 30528979 DOI: 10.1016/J.Bmcl.2018.10.033 |
0.324 |
|
| 2018 |
Panarese JD, Engers DW, Wu YJ, Guernon JM, Chun A, Gregro AR, Bender AM, Capstick RA, Wieting JM, Bronson JJ, Macor JE, Westphal R, Soars M, Engers JE, Felts AS, ... ... Lindsley CW, et al. The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu PAM development candidate. Bioorganic & Medicinal Chemistry Letters. PMID 30503632 DOI: 10.1016/J.Bmcl.2018.10.050 |
0.341 |
|
| 2018 |
Felts AS, Bollinger KA, Brassard CJ, Rodriguez AL, Morrison RD, Scott Daniels J, Blobaum AL, Niswender CM, Jones CK, Jeffrey Conn P, Emmitte KA, Lindsley CW. Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. Bioorganic & Medicinal Chemistry Letters. PMID 30446311 DOI: 10.1016/J.Bmcl.2018.11.017 |
0.348 |
|
| 2018 |
Fisher NM, Seto M, Lindsley CW, Niswender CM. Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental Disorders. Frontiers in Molecular Neuroscience. 11: 387. PMID 30405350 DOI: 10.3389/Fnmol.2018.00387 |
0.335 |
|
| 2018 |
Childress ES, Wieting JM, Felts AS, Breiner MM, Long MF, Luscombe VB, Rodriguez AL, Cho HP, Blobaum AL, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW. Discovery of novel central nervous system penetrant metabotropic glutamate receptor subtype 2 (mGlu) Negative Allosteric Modulators (NAMs) based on functionalized pyrazolo[1,5- a]pyrimidine-5-carboxamide and thieno[3,2- b]pyridine-5-carboxamide cores. Journal of Medicinal Chemistry. PMID 30350962 DOI: 10.1021/Acs.Jmedchem.8B01266 |
0.367 |
|
| 2018 |
Bender AM, Garrison AT, Lindsley CW. The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation. Acs Chemical Neuroscience. PMID 30280567 DOI: 10.1021/Acschemneuro.8B00481 |
0.772 |
|
| 2018 |
Engers JL, Childress ES, Long MF, Capstick RA, Luscombe VB, Cho HP, Dickerson JW, Rook JM, Blobaum AL, Niswender CM, Engers DW, Conn PJ, Lindsley CW. VU6007477, a Novel M PAM Based on a Pyrrolo[2,3-]pyridine Carboxamide Core Devoid of Cholinergic Adverse Events. Acs Medicinal Chemistry Letters. 9: 917-922. PMID 30258541 DOI: 10.1021/Acsmedchemlett.8B00261 |
0.373 |
|
| 2018 |
Bollinger S, Engers DW, Panarese JD, West M, Engers JL, Loch MT, Rodriguez AL, Blobaum AL, Jones CK, Thompson Gray A, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. The discovery, SAR and biological characterization of a novel series of 6-((1H-pyrazolo[4,3-b]pyridin-3-yl)amino)-benzo[d]isothiazole-3-carboxamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4). Journal of Medicinal Chemistry. PMID 30247901 DOI: 10.1021/Acs.Jmedchem.8B00994 |
0.344 |
|
| 2018 |
Yohn SE, Foster DJ, Covey DP, Moehle MS, Galbraith J, Garcia-Barrantes PM, Cho HP, Bubser M, Blobaum AL, Joffe ME, Cheer JF, Jones CK, Lindsley CW, Conn PJ. Activation of the mGlu metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M muscarinic receptor allosteric modulators. Molecular Psychiatry. PMID 30116027 DOI: 10.1038/S41380-018-0206-2 |
0.763 |
|
| 2018 |
Engers JL, Bender AM, Kalbfleisch JJ, Cho HP, Ligenfelter KS, Luscombe VB, Han C, Melancon B, Blobaum AL, Dickerson JW, Rook JM, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW. Discovery of tricyclic triazolo- and imidazopyridine lactams as M1 positive allosteric modulators (PAMs). Acs Chemical Neuroscience. PMID 30086237 DOI: 10.1021/Acschemneuro.8B00311 |
0.375 |
|
| 2018 |
Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, ... ... Lindsley CW, et al. Corrigendum to "Challenges in the development of an M PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184]. Bioorganic & Medicinal Chemistry Letters. PMID 30076050 DOI: 10.1016/J.Bmcl.2018.07.022 |
0.378 |
|
| 2018 |
Engers DW, Bollinger SR, Engers JL, Panarese JD, Breiner MM, Gregro A, Blobaum AL, Bronson JJ, Wu YJ, Macor JE, Rodriguez AL, Zamorano R, Conn PJ, Lindsley CW, Niswender CM, et al. Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu positive allosteric modulators that mitigate CYP1A2 induction liability. Bioorganic & Medicinal Chemistry Letters. PMID 29958762 DOI: 10.1016/J.Bmcl.2018.06.034 |
0.368 |
|
| 2018 |
Kharade SV, Kurata H, Bender A, Blobaum AL, Figueroa EE, Duran AM, Kramer M, Days E, Vinson P, Flores D, Satlin LM, Meiler J, Weaver CD, Lindsley CW, Hopkins CR, et al. Discovery, characterization, and effects on renal fluid and electrolyte excretion of the Kir4.1 potassium channel pore blocker, VU0134992. Molecular Pharmacology. PMID 29895592 DOI: 10.1124/Mol.118.112359 |
0.324 |
|
| 2018 |
Friggeri L, Hargrove TY, Wawrzak Z, Blobaum AL, Rachakonda G, Lindsley CW, Villalta F, Nes WD, Botta M, Guengerich FP, Lepesheva GI. Sterol 14α-Demethylase Structure-Based Design of VNI ((R)-N-(1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives to Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis. Journal of Medicinal Chemistry. PMID 29894182 DOI: 10.1021/Acs.Jmedchem.8B00641 |
0.345 |
|
| 2018 |
Khajehali E, Valant C, Jörg M, Tobin AB, Jeffrey Conn P, Lindsley CW, Sexton PM, Scammells PJ, Christopoulos A. Probing the binding site of novel selective positive allosteric modulators at the M mAChR. Biochemical Pharmacology. PMID 29777683 DOI: 10.1016/J.Bcp.2018.05.009 |
0.388 |
|
| 2018 |
Bertron JL, Cho HP, Garcia-Barrantes PM, Panarese JD, Salovich JM, Nance KD, Engers DW, Rook JM, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW. The discovery of VU0486846: steep SAR from a series of M PAMs based on a novel benzomorpholine core. Bioorganic & Medicinal Chemistry Letters. PMID 29754948 DOI: 10.1016/J.Bmcl.2018.05.009 |
0.808 |
|
| 2018 |
Felts AS, Rodriguez AL, Morrison RD, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. Bioorganic & Medicinal Chemistry Letters. PMID 29705142 DOI: 10.1016/J.Bmcl.2018.04.053 |
0.365 |
|
| 2018 |
Rook JM, Bertron JL, Cho HP, Garcia-Barrantes PM, Moran SP, Maksymetz JT, Nance KD, Dickerson JW, Remke DH, Chang S, Harp J, Blobaum AL, Niswender CM, Jones CK, Stauffer SR, ... ... Lindsley CW, et al. A novel M1 PAM VU0486846 exerts efficacy in cognition models without displaying agonist activity or cholinergic toxicity. Acs Chemical Neuroscience. PMID 29701957 DOI: 10.1021/Acschemneuro.8B00131 |
0.805 |
|
| 2018 |
Berizzi A, Bender AM, Lindsley CW, Conn PJ, Sexton PM, Langmead C, Christopoulos A. Structure-activity relationships of pan-Gα coupled muscarinic acetylcholine receptor positive allosteric modulators. Acs Chemical Neuroscience. PMID 29683647 DOI: 10.1021/Acschemneuro.8B00136 |
0.412 |
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| 2018 |
Moran SP, Cho HP, Maksymetz J, Remke DH, Hanson RM, Niswender CM, Lindsley CW, Rook JM, Conn PJ. PF-06827443 displays robust allosteric agonist and positive allosteric modulator activity in high receptor reserve and native systems. Acs Chemical Neuroscience. PMID 29683646 DOI: 10.1021/Acschemneuro.8B00106 |
0.38 |
|
| 2018 |
Bender AM, Cho HP, Nance KD, Lingenfelter KS, Luscombe VB, Gentry PR, Voigtritter K, Berizzi AE, Sexton PM, Langmead C, Christopoulos A, Locuson CW, Bridges TM, Chang S, O'Neil JC, ... ... Lindsley CW, et al. Discovery and Optimization of Potent and CNS Penetrant M5-Preferring PAMs Derived From a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold. Acs Chemical Neuroscience. PMID 29678111 DOI: 10.1021/Acschemneuro.8B00126 |
0.801 |
|
| 2018 |
Moran SP, Dickerson JW, Cho HP, Xiang Z, Maksymetz J, Remke DH, Lv X, Doyle CA, Rajan DH, Niswender CM, Engers DW, Lindsley CW, Rook JM, Conn PJ. M-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 29581537 DOI: 10.1038/S41386-018-0033-9 |
0.325 |
|
| 2018 |
O'Brien DE, Shaw DM, Cho HP, Cross AJ, Wesolowski SS, Felts AS, Bergare J, Elmore CS, Lindsley CW, Niswender CM, Conn PJ. Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators. Molecular Pharmacology. PMID 29545267 DOI: 10.1124/Mol.117.110114 |
0.311 |
|
| 2018 |
Gogliotti R, Fisher N, Stansley B, Jones C, Lindsley C, Conn J, Niswender C. Total RNA-sequencing of Rett Syndrome Autopsy Samples Identifies the M4 Muscarinic Receptor as a Novel Therapeutic Target. The Journal of Pharmacology and Experimental Therapeutics. PMID 29523700 DOI: 10.1124/Jpet.117.246991 |
0.789 |
|
| 2018 |
Stansley B, Joffe M, Yohn S, Lindsley C, Niswender C, Jeffrey Conn P. T39. NEURAL MECHANISMS OF METABOTROPIC GLUTAMATE RECEPTOR 3 MEDIATED ENHANCEMENT OF SYNAPTIC PLASTICITY AND COGNITION Schizophrenia Bulletin. 44: S127-S128. DOI: 10.1093/Schbul/Sby016.315 |
0.304 |
|
| 2017 |
Moehle MS, Pancani T, Byun N, Yohn SE, Wilson GH, Dickerson JW, Remke DH, Xiang Z, Niswender CM, Wess J, Jones CK, Lindsley CW, Rook JM, Conn PJ. Cholinergic Projections to the Substantia Nigra Pars Reticulata Inhibit Dopamine Modulation of Basal Ganglia through the M4 Muscarinic Receptor. Neuron. 96: 1358-1372.e4. PMID 29268098 DOI: 10.1016/J.Neuron.2017.12.008 |
0.318 |
|
| 2017 |
Reed CW, McGowan KM, Spearing PK, Stansley BJ, Roenfanz HF, Engers DW, Rodriguez AL, Engelberg EM, Luscombe VB, Loch MT, Remke DH, Rook JM, Blobaum AL, Conn PJ, Niswender CM, ... Lindsley CW, et al. VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides. Acs Medicinal Chemistry Letters. 8: 1326-1330. PMID 29259756 DOI: 10.1021/Acsmedchemlett.7B00429 |
0.303 |
|
| 2017 |
Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, ... ... Lindsley CW, et al. Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides. Bioorganic & Medicinal Chemistry Letters. PMID 29089231 DOI: 10.1016/J.Bmcl.2017.10.053 |
0.403 |
|
| 2017 |
Abe M, Seto M, Gogliotti RG, Loch MT, Bollinger KA, Chang S, Engelberg EM, Luscombe VB, Harp JM, Bubser M, Engers DW, Jones CK, Rodriguez AL, Blobaum AL, Conn PJ, ... ... Lindsley CW, et al. Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines. Acs Medicinal Chemistry Letters. 8: 1110-1115. PMID 29057060 DOI: 10.1021/Acsmedchemlett.7B00317 |
0.35 |
|
| 2017 |
Gunter BW, Gould RW, Bubser M, McGowan KM, Lindsley CW, Jones CK. Selective inhibition of M5 muscarinic acetylcholine receptors attenuates cocaine self-administration in rats. Addiction Biology. PMID 29044937 DOI: 10.1111/Adb.12567 |
0.306 |
|
| 2017 |
Long MF, Engers JL, Chang S, Zhan X, Weiner RL, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW. Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping. Bioorganic & Medicinal Chemistry Letters. PMID 29037946 DOI: 10.1016/J.Bmcl.2017.10.016 |
0.37 |
|
| 2017 |
Felts AS, Rodriguez AL, Morrison RD, Bollinger KA, Venable DF, Blobaum AL, Byers FW, Thompson Gray A, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. Bioorganic & Medicinal Chemistry Letters. PMID 28958625 DOI: 10.1016/J.Bmcl.2017.09.042 |
0.382 |
|
| 2017 |
Engers JL, Bollinger KA, Weiner RL, Rodriguez AL, Long MF, Breiner MM, Chang S, Bollinger SR, Bubser M, Jones CK, Morrison RD, Bridges TM, Blobaum AL, Niswender CM, Conn PJ, ... ... Lindsley CW, et al. Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs. Acs Medicinal Chemistry Letters. 8: 925-930. PMID 28947938 DOI: 10.1021/Acsmedchemlett.7B00249 |
0.346 |
|
| 2017 |
Bollinger KA, Felts AS, Brassard CJ, Engers JL, Rodriguez AL, Weiner RL, Cho HP, Chang S, Bubser M, Jones CK, Blobaum AL, Niswender CM, Conn PJ, Emmitte KA, Lindsley CW. Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core. Acs Medicinal Chemistry Letters. 8: 919-924. PMID 28947937 DOI: 10.1021/Acsmedchemlett.7B00279 |
0.355 |
|
| 2017 |
Bewley BR, Spearing PK, Weiner RL, Luscombe VB, Zhan X, Chang S, Cho HP, Rodriguez AL, Niswender CM, Conn PJ, Bridges TM, Engers DW, Lindsley CW. Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core. Bioorganic & Medicinal Chemistry Letters. PMID 28866269 DOI: 10.1016/J.Bmcl.2017.08.043 |
0.368 |
|
| 2017 |
Alam S, Lingenfelter KS, Bender AM, Lindsley CW. Classics in Chemical Neuroscience: Memantine. Acs Chemical Neuroscience. PMID 28737885 DOI: 10.1021/Acschemneuro.7B00270 |
0.313 |
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| 2017 |
Gould RW, Grannan MD, Gunter BW, Ball J, Bubser M, Bridges TM, Wess J, Wood MW, Brandon NJ, Duggan ME, Niswender CM, Lindsley CW, Conn PJ, Jones CK. Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M4 PAM VU0467154. Neuropharmacology. PMID 28729220 DOI: 10.1016/J.Neuropharm.2017.07.013 |
0.338 |
|
| 2017 |
Ghoshal A, Moran SP, Dickerson JW, Joffe ME, Grueter BA, Xiang Z, Lindsley CW, Rook JM, Conn PJ. Role of mGlu5 receptors and inhibitory neurotransmission in M1 dependent muscarinic LTD in the prefrontal cortex: implications in schizophrenia. Acs Chemical Neuroscience. PMID 28679049 DOI: 10.1021/Acschemneuro.7B00167 |
0.352 |
|
| 2017 |
Walker AG, Sheffler DJ, Lewis AS, Dickerson JW, Foster DJ, Senter RK, Moehle MS, Lv X, Stansley BJ, Xiang Z, Rook JM, Emmitte KA, Lindsley CW, Conn PJ. Co-Activation of Metabotropic Glutamate Receptor 3 and Beta-Adrenergic Receptors Modulates Cyclic-AMP, Long-Term Potentiation, and Disrupts Memory Reconsolidation. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 28664928 DOI: 10.1038/Npp.2017.136 |
0.326 |
|
| 2017 |
Bender AM, Weiner RL, Luscombe VB, Ajmera S, Cho HP, Chang S, Zhan X, Rodriguez AL, Niswender CM, Engers DW, Bridges TM, Conn PJ, Lindsley CW. Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists. Bioorganic & Medicinal Chemistry Letters. PMID 28633897 DOI: 10.1016/J.Bmcl.2017.05.042 |
0.431 |
|
| 2017 |
Felts AS, Rodriguez AL, Blobaum AL, Morrison RD, Bates BS, Thompson Gray A, Rook JM, Tantawy MN, Byers FW, Chang S, Venable DF, Luscombe VB, Tamagnan GD, Niswender CM, Daniels JS, ... ... Lindsley CW, et al. Discovery of N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A novel negative allosteric modulator of metabotropic glutamate receptor subtype 5 selected for clinical evaluation. Journal of Medicinal Chemistry. PMID 28530802 DOI: 10.1021/Acs.Jmedchem.7B00410 |
0.346 |
|
| 2017 |
Tarr JC, Wood MR, Noetzel MJ, Bertron JL, Weiner RL, Rodriguez AL, Lamsal A, Byers FW, Chang S, Cho HP, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, ... ... Lindsley CW, et al. Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides. Bioorganic & Medicinal Chemistry Letters. PMID 28522253 DOI: 10.1016/J.Bmcl.2017.05.014 |
0.816 |
|
| 2017 |
Melancon BJ, Wood MR, Noetzel MJ, Nance KD, Engelberg EM, Han C, Lamsal A, Chang S, Cho HP, Byers FW, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, ... ... Lindsley CW, et al. Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology. Bioorganic & Medicinal Chemistry Letters. PMID 28442253 DOI: 10.1016/J.Bmcl.2017.04.043 |
0.767 |
|
| 2017 |
Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM, Schepartz A, Wang S. The Ecstasy and Agony of Assay Interference Compounds. Acs Medicinal Chemistry Letters. 8: 379-382. PMID 28435522 DOI: 10.1021/Acsmedchemlett.7B00056 |
0.32 |
|
| 2017 |
Bender AM, Weiner RL, Luscombe VB, Cho HP, Niswender CM, Engers DW, Bridges TM, Jeffrey Conn P, Lindsley CW. Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype. Bioorganic & Medicinal Chemistry Letters. PMID 28427812 DOI: 10.1016/J.Bmcl.2017.04.009 |
0.414 |
|
| 2017 |
Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM, Schepartz A, Wang S. The Ecstasy and Agony of Assay Interference Compounds. Acs Central Science. 3: 143-147. PMID 28386587 DOI: 10.1021/Acscentsci.7B00069 |
0.32 |
|
| 2017 |
Pulley JM, Shirey-Rice JK, Lavieri RR, Jerome RN, Zaleski NM, Aronoff DM, Bastarache L, Niu X, Holroyd KJ, Roden DM, Skaar EP, Niswender CM, Marnett LJ, Lindsley CW, Ekstrom LB, et al. Accelerating Precision Drug Development and Drug Repurposing by Leveraging Human Genetics. Assay and Drug Development Technologies. PMID 28379727 DOI: 10.1089/Adt.2016.772 |
0.699 |
|
| 2017 |
Sheffler DJ, Nedelcovych MT, Williams R, Turner SC, Duerk BB, Robbins MR, Jadhav SB, Niswender CM, Jones CK, Jeffrey Conn P, Nathan Daniels R, Lindsley CW. Corrigendum to "Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres" [Bioorg. Med. Chem. Lett. 24 (2014) 1062-1066]. Bioorganic & Medicinal Chemistry Letters. PMID 28347668 DOI: 10.1016/J.Bmcl.2017.03.046 |
0.326 |
|
| 2017 |
Lv X, Dickerson JW, Rook JM, Lindsley CW, Conn PJ, Xiang Z. M1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons. Neuropharmacology. PMID 28336323 DOI: 10.1016/J.Neuropharm.2017.03.017 |
0.338 |
|
| 2017 |
Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM, Schepartz A, Wang S. The Ecstasy and Agony of Assay Interference Compounds. Acs Chemical Biology. PMID 28244728 DOI: 10.1021/Acschembio.7B00119 |
0.32 |
|
| 2017 |
Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM, Schepartz A, Wang S. The Ecstasy and Agony of Assay Interference Compounds. Acs Infectious Diseases. PMID 28244723 DOI: 10.1021/Acsinfecdis.7B00023 |
0.32 |
|
| 2017 |
McGowan KM, Nance KD, Cho HP, Bridges TM, Jeffrey Conn P, Jones CK, Lindsley CW. Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies. Bioorganic & Medicinal Chemistry Letters. PMID 28237763 DOI: 10.1016/J.Bmcl.2017.02.020 |
0.749 |
|
| 2017 |
Lebois EP, Schroeder JP, Esparza TJ, Bridges TM, Lindsley CW, Conn PJ, Brody DL, Daniels JS, Levey AI. Disease-Modifying Effects of M1 Muscarinic Acetylcholine Receptor Activation in an Alzheimer's Disease Mouse Model. Acs Chemical Neuroscience. PMID 28230352 DOI: 10.1021/Acschemneuro.6B00278 |
0.785 |
|
| 2017 |
Brown HA, Thomas PG, Lindsley CW. Targeting phospholipase D in cancer, infection and neurodegenerative disorders. Nature Reviews. Drug Discovery. PMID 28209987 DOI: 10.1038/Nrd.2016.252 |
0.349 |
|
| 2017 |
Wood MR, Noetzel MJ, Melancon BJ, Poslusney MS, Nance KD, Hurtado MA, Luscombe VB, Weiner RL, Rodriguez AL, Lamsal A, Chang S, Bubser M, Blobaum AL, Engers DW, Niswender CM, ... ... Lindsley CW, et al. Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia. Acs Medicinal Chemistry Letters. 8: 233-238. PMID 28197318 DOI: 10.1021/Acsmedchemlett.6B00461 |
0.766 |
|
| 2017 |
Bender AM, Jones CK, Lindsley CW. Classics in Chemical Neuroscience: Xanomeline. Acs Chemical Neuroscience. PMID 28141924 DOI: 10.1021/Acschemneuro.7B00001 |
0.381 |
|
| 2017 |
Nance KD, Days EL, Weaver CD, Coldren A, Farmer TD, Cho HP, Niswender CM, Blobaum AL, Niswender KD, Lindsley CW. Discovery of a novel series of orally bioavailable and CNS penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) non-competitive antagonists based on a 1,3-disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione core. Journal of Medicinal Chemistry. PMID 28103022 DOI: 10.1021/Acs.Jmedchem.6B01706 |
0.739 |
|
| 2017 |
David TK, Prashanth NK, Rajendraswami M, Pallalu D, Castelhano AL, Kates MJ, Blobaum AL, Jones CK, Emmitte KA, Conn PJ, Lindsley CW. Development and kilogram-scale synthesis of mGlu5 negative allosteric modulator VU0424238 (auglurant) Tetrahedron Letters. 58: 3554-3558. DOI: 10.1016/J.Tetlet.2017.07.100 |
0.324 |
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| 2017 |
Garcia-Barrantes PM, McGowan K, Ingram SW, Lindsley CW. One pot synthesis of unsymmetrical ketones from carboxylic and boronic acids via PyClU-mediated acylative Suzuki coupling Tetrahedron Letters. 58: 898-901. DOI: 10.1016/J.Tetlet.2017.01.064 |
0.728 |
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| 2017 |
Jeffries DE, Lindsley CW. A one-pot, multi-component reaction cascade for the rapid synthesis of diversely functionalized heteroaryl methyl substrates Tetrahedron Letters. 58: 112-116. DOI: 10.1016/J.Tetlet.2016.11.120 |
0.307 |
|
| 2016 |
Jeffries DE, Witt JO, McCollum AL, Temple KJ, Hurtado MA, Harp JM, Blobaum AL, Lindsley CW, Hopkins CR. Discovery, characterization and biological evaluation of a novel (R)-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D4R) antagonists. Bioorganic & Medicinal Chemistry Letters. 26: 5757-5764. PMID 28327307 DOI: 10.1016/J.Bmcl.2016.10.049 |
0.681 |
|
| 2016 |
Rook JM, Abe M, Cho HP, Nance KD, Luscombe VB, Adams JJ, Dickerson JW, Remke DH, Garcia-Barrantes PM, Engers DW, Engers JL, Chang S, Foster JJ, Blobaum AL, Niswender CM, ... ... Lindsley CW, et al. Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs. Acs Chemical Neuroscience. PMID 28001356 DOI: 10.1021/Acschemneuro.6B00429 |
0.815 |
|
| 2016 |
Jeffries DE, Lindsley CW. Total Synthesis and Biological Evaluation of Hybrubin A. The Journal of Organic Chemistry. PMID 27966952 DOI: 10.1021/Acs.Joc.6B02534 |
0.353 |
|
| 2016 |
Wood MR, Noetzel MJ, Poslusney MS, Melancon BJ, Tarr JC, Lamsal A, Chang S, Luscombe VB, Weiner RL, Cho HP, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, ... ... Lindsley CW, et al. Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs. Bioorganic & Medicinal Chemistry Letters. PMID 27939174 DOI: 10.1016/J.Bmcl.2016.11.086 |
0.4 |
|
| 2016 |
Borza CM, Su Y, Tran TL, Yu L, Steyns N, Temple KJ, Skwark MJ, Meiler J, Lindsley CW, Hicks BR, Leitinger B, Zent R, Pozzi A. Discoidin domain receptor 1 kinase activity is required for regulating collagen IV synthesis. Matrix Biology : Journal of the International Society For Matrix Biology. PMID 27915093 DOI: 10.1016/J.Matbio.2016.11.009 |
0.648 |
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| 2016 |
Duvernay MT, Temple KJ, Maeng JG, Blobaum AL, Stauffer SR, Lindsley CW, Hamm HE. Contributions of PAR1 and PAR4 to thrombin induced GPIIbIIIa activation in human platelets. Molecular Pharmacology. PMID 27784794 DOI: 10.1124/Mol.116.106666 |
0.672 |
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| 2016 |
Temple KJ, Duvernay MT, Maeng JG, Blobaum AL, Stauffer SR, Hamm HE, Lindsley CW. Identification of the minimum PAR4 inhibitor pharmacophore and optimization of a series of 2-methoxy-6-arylimidazo[2,1-b][1,3,4]thiadiazoles. Bioorganic & Medicinal Chemistry Letters. PMID 27777004 DOI: 10.1016/J.Bmcl.2016.10.020 |
0.675 |
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| 2016 |
Foster DJ, Wilson JM, Remke DH, Mahmood MS, Uddin MJ, Wess J, Patel S, Marnett LJ, Niswender CM, Jones CK, Xiang Z, Lindsley CW, Rook JM, Conn PJ. Antipsychotic-like Effects of M4 Positive Allosteric Modulators Are Mediated by CB2 Receptor-Dependent Inhibition of Dopamine Release. Neuron. PMID 27618677 DOI: 10.1016/J.Neuron.2016.08.017 |
0.351 |
|
| 2016 |
Grannan MD, Mielnik CA, Moran S, Gould RW, Ball JR, Lu Z, Bubser M, Ramsey AJ, Abe M, Cho HP, Nance KD, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW, et al. Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction are Reversed by the Novel M1 PAM VU6004256. Acs Chemical Neuroscience. PMID 27617634 DOI: 10.1021/Acschemneuro.6B00230 |
0.76 |
|
| 2016 |
Bertron JL, Ennis EA, Tarr CJ, Wright J, Dickerson JW, Locuson CW, Blobaum AL, Rook JM, Blakely RD, Lindsley CW. Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. Bioorganic & Medicinal Chemistry Letters. PMID 27575469 DOI: 10.1016/J.Bmcl.2016.08.062 |
0.798 |
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| 2016 |
Geanes AR, Cho HP, Nance KD, McGowan KM, Conn PJ, Jones CK, Meiler J, Lindsley CW. Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes. Bioorganic & Medicinal Chemistry Letters. PMID 27503678 DOI: 10.1016/J.Bmcl.2016.07.071 |
0.764 |
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| 2016 |
Temple KJ, Duvernay MT, Young SE, Wen W, Wu W, Maeng J, Blobaum AL, Stauffer SR, Hamm HE, Lindsley CW. Development of a Series of (1-Benzyl-3-(6-methoxypyrimidin-3-yl)-5-(trifluoromethoxy)-1H-indol-2-yl)methanols as Selective Protease Activated Receptor 4 (PAR4) Antagonists with In Vivo Utility and Activity Against γ-Thrombin. Journal of Medicinal Chemistry. PMID 27482618 DOI: 10.1021/Acs.Jmedchem.6B00928 |
0.667 |
|
| 2016 |
Wood MR, Noetzel MJ, Tarr JC, Rodriguez AL, Lamsal A, Chang S, Foster JJ, Smith E, Chase P, Hodder PS, Engers DW, Niswender CM, Brandon NJ, Wood MW, Duggan ME, ... ... Lindsley CW, et al. Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition. Bioorganic & Medicinal Chemistry Letters. PMID 27476142 DOI: 10.1016/J.Bmcl.2016.07.042 |
0.401 |
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| 2016 |
Garcia-Barrantes PM, Lindsley CW. Total Synthesis of Gombamide A. Organic Letters. PMID 27442228 DOI: 10.1021/Acs.Orglett.6B01825 |
0.753 |
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| 2016 |
Niswender CM, Jones CK, Lin X, Bubser M, Thompson Gray A, Blobaum AL, Engers DW, Rodriguez AL, Loch MT, Daniels JS, Lindsley CW, Hopkins CR, Javitch JA, Conn PJ. Development and antiparkinsonian activity of VU0418506, a selective positive allosteric modulator of metabotropic glutamate receptor 4 homomers without activity at mGlu2/4 heteromers. Acs Chemical Neuroscience. PMID 27441572 DOI: 10.1021/Acschemneuro.6B00036 |
0.338 |
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| 2016 |
Gogliotti RD, Blobaum AL, Morrison RM, Daniels JS, Salovich JM, Cheung YY, Rodriguez AL, Loch MT, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4). Bioorganic & Medicinal Chemistry Letters. PMID 27234146 DOI: 10.1016/J.Bmcl.2016.05.029 |
0.347 |
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| 2016 |
Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, ... ... Lindsley CW, et al. Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core. Bioorganic & Medicinal Chemistry Letters. PMID 27185330 DOI: 10.1016/J.Bmcl.2016.05.010 |
0.395 |
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| 2016 |
Swale DR, Kurata H, Kharade SV, Sheehan JH, Raphemot RR, Voigtritter KR, Figueroa E, Meiler J, Flobaum AL, Lindsley CW, Hopkins CR, Denton JS. ML418: The first selective, sub-micromolar pore blocker of Kir7.1 potassium channels. Acs Chemical Neuroscience. PMID 27184474 DOI: 10.1021/Acschemneuro.6B00111 |
0.766 |
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| 2016 |
Panarese JD, Cho HP, Adams JJ, Nance KD, Garcia-Barrantes PM, Chang S, Morrison RD, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW. Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration. Bioorganic & Medicinal Chemistry Letters. PMID 27173801 DOI: 10.1016/J.Bmcl.2016.04.083 |
0.801 |
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| 2016 |
Gogliotti RD, Engers DW, Garcia-Barrantes PM, Panarese JD, Gentry PR, Blobaum AL, Morrison RD, Daniels JS, Thompson AD, Jones CK, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR. Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy. Bioorganic & Medicinal Chemistry Letters. PMID 27131990 DOI: 10.1016/J.Bmcl.2016.04.041 |
0.755 |
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| 2016 |
Witt JO, McCollum AL, Hurtado MA, Huseman ED, Jeffries DE, Temple KJ, Plumley HC, Blobaum AL, Lindsley CW, Hopkins CR. Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists. Bioorganic & Medicinal Chemistry Letters. PMID 27080176 DOI: 10.1016/J.Bmcl.2016.03.102 |
0.682 |
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| 2016 |
Engers DW, Blobaum AL, Gogliotti RD, Cheung YY, Salovich JM, Garcia-Barrantes PM, Daniels JS, Morrison R, Jones CK, Soars MG, Zhuo X, Hurley J, Macor JE, Bronson JJ, Conn PJ, ... Lindsley CW, et al. Discovery, Synthesis and Pre-Clinical Characterization of N-(3-chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4). Acs Chemical Neuroscience. PMID 27075300 DOI: 10.1021/Acschemneuro.6B00035 |
0.76 |
|
| 2016 |
Garcia-Barrantes PM, Cho HP, Starr TM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Re-exploration of the mGlu1 PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR. Bioorganic & Medicinal Chemistry Letters. PMID 27013388 DOI: 10.1016/J.Bmcl.2016.03.044 |
0.766 |
|
| 2016 |
Felts AS, Rodriguez AL, Morrison RD, Venable DF, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents. Bioorganic & Medicinal Chemistry Letters. PMID 26988308 DOI: 10.1016/J.Bmcl.2016.03.026 |
0.379 |
|
| 2016 |
Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs. Bioorganic & Medicinal Chemistry Letters. PMID 26988302 DOI: 10.1016/J.Bmcl.2016.03.031 |
0.739 |
|
| 2016 |
Lindsley CW, Emmitte KA, Hopkins CR, Bridges TM, Gregory KJ, Niswender CM, Conn PJ. Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors. Chemical Reviews. PMID 26882314 DOI: 10.1021/Acs.Chemrev.5B00656 |
0.337 |
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| 2016 |
Garcia-Barrantes PM, Cho HP, Metts AM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool. Bioorganic & Medicinal Chemistry Letters. PMID 26778256 DOI: 10.1016/J.Bmcl.2015.12.104 |
0.76 |
|
| 2016 |
Garcia-Barrantes PM, Harp JR, Lindsley CW. Total synthesis of actinophenanthroline A Tetrahedron Letters. 57: 2194-2196. DOI: 10.1016/J.Tetlet.2016.04.019 |
0.737 |
|
| 2015 |
Senter TJ, O'Reilly MC, Chong KM, Sulikowski GA, Lindsley CW. A general, enantioselective synthesis of N-alkyl terminal aziridines and C2-functionalized azetidines via organocatalysis. Tetrahedron Letters. 56: 1276-1279. PMID 26834294 DOI: 10.1016/J.Tetlet.2015.01.140 |
0.786 |
|
| 2015 |
Conde-Ceide S, Alcázar J, Alonso de Diego SA, López S, Martín-Martín ML, Martínez-Viturro CM, Pena MA, Tong HM, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, ... ... Lindsley CW, et al. Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia. Bioorganic & Medicinal Chemistry Letters. PMID 26684851 DOI: 10.1016/J.Bmcl.2015.11.098 |
0.364 |
|
| 2015 |
Felts AS, Rodriguez AL, Smith KA, Engers JL, Morrison RD, Byers FW, Blobaum AL, Locuson CW, Chang S, Venable DF, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Emmitte KA. Design of 4-oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as selective negative allosteric modulators of metabotropic glutamate receptor subtype 2. Journal of Medicinal Chemistry. PMID 26524606 DOI: 10.1021/Acs.Jmedchem.5B01371 |
0.379 |
|
| 2015 |
Pancani T, Foster DJ, Moehle MS, Bichell TJ, Bradley E, Bridges TM, Klar R, Poslusney M, Rook JM, Daniels JS, Niswender CM, Jones CK, Wood MR, Bowman AB, Lindsley CW, et al. Allosteric activation of M4 muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice. Proceedings of the National Academy of Sciences of the United States of America. 112: 14078-83. PMID 26508634 DOI: 10.1073/Pnas.1512812112 |
0.332 |
|
| 2015 |
Nickols HH, Yuh JP, Gregory KJ, Morrison RD, Bates BS, Stauffer SR, Emmitte KA, Bubser M, Peng W, Nedelcovych MT, Thompson A, Lv X, Xiang Z, Daniels JS, Niswender CM, ... Lindsley CW, et al. VU0477573: Partial negative allosteric modulator of the subtype 5 metabotropic glutamate receptor with in vivo efficacy. The Journal of Pharmacology and Experimental Therapeutics. PMID 26503377 DOI: 10.1124/Jpet.115.226597 |
0.355 |
|
| 2015 |
Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core. Bioorganic & Medicinal Chemistry Letters. 25: 5107-10. PMID 26476971 DOI: 10.1016/J.Bmcl.2015.10.013 |
0.762 |
|
| 2015 |
Malosh C, Turlington M, Bridges TM, Rook JM, Noetzel MJ, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martínez-Viturro CM, Piedrafita M, Sánchez-Casado MR, Macdonald GJ, ... ... Lindsley CW, et al. Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators. Bioorganic & Medicinal Chemistry Letters. PMID 26475522 DOI: 10.1016/J.Bmcl.2015.10.009 |
0.342 |
|
| 2015 |
Wu Y, Stauffer SR, Stanfield RL, Tapia PH, Ursu O, Fisher GW, Szent-Gyorgyi C, Evangelisti A, Waller A, Strouse JJ, Carter MB, Bologa C, Gouveia K, Poslusney M, Waggoner AS, ... Lindsley CW, et al. Discovery of Small-Molecule Nonfluorescent Inhibitors of Fluorogen-Fluorogen Activating Protein Binding Pair. Journal of Biomolecular Screening. PMID 26442911 DOI: 10.1177/1087057115609145 |
0.322 |
|
| 2015 |
Garcia-Barrantes PM, Cho HP, Niswender CM, Byers FW, Locuson CW, Blobaum AL, Xiang Z, Rook JM, Conn PJ, Lindsley CW. Development of novel, CNS penetrant positive allosteric modulators for the metabotropic glutamate receptor subtype 1 (mGlu1), based on an N-(3-chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide scaffold, that potentiate both wild type and mutant mGlu1 receptors found in schizophrenics. Journal of Medicinal Chemistry. PMID 26426481 DOI: 10.1021/Acs.Jmedchem.5B00727 |
0.767 |
|
| 2015 |
Engers JL, Rodriguez AL, Konkol LC, Morrison RD, Thompson AD, Byers FW, Blobaum AL, Chang S, Venable DF, Loch MT, Niswender CM, Daniels JS, Jones CK, Conn PJ, Lindsley CW, et al. Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. Journal of Medicinal Chemistry. 58: 7485-500. PMID 26335039 DOI: 10.1021/Acs.Jmedchem.5B01005 |
0.351 |
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| 2015 |
Gould RW, Amato RJ, Bubser M, Joffe ME, Nedelcovych MT, Thompson AD, Nickols HH, Yuh JP, Zhan X, Felts AS, Rodriguez AL, Morrison RD, Byers FW, Rook JM, Daniels JS, ... ... Lindsley CW, et al. Partial mGlu5 Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 26315507 DOI: 10.1038/Npp.2015.265 |
0.322 |
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| 2015 |
Brogan JT, Stoops SL, Brady S, An H, Weaver C, Daniels JS, Beauchamp RD, Lindsley CW, Waterson AG. Optimization of a small molecule probe that restores e-cadherin expression. Bioorganic & Medicinal Chemistry Letters. 25: 4260-4. PMID 26299347 DOI: 10.1016/J.Bmcl.2015.07.104 |
0.772 |
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| 2015 |
Blobaum AL, Byers FW, Bridges TM, Locuson CW, Conn PJ, Lindsley CW, Daniels JS. A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 43: 1718-26. PMID 26265743 DOI: 10.1124/Dmd.115.064006 |
0.319 |
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| 2015 |
Zhou Y, Malosh C, Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, ... ... Lindsley CW, et al. Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound. Bioorganic & Medicinal Chemistry Letters. PMID 26183084 DOI: 10.1016/J.Bmcl.2015.06.096 |
0.34 |
|
| 2015 |
Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Garcia-Barrantes PM, Lavreysen H, Mackie C, Vinson PN, Rook JM, Bridges TM, Daniels JS, Megens A, Langlois X, Drinkenburg WH, Ahnaou A, Niswender CM, ... ... Lindsley CW, et al. Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia. Acs Medicinal Chemistry Letters. 6: 716-20. PMID 26157544 DOI: 10.1021/Acsmedchemlett.5B00181 |
0.76 |
|
| 2015 |
Ghoshal A, Rook JM, Dickerson JW, Roop GN, Morrison RD, Jalan-Sakrikar N, Lamsal A, Noetzel MJ, Poslusney MS, Wood MR, Melancon BJ, Stauffer SR, Xiang Z, Daniels JS, Niswender CM, ... ... Lindsley CW, et al. Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 26108886 DOI: 10.1038/Npp.2015.189 |
0.345 |
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| 2015 |
An H, Stoops SL, Deane NG, Zhu J, Zi J, Weaver C, Waterson AG, Zijlstra A, Lindsley CW, Beauchamp RD. Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition. Oncotarget. PMID 26082441 DOI: 10.18632/Oncotarget.4473 |
0.764 |
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| 2015 |
Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, et al. Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes. Cell. 161: 1252-1265. PMID 26046436 DOI: 10.1016/J.Cell.2015.05.023 |
0.446 |
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| 2015 |
Senter T, Gogliotti RD, Han C, Locuson CW, Morrison R, Daniels JS, Cierpicki T, Grembecka J, Lindsley CW, Stauffer SR. Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility. Bioorganic & Medicinal Chemistry Letters. 25: 2720-5. PMID 25987377 DOI: 10.1016/J.Bmcl.2015.04.026 |
0.794 |
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| 2015 |
Rook JM, Xiang Z, Lv X, Ghoshal A, Dickerson JW, Bridges TM, Johnson KA, Foster DJ, Gregory KJ, Vinson PN, Thompson AD, Byun N, Collier RL, Bubser M, Nedelcovych MT, ... ... Lindsley CW, et al. Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents. Neuron. 86: 1029-40. PMID 25937172 DOI: 10.1016/J.Neuron.2015.03.063 |
0.318 |
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| 2015 |
Smith E, Chase P, Niswender CM, Utley TJ, Sheffler DJ, Noetzel MJ, Lamsal A, Wood MR, Conn PJ, Lindsley CW, Madoux F, Acosta M, Scampavia L, Spicer T, Hodder P. Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4). Journal of Biomolecular Screening. PMID 25877150 DOI: 10.1177/1087057115581770 |
0.395 |
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| 2015 |
Bollinger SR, Engers DW, Ennis EA, Wright J, Locuson CW, Lindsley CW, Blakely RD, Hopkins CR. Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. Bioorganic & Medicinal Chemistry Letters. 25: 1757-60. PMID 25801932 DOI: 10.1016/J.Bmcl.2015.02.058 |
0.408 |
|
| 2015 |
Martín-Martín ML, Bartolomé-Nebreda JM, Conde-Ceide S, Alonso de Diego SA, López S, Martínez-Viturro CM, Tong HM, Lavreysen H, Macdonald GJ, Steckler T, Mackie C, Bridges TM, Daniels JS, Niswender CM, Noetzel MJ, ... ... Lindsley CW, et al. Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). Bioorganic & Medicinal Chemistry Letters. 25: 1310-7. PMID 25683622 DOI: 10.1016/J.Bmcl.2015.01.038 |
0.364 |
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| 2015 |
Walker AG, Wenthur CJ, Xiang Z, Rook JM, Emmitte KA, Niswender CM, Lindsley CW, Conn PJ. Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction. Proceedings of the National Academy of Sciences of the United States of America. 112: 1196-201. PMID 25583490 DOI: 10.1073/Pnas.1416196112 |
0.693 |
|
| 2015 |
Ennis EA, Wright J, Retzlaff CL, McManus OB, Lin Z, Huang X, Wu M, Li M, Daniels JS, Lindsley CW, Hopkins CR, Blakely RD. Identification and characterization of ML352: a novel, noncompetitive inhibitor of the presynaptic choline transporter. Acs Chemical Neuroscience. 6: 417-27. PMID 25560927 DOI: 10.1021/Cn5001809 |
0.322 |
|
| 2015 |
Kurata H, Gentry PR, Kokubo M, Cho HP, Bridges TM, Niswender CM, Byers FW, Wood MR, Daniels JS, Conn PJ, Lindsley CW. Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges. Bioorganic & Medicinal Chemistry Letters. 25: 690-4. PMID 25542588 DOI: 10.1016/J.Bmcl.2014.11.082 |
0.377 |
|
| 2015 |
Han C, Chatterjee A, Noetzel MJ, Panarese JD, Smith E, Chase P, Hodder P, Niswender C, Conn PJ, Lindsley CW, Stauffer SR. Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators. Bioorganic & Medicinal Chemistry Letters. 25: 384-8. PMID 25435150 DOI: 10.1016/J.Bmcl.2014.11.011 |
0.364 |
|
| 2015 |
Scott SA, Spencer CT, O'Reilly MC, Brown KA, Lavieri RR, Cho CH, Jung DI, Larock RC, Brown HA, Lindsley CW. Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes. Acs Chemical Biology. 10: 421-32. PMID 25384256 DOI: 10.1021/Cb500828M |
0.741 |
|
| 2015 |
Rook JM, Tantawy MN, Ansari MS, Felts AS, Stauffer SR, Emmitte KA, Kessler RM, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ. Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 40: 755-65. PMID 25241804 DOI: 10.1038/Npp.2014.245 |
0.321 |
|
| 2015 |
Wen W, Wang Y, Li Z, Tseng PY, McManus OB, Wu M, Li M, Lindsley CW, Dong X, Hopkins CR. Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1. Chemmedchem. 10: 57-61. PMID 25209672 DOI: 10.1002/Cmdc.201402277 |
0.341 |
|
| 2015 |
An H, Deane N, Stoops S, Zhu J, Waterson A, Zijlstra A, Lindsley C, Beauchamp RD. Abstract 4097: Small molecule mediated transcriptional derepression of E-cadherin and inhibition of epithelial to mesenchymal transition Cancer Research. 75: 4097-4097. DOI: 10.1158/1538-7445.Am2015-4097 |
0.78 |
|
| 2015 |
Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Garcia-Barrantes PM, Lavreysen H, Mackie C, Vinson PN, Rook JM, Bridges TM, Daniels JS, Megens A, Langlois X, Drinkenburg WH, Ahnaou A, Niswender CM, ... ... Lindsley CW, et al. Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia Acs Medicinal Chemistry Letters. 6: 716-720. DOI: 10.1021/acsmedchemlett.5b00181 |
0.708 |
|
| 2015 |
Senter TJ, O'Reilly MC, Chong KM, Sulikowski GA, Lindsley CW. A general, enantioselective synthesis of N-alkyl terminal aziridines and C2-functionalized azetidines via organocatalysis Tetrahedron Letters. 56: 1276-1279. DOI: 10.1016/j.tetlet.2015.01.140 |
0.778 |
|
| 2014 |
O'Reilly MC, Scott SA, Brown HA, Lindsley CW. Further evaluation of novel structural modifications to scaffolds that engender PLD isoform selective inhibition. Bioorganic & Medicinal Chemistry Letters. 24: 5553-7. PMID 25466173 DOI: 10.1016/J.Bmcl.2014.11.017 |
0.356 |
|
| 2014 |
Morris LC, Nance KD, Gentry PR, Days EL, Weaver CD, Niswender CM, Thompson AD, Jones CK, Locuson CW, Morrison RD, Daniels JS, Niswender KD, Lindsley CW. Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM). Journal of Medicinal Chemistry. 57: 10192-7. PMID 25423411 DOI: 10.1021/Jm501375C |
0.738 |
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| 2014 |
Wen W, Wu W, Weaver CD, Lindsley CW. Discovery of potent and selective GIRK1/2 modulators via 'molecular switches' within a series of 1-(3-cyclopropyl-1-phenyl-1H-pyrazol-5-yl)ureas. Bioorganic & Medicinal Chemistry Letters. 24: 5102-6. PMID 25264075 DOI: 10.1016/J.Bmcl.2014.08.061 |
0.38 |
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| 2014 |
Jalan-Sakrikar N, Field JR, Klar R, Mattmann ME, Gregory KJ, Zamorano R, Engers DW, Bollinger SR, Weaver CD, Days EL, Lewis LM, Utley TJ, Hurtado M, Rigault D, Acher F, ... ... Lindsley CW, et al. Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7. Acs Chemical Neuroscience. 5: 1221-37. PMID 25225882 DOI: 10.1021/Cn500153Z |
0.337 |
|
| 2014 |
Berry CB, Bubser M, Jones CK, Hayes JP, Wepy JA, Locuson CW, Daniels JS, Lindsley CW, Hopkins CR. Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity. Acs Medicinal Chemistry Letters. 5: 1060-4. PMID 25221667 DOI: 10.1021/Ml500267C |
0.332 |
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| 2014 |
O'Reilly MC, Oguin TH, Scott SA, Thomas PG, Locuson CW, Morrison RD, Daniels JS, Brown HA, Lindsley CW. Discovery of a highly selective PLD2 inhibitor (ML395): a new probe with improved physiochemical properties and broad-spectrum antiviral activity against influenza strains. Chemmedchem. 9: 2633-7. PMID 25210004 DOI: 10.1002/Cmdc.201402333 |
0.308 |
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| 2014 |
Lindsley CW. 2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites. Journal of Medicinal Chemistry. 57: 7485-98. PMID 25180768 DOI: 10.1021/Jm5011786 |
0.343 |
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| 2014 |
Conn PJ, Lindsley CW, Meiler J, Niswender CM. Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders. Nature Reviews. Drug Discovery. 13: 692-708. PMID 25176435 DOI: 10.1038/Nrd4308 |
0.344 |
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| 2014 |
Wen W, Young SE, Duvernay MT, Schulte ML, Nance KD, Melancon BJ, Engers J, Locuson CW, Wood MR, Daniels JS, Wu W, Lindsley CW, Hamm HE, Stauffer SR. Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354. Bioorganic & Medicinal Chemistry Letters. 24: 4708-13. PMID 25176330 DOI: 10.1016/J.Bmcl.2014.08.021 |
0.797 |
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| 2014 |
Gentry PR, Kokubo M, Bridges TM, Noetzel MJ, Cho HP, Lamsal A, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380). Journal of Medicinal Chemistry. 57: 7804-10. PMID 25147929 DOI: 10.1021/Jm500995Y |
0.397 |
|
| 2014 |
Bubser M, Bridges TM, Dencker D, Gould RW, Grannan M, Noetzel MJ, Lamsal A, Niswender CM, Daniels JS, Poslusney MS, Melancon BJ, Tarr JC, Byers FW, Wess J, Duggan ME, ... ... Lindsley CW, et al. Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents. Acs Chemical Neuroscience. 5: 920-42. PMID 25137629 DOI: 10.1021/Cn500128B |
0.379 |
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| 2014 |
Cho HP, Garcia-Barrantes PM, Brogan JT, Hopkins CR, Niswender CM, Rodriguez AL, Venable DF, Morrison RD, Bubser M, Daniels JS, Jones CK, Conn PJ, Lindsley CW. Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics. Acs Chemical Biology. 9: 2334-46. PMID 25137254 DOI: 10.1021/Cb500560H |
0.751 |
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| 2014 |
Turlington M, Noetzel MJ, Bridges TM, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Tong HM, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, ... Lindsley CW, et al. Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency. Bioorganic & Medicinal Chemistry Letters. 24: 3641-6. PMID 24961642 DOI: 10.1016/J.Bmcl.2014.04.087 |
0.374 |
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| 2014 |
Turlington M, Malosh C, Jacobs J, Manka JT, Noetzel MJ, Vinson PN, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, MartÃn-MartÃn ML, Tong HM, López S, ... ... Lindsley CW, et al. Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGluâ‚…). Journal of Medicinal Chemistry. 57: 5620-37. PMID 24914612 DOI: 10.1021/Jm500259Z |
0.366 |
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| 2014 |
Cho HP, Engers DW, Venable DF, Niswender CM, Lindsley CW, Conn PJ, Emmitte KA, Rodriguez AL. A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors. Acs Chemical Neuroscience. 5: 597-610. PMID 24798819 DOI: 10.1021/Cn5000343 |
0.366 |
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| 2014 |
Wenthur CJ, Morrison RD, Daniels JS, Conn PJ, Lindsley CW. Synthesis and SAR of substituted pyrazolo[1,5-a]quinazolines as dual mGlu(2)/mGlu(3) NAMs. Bioorganic & Medicinal Chemistry Letters. 24: 2693-8. PMID 24794112 DOI: 10.1016/J.Bmcl.2014.04.051 |
0.745 |
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| 2014 |
Gentry PR, Kokubo M, Bridges TM, Cho HP, Smith E, Chase P, Hodder PS, Utley TJ, Rajapakse A, Byers F, Niswender CM, Morrison RD, Daniels JS, Wood MR, Conn PJ, ... Lindsley CW, et al. Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe. Chemmedchem. 9: 1677-82. PMID 24692176 DOI: 10.1002/Cmdc.201402051 |
0.407 |
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| 2014 |
Gregory KJ, Nguyen ED, Malosh C, Mendenhall JL, Zic JZ, Bates BS, Noetzel MJ, Squire EF, Turner EM, Rook JM, Emmitte KA, Stauffer SR, Lindsley CW, Meiler J, Conn PJ. Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site. Acs Chemical Neuroscience. 5: 282-95. PMID 24528109 DOI: 10.1021/Cn400225X |
0.321 |
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| 2014 |
Pancani T, Bolarinwa C, Smith Y, Lindsley CW, Conn PJ, Xiang Z. M4 mAChR-mediated modulation of glutamatergic transmission at corticostriatal synapses. Acs Chemical Neuroscience. 5: 318-24. PMID 24528004 DOI: 10.1021/Cn500003Z |
0.363 |
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| 2014 |
Morris LC, Days EL, Turney M, Mi D, Lindsley CW, Weaver CD, Niswender KD. A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptors. Journal of Biomolecular Screening. 19: 847-858. PMID 24525870 DOI: 10.1177/1087057114520971 |
0.327 |
|
| 2014 |
He S, Senter TJ, Pollock J, Han C, Upadhyay SK, Purohit T, Gogliotti RD, Lindsley CW, Cierpicki T, Stauffer SR, Grembecka J. High-affinity small-molecule inhibitors of the menin-mixed lineage leukemia (MLL) interaction closely mimic a natural protein-protein interaction. Journal of Medicinal Chemistry. 57: 1543-56. PMID 24472025 DOI: 10.1021/Jm401868D |
0.793 |
|
| 2014 |
Sheffler DJ, Nedelovych MT, Williams R, Turner SC, Duerk BB, Robbins MR, Jadhav SB, Niswender CM, Jones CK, Conn PJ, Daniels RN, Lindsley CW. Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: development of a [3.3.0]-based series and other piperidine bioisosteres. Bioorganic & Medicinal Chemistry Letters. 24: 1062-6. PMID 24462664 DOI: 10.1016/J.Bmcl.2014.01.011 |
0.766 |
|
| 2014 |
Jones CK, Sheffler DJ, Williams R, Jadhav SB, Felts AS, Morrison RD, Niswender CM, Daniels JS, Conn PJ, Lindsley CW. Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead. Bioorganic & Medicinal Chemistry Letters. 24: 1067-70. PMID 24461352 DOI: 10.1016/J.Bmcl.2014.01.013 |
0.363 |
|
| 2014 |
Byun NE, Grannan M, Bubser M, Barry RL, Thompson A, Rosanelli J, Gowrishankar R, Kelm ND, Damon S, Bridges TM, Melancon BJ, Tarr JC, Brogan JT, Avison MJ, Deutch AY, ... ... Lindsley CW, et al. Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 39: 1578-93. PMID 24442096 DOI: 10.1038/Npp.2014.2 |
0.387 |
|
| 2014 |
Macdonald GJ, Lindsley CW. A unique industrial-academic collaboration towards the next generation of schizophrenia therapeutics. Current Topics in Medicinal Chemistry. 14: 304-12. PMID 24283972 DOI: 10.2174/1568026613666131127154443 |
0.305 |
|
| 2014 |
Wenthur CJ, Gentry PR, Mathews TP, Lindsley CW. Drugs for allosteric sites on receptors. Annual Review of Pharmacology and Toxicology. 54: 165-84. PMID 24111540 DOI: 10.1146/Annurev-Pharmtox-010611-134525 |
0.716 |
|
| 2014 |
Wenthur CJ, Bennett MR, Lindsley CW. Classics in chemical neuroscience: Fluoxetine (Prozac) Acs Chemical Neuroscience. 5: 14-23. DOI: 10.1021/Cn400186J |
0.689 |
|
| 2014 |
Schulte ML, Turlington ML, Phatak SS, Harp JM, Stauffer SR, Lindsley CW. ChemInform Abstract: Total Synthesis of Stemaphylline N-Oxide (II) and Related C9a-Epimeric Analogues (III) and (IV). Cheminform. 45: no-no. DOI: 10.1002/chin.201404206 |
0.555 |
|
| 2013 |
Aldrich LN, Berry CB, Bates BS, Konkol LC, So M, Lindsley CW. Towards the Total Synthesis of Marineosin A: Construction of the Macrocyclic Pyrrole and an Advanced, Functionalized Spiroaminal Model. European Journal of Organic Chemistry. 2013. PMID 24415906 DOI: 10.1002/Ejoc.201300643 |
0.792 |
|
| 2013 |
Lindsley CW, Stauffer SR. Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012). Pharmaceutical Patent Analyst. 2: 93-108. PMID 24236973 DOI: 10.4155/Ppa.12.82 |
0.317 |
|
| 2013 |
Gentry PR, Kokubo M, Bridges TM, Kett NR, Harp JM, Cho HP, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Wood MR, Lindsley CW. Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375). Journal of Medicinal Chemistry. 56: 9351-5. PMID 24164599 DOI: 10.1021/Jm4013246 |
0.374 |
|
| 2013 |
Turlington M, Chun A, Tomar S, Eggler A, Grum-Tokars V, Jacobs J, Daniels JS, Dawson E, Saldanha A, Chase P, Baez-Santos YM, Lindsley CW, Hodder P, Mesecar AD, Stauffer SR. Discovery of N-(benzo[1,2,3]triazol-1-yl)-N-(benzyl)acetamido)phenyl) carboxamides as severe acute respiratory syndrome coronavirus (SARS-CoV) 3CLpro inhibitors: identification of ML300 and noncovalent nanomolar inhibitors with an induced-fit binding. Bioorganic & Medicinal Chemistry Letters. 23: 6172-7. PMID 24080461 DOI: 10.1016/J.Bmcl.2013.08.112 |
0.311 |
|
| 2013 |
Felts AS, Rodriguez AL, Morrison RD, Venable DF, Manka JT, Bates BS, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorganic & Medicinal Chemistry Letters. 23: 5779-85. PMID 24074843 DOI: 10.1016/J.Bmcl.2013.09.001 |
0.334 |
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| 2013 |
Melancon BJ, Tarr JC, Panarese JD, Wood MR, Lindsley CW. Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease. Drug Discovery Today. 18: 1185-99. PMID 24051397 DOI: 10.1016/J.Drudis.2013.09.005 |
0.382 |
|
| 2013 |
Turlington M, Noetzel MJ, Chun A, Zhou Y, Gogliotti RD, Nguyen ED, Gregory KJ, Vinson PN, Rook JM, Gogi KK, Xiang Z, Bridges TM, Daniels JS, Jones C, Niswender CM, ... ... Lindsley CW, et al. Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254). Journal of Medicinal Chemistry. 56: 7976-96. PMID 24050755 DOI: 10.1021/Jm401028T |
0.351 |
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| 2013 |
Engers DW, Lindsley CW. Allosteric modulation of Class C GPCRs: a novel approach for the treatment of CNS disorders. Drug Discovery Today. Technologies. 10: e269-76. PMID 24050278 DOI: 10.1016/J.Ddtec.2012.10.007 |
0.314 |
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| 2013 |
Wenthur CJ, Lindsley CW. Classics in chemical neuroscience: clozapine. Acs Chemical Neuroscience. 4: 1018-25. PMID 24047509 DOI: 10.1021/Cn400121Z |
0.69 |
|
| 2013 |
Blobaum AL, Bridges TM, Byers FW, Turlington ML, Mattmann ME, Morrison RD, Mackie C, Lavreysen H, Bartolomé JM, Macdonald GJ, Steckler T, Jones CK, Niswender CM, Conn PJ, Lindsley CW, et al. Heterotropic activation of the midazolam hydroxylase activity of CYP3A by a positive allosteric modulator of mGlu5: in vitro to in vivo translation and potential impact on clinically relevant drug-drug interactions. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 41: 2066-75. PMID 24003250 DOI: 10.1124/Dmd.113.052662 |
0.347 |
|
| 2013 |
Gregory KJ, Herman EJ, Ramsey AJ, Hammond AS, Byun NE, Stauffer SR, Manka JT, Jadhav S, Bridges TM, Weaver CD, Niswender CM, Steckler T, Drinkenburg WH, Ahnaou A, Lavreysen H, ... ... Lindsley CW, et al. N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement. The Journal of Pharmacology and Experimental Therapeutics. 347: 438-57. PMID 23965381 DOI: 10.1124/Jpet.113.206623 |
0.33 |
|
| 2013 |
Schulte ML, Turlington ML, Phatak SS, Harp JM, Stauffer SR, Lindsley CW. Total synthesis of stemaphylline N-oxide and related C9a-epimeric analogues. Chemistry (Weinheim An Der Bergstrasse, Germany). 19: 11847-52. PMID 23956045 DOI: 10.1002/Chem.201302669 |
0.605 |
|
| 2013 |
Bartolomé-Nebreda JM, Conde-Ceide S, Delgado F, Iturrino L, Pastor J, Pena MÃ, Trabanco AA, Tresadern G, Wassvik CM, Stauffer SR, Jadhav S, Gogi K, Vinson PN, Noetzel MJ, Days E, ... ... Lindsley CW, et al. Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor. Journal of Medicinal Chemistry. 56: 7243-59. PMID 23947773 DOI: 10.1021/Jm400650W |
0.367 |
|
| 2013 |
Manka JT, Rodriguez AL, Morrison RD, Venable DF, Cho HP, Blobaum AL, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1. Bioorganic & Medicinal Chemistry Letters. 23: 5091-6. PMID 23932792 DOI: 10.1016/J.Bmcl.2013.07.029 |
0.346 |
|
| 2013 |
Ramos-Hunter SJ, Engers DW, Kaufmann K, Du Y, Lindsley CW, Weaver CD, Sulikowski GA. Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators. Bioorganic & Medicinal Chemistry Letters. 23: 5195-8. PMID 23916258 DOI: 10.1016/J.Bmcl.2013.07.002 |
0.333 |
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| 2013 |
Wen W, Wu W, Romaine IM, Kaufmann K, Du Y, Sulikowski GA, Weaver CD, Lindsley CW. Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors. Bioorganic & Medicinal Chemistry Letters. 23: 4562-6. PMID 23838260 DOI: 10.1016/J.Bmcl.2013.06.023 |
0.351 |
|
| 2013 |
Bridges TM, Rook JM, Noetzel MJ, Morrison RD, Zhou Y, Gogliotti RD, Vinson PN, Xiang Z, Jones CK, Niswender CM, Lindsley CW, Stauffer SR, Conn PJ, Daniels JS. Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 41: 1703-14. PMID 23821185 DOI: 10.1124/Dmd.113.052084 |
0.369 |
|
| 2013 |
Young SE, Duvernay MT, Schulte ML, Lindsley CW, Hamm HE. Synthesis of indole derived protease-activated receptor 4 antagonists and characterization in human platelets. Plos One. 8: e65528. PMID 23776495 DOI: 10.1371/Journal.Pone.0065528 |
0.669 |
|
| 2013 |
Lovell KM, Felts AS, Rodriguez AL, Venable DF, Cho HP, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorganic & Medicinal Chemistry Letters. 23: 3713-8. PMID 23727046 DOI: 10.1016/J.Bmcl.2013.05.020 |
0.326 |
|
| 2013 |
Wenthur CJ, Morrison R, Felts AS, Smith KA, Engers JL, Byers FW, Daniels JS, Emmitte KA, Conn PJ, Lindsley CW. Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM). Journal of Medicinal Chemistry. 56: 5208-12. PMID 23718281 DOI: 10.1021/Jm400439T |
0.713 |
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| 2013 |
Engers DW, Frist AY, Lindsley CW, Hong CC, Hopkins CR. Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorganic & Medicinal Chemistry Letters. 23: 3248-52. PMID 23639540 DOI: 10.1016/J.Bmcl.2013.03.113 |
0.371 |
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| 2013 |
Panarese JD, Konkol LC, Berry CB, Bates BS, Aldrich LN, Lindsley CW. Spiroaminal Model Systems of the Marineosins with Final Step Pyrrole Incorporation. Tetrahedron Letters. 54: 2231-2234. PMID 23606772 DOI: 10.1016/J.Tetlet.2013.02.059 |
0.779 |
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| 2013 |
Gentry PR, Bridges TM, Lamsal A, Vinson PN, Smith E, Chase P, Hodder PS, Engers JL, Niswender CM, Daniels JS, Conn PJ, Wood MR, Lindsley CW. Discovery of ML326: The first sub-micromolar, selective M5 PAM. Bioorganic & Medicinal Chemistry Letters. 23: 2996-3000. PMID 23562060 DOI: 10.1016/J.Bmcl.2013.03.032 |
0.348 |
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| 2013 |
Senter TJ, Schulte ML, Konkol LC, Wadzinski TE, Lindsley CW. A General, Enantioselective Synthesis of 1-Azabicyclo[m.n.0]alkane Ring Systems. Tetrahedron Letters. 54: 1645-1648. PMID 23459400 DOI: 10.1016/J.Tetlet.2013.01.041 |
0.797 |
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| 2013 |
Gregory KJ, Nguyen ED, Reiff SD, Squire EF, Stauffer SR, Lindsley CW, Meiler J, Conn PJ. Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology. Molecular Pharmacology. 83: 991-1006. PMID 23444015 DOI: 10.1124/Mol.112.083949 |
0.321 |
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| 2013 |
Poslusney MS, Melancon BJ, Gentry PR, Sheffler DJ, Bridges TM, Utley TJ, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR. Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule. Bioorganic & Medicinal Chemistry Letters. 23: 1860-4. PMID 23416001 DOI: 10.1016/J.Bmcl.2013.01.017 |
0.389 |
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| 2013 |
Noetzel MJ, Gregory KJ, Vinson PN, Manka JT, Stauffer SR, Lindsley CW, Niswender CM, Xiang Z, Conn PJ. A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias tomGlu5 signaling Molecular Pharmacology. 83: 835-847. PMID 23348500 DOI: 10.1124/Mol.112.082891 |
0.323 |
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| 2013 |
Melancon BJ, Poslusney MS, Gentry PR, Tarr JC, Sheffler DJ, Mattmann ME, Bridges TM, Utley TJ, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR. Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule. Bioorganic & Medicinal Chemistry Letters. 23: 412-6. PMID 23237839 DOI: 10.1016/J.Bmcl.2012.11.092 |
0.394 |
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| 2013 |
Jacobs J, Grum-Tokars V, Zhou Y, Turlington M, Saldanha SA, Chase P, Eggler A, Dawson ES, Baez-Santos YM, Tomar S, Mielech AM, Baker SC, Lindsley CW, Hodder P, Mesecar A, et al. Discovery, synthesis, and structure-based optimization of a series of N-(tert-butyl)-2-(N-arylamido)-2-(pyridin-3-yl) acetamides (ML188) as potent noncovalent small molecule inhibitors of the severe acute respiratory syndrome coronavirus (SARS-CoV) 3CL protease. Journal of Medicinal Chemistry. 56: 534-46. PMID 23231439 DOI: 10.1021/Jm301580N |
0.324 |
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| 2013 |
Downey JD, Saleh SA, Bridges TM, Morrison RD, Daniels JS, Lindsley CW, Breyer RM. Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere. Bioorganic & Medicinal Chemistry Letters. 23: 37-41. PMID 23218714 DOI: 10.1016/J.Bmcl.2012.11.046 |
0.361 |
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| 2013 |
Sheffler DJ, Sevel C, Le U, Lovell KM, Tarr JC, Carrington SJ, Cho HP, Digby GJ, Niswender CM, Conn PJ, Hopkins CR, Wood MR, Lindsley CW. Further exploration of Mâ‚ allosteric agonists: subtle structural changes abolish Mâ‚ allosteric agonism and result in pan-mAChR orthosteric antagonism. Bioorganic & Medicinal Chemistry Letters. 23: 223-7. PMID 23200253 DOI: 10.1016/J.Bmcl.2012.10.132 |
0.362 |
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| 2013 |
Le U, Melancon BJ, Bridges TM, Vinson PN, Utley TJ, Lamsal A, Rodriguez AL, Venable D, Sheffler DJ, Jones CK, Blobaum AL, Wood MR, Daniels JS, Conn PJ, Niswender CM, ... Lindsley CW, et al. Discovery of a selective Mâ‚„ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorganic & Medicinal Chemistry Letters. 23: 346-50. PMID 23177787 DOI: 10.1016/J.Bmcl.2012.10.073 |
0.377 |
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| 2013 |
Rook JM, Noetzel MJ, Pouliot WA, Bridges TM, Vinson PN, Cho HP, Zhou Y, Gogliotti RD, Manka JT, Gregory KJ, Stauffer SR, Dudek FE, Xiang Z, Niswender CM, Daniels JS, ... ... Lindsley CW, et al. Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biological Psychiatry. 73: 501-9. PMID 23140665 DOI: 10.1016/J.Biopsych.2012.09.012 |
0.345 |
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| 2013 |
Lindsley C. GlyT1 - Up from the Ashes. The importance of not condemning a mechanism based on a single chemotype. Acs Chemical Neuroscience. 1: 165-6. PMID 22778822 DOI: 10.1021/Cn100017A |
0.312 |
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| 2013 |
Lindsley C. Screening and beyond: new opportunities to advance neuroscience discovery. Acs Chemical Neuroscience. 1: 84. PMID 22778818 DOI: 10.1021/Cn1000028 |
0.344 |
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| 2013 |
Downey JD, Saleh SA, Bridges TM, Morrison RD, Daniels JS, Lindsley CW, Breyer RM. Corrigendum to “Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere” [Bioorg. Med. Chem. Lett. 23 (2013) 37–41] Bioorganic & Medicinal Chemistry Letters. 23: 6939. DOI: 10.1016/J.Bmcl.2013.10.023 |
0.348 |
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| 2013 |
Schulte ML, Lindsley CW. Tropane-Based Alkaloids as Muscarinic Antagonists for the Treatment of Asthma, Obstructive Pulmonary Disease, and Motion Sickness Bioactive Heterocyclic Compound Classes: Pharmaceuticals. 21-36. DOI: 10.1002/9783527664450.ch2 |
0.543 |
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| 2012 |
Digby GJ, Utley TJ, Lamsal A, Sevel C, Sheffler DJ, Lebois EP, Bridges TM, Wood MR, Niswender CM, Lindsley CW, Conn PJ. Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode. Acs Chemical Neuroscience. 3: 1025-36. PMID 23259038 DOI: 10.1021/Cn300103E |
0.809 |
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| 2012 |
Lindsley CW. ACS chemical neuroscience and neuroscience drug discovery as 2012 comes to a close Acs Chemical Neuroscience. 3: 988. PMID 23259032 DOI: 10.1021/Cn300221H |
0.311 |
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| 2012 |
Tarr JC, Turlington ML, Reid PR, Utley TJ, Sheffler DJ, Cho HP, Klar R, Pancani T, Klein MT, Bridges TM, Morrison RD, Blobaum AL, Xiang Z, Daniels JS, Niswender CM, ... ... Lindsley CW, et al. Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169. Acs Chemical Neuroscience. 3: 884-95. PMID 23173069 DOI: 10.1021/Cn300068S |
0.41 |
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| 2012 |
Rodriguez AL, Zhou Y, Williams R, Weaver CD, Vinson PN, Dawson ES, Steckler T, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Daniels JS, Niswender CM, Jones CK, Conn PJ, ... Lindsley CW, et al. Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold. Bioorganic & Medicinal Chemistry Letters. 22: 7388-92. PMID 23142615 DOI: 10.1016/J.Bmcl.2012.10.068 |
0.329 |
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| 2012 |
Panarese JD, Lindsley CW. Biomimetic synthesis and biological evaluation of aplidiopsamine A Organic Letters. 14: 5808-5810. PMID 23106227 DOI: 10.1021/Ol3024665 |
0.354 |
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| 2012 |
Poslusney MS, Sevel C, Utley TJ, Bridges TM, Morrison RD, Kett NR, Sheffler DJ, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Synthesis and biological characterization of a series of novel diaryl amide Mâ‚ antagonists. Bioorganic & Medicinal Chemistry Letters. 22: 6923-8. PMID 23062550 DOI: 10.1016/J.Bmcl.2012.09.011 |
0.434 |
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| 2012 |
Potet F, Lorinc AN, Chaigne S, Hopkins CR, Venkataraman R, Stepanovic SZ, Lewis LM, Days E, Sidorov VY, Engers DW, Zou B, Afshartous D, George AL, Campbell CM, Balser JR, ... ... Lindsley CW, et al. Identification and characterization of a compound that protects cardiac tissue from human Ether-Ã -go-go-related gene (hERG)-related drug-induced arrhythmias. The Journal of Biological Chemistry. 287: 39613-25. PMID 23033485 DOI: 10.1074/Jbc.M112.380162 |
0.319 |
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| 2012 |
Brogan JT, Stoops SL, Lindsley CW. Total synthesis and biological evaluation of phidianidines A and B uncovers unique pharmacological profiles at CNS targets. Acs Chemical Neuroscience. 3: 658-64. PMID 23019492 DOI: 10.1021/Cn300064R |
0.796 |
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| 2012 |
Manka JT, Vinson PN, Gregory KJ, Zhou Y, Williams R, Gogi K, Days E, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Steckler T, Daniels JS, ... ... Lindsley CW, et al. Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover. Bioorganic & Medicinal Chemistry Letters. 22: 6481-5. PMID 22981332 DOI: 10.1016/J.Bmcl.2012.08.043 |
0.314 |
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| 2012 |
Gregory KJ, Noetzel MJ, Rook JM, Vinson PN, Stauffer SR, Rodriguez AL, Emmitte KA, Zhou Y, Chun AC, Felts AS, Chauder BA, Lindsley CW, Niswender CM, Conn PJ. Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships. Molecular Pharmacology. 82: 860-75. PMID 22863693 DOI: 10.1124/Mol.112.080531 |
0.335 |
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| 2012 |
Hahn KN, Fadeyi OO, Cho HP, Lindsley CW. Synthesis and Biological Evaluation of Cremastrine and an Unnatural Analogue. Tetrahedron Letters. 53: 3577-3580. PMID 22822275 DOI: 10.1016/J.Tetlet.2012.05.009 |
0.797 |
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| 2012 |
Cheung YY, Yu H, Xu K, Zou B, Wu M, McManus OB, Li M, Lindsley CW, Hopkins CR. Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor. Journal of Medicinal Chemistry. 55: 6975-9. PMID 22793372 DOI: 10.1021/Jm300700V |
0.319 |
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| 2012 |
Melancon BJ, Utley TJ, Sevel C, Mattmann ME, Cheung YY, Bridges TM, Morrison RD, Sheffler DJ, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012. Bioorganic & Medicinal Chemistry Letters. 22: 5035-40. PMID 22749871 DOI: 10.1016/J.Bmcl.2012.06.018 |
0.405 |
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| 2012 |
Salovich JM, Vinson PN, Sheffler DJ, Lamsal A, Utley TJ, Blobaum AL, Bridges TM, Le U, Jones CK, Wood MR, Daniels JS, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR. Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor. Bioorganic & Medicinal Chemistry Letters. 22: 5084-8. PMID 22738637 DOI: 10.1016/J.Bmcl.2012.05.109 |
0.374 |
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| 2012 |
Delpire E, Baranczak A, Waterson AG, Kim K, Kett N, Morrison RD, Daniels JS, Weaver CD, Lindsley CW. Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Bioorganic & Medicinal Chemistry Letters. 22: 4532-5. PMID 22727639 DOI: 10.1016/J.Bmcl.2012.05.126 |
0.312 |
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| 2012 |
Digby GJ, Noetzel MJ, Bubser M, Utley TJ, Walker AG, Byun NE, Lebois EP, Xiang Z, Sheffler DJ, Cho HP, Davis AA, Nemirovsky NE, Mennenga SE, Camp BW, Bimonte-Nelson HA, ... ... Lindsley CW, et al. Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models. The Journal of Neuroscience : the Official Journal of the Society For Neuroscience. 32: 8532-44. PMID 22723693 DOI: 10.1523/Jneurosci.0337-12.2012 |
0.81 |
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| 2012 |
Morrison RD, Blobaum AL, Byers FW, Santomango TS, Bridges TM, Stec D, Brewer KA, Sanchez-Ponce R, Corlew MM, Rush R, Felts AS, Manka J, Bates BS, Venable DF, Rodriguez AL, ... ... Lindsley CW, et al. The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 40: 1834-45. PMID 22711749 DOI: 10.1124/Dmd.112.046136 |
0.366 |
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| 2012 |
O'Reilly MC, Lindsley CW. A general, enantioselective synthesis of protected morpholines and piperazines Organic Letters. 14: 2910-2913. PMID 22616979 DOI: 10.1021/Ol301203Z |
0.303 |
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| 2012 |
Sheffler DJ, Wenthur CJ, Bruner JA, Carrington SJ, Vinson PN, Gogi KK, Blobaum AL, Morrison RD, Vamos M, Cosford ND, Stauffer SR, Daniels JS, Niswender CM, Conn PJ, Lindsley CW. Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM. Bioorganic & Medicinal Chemistry Letters. 22: 3921-5. PMID 22607673 DOI: 10.1016/J.Bmcl.2012.04.112 |
0.727 |
|
| 2012 |
Mueller R, Dawson ES, Niswender CM, Butkiewicz M, Hopkins CR, Weaver CD, Lindsley CW, Conn PJ, Meiler J. Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators. Journal of Molecular Modeling. 18: 4437-46. PMID 22592386 DOI: 10.1007/S00894-012-1441-0 |
0.339 |
|
| 2012 |
Melancon BJ, Gogliotti RD, Tarr JC, Saleh SA, Chauder BA, Lebois EP, Cho HP, Utley TJ, Sheffler DJ, Bridges TM, Morrison RD, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, et al. Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor. Bioorganic & Medicinal Chemistry Letters. 22: 3467-72. PMID 22507963 DOI: 10.1016/J.Bmcl.2012.03.088 |
0.806 |
|
| 2012 |
Lindsley CW, Hopkins CR. Metabotropic glutamate receptor 4 (mGlu4)-positive allosteric modulators for the treatment of Parkinson's disease: historical perspective and review of the patent literature. Expert Opinion On Therapeutic Patents. 22: 461-81. PMID 22506633 DOI: 10.1517/13543776.2012.679437 |
0.302 |
|
| 2012 |
Fadeyi OO, Senter TJ, Hahn KN, Lindsley CW. A versatile enantioselective synthesis of azabicyclic ring systems: a concise total synthesis of (+)-grandisine D and unnatural analogues. Chemistry (Weinheim An Der Bergstrasse, Germany). 18: 5826-31. PMID 22473565 DOI: 10.1002/Chem.201200629 |
0.786 |
|
| 2012 |
Senter TJ, Fadeyi OO, Lindsley CW. Enantioselective total synthesis of (+)-amabiline. Organic Letters. 14: 1869-71. PMID 22432912 DOI: 10.1021/Ol300466A |
0.787 |
|
| 2012 |
Wells CA, Betke KM, Lindsley CW, Hamm HE. Label-free detection of G protein-SNARE interactions and screening for small molecule modulators. Acs Chemical Neuroscience. 3: 69-78. PMID 22368765 DOI: 10.1021/Cn200102D |
0.319 |
|
| 2012 |
Mueller R, Dawson ES, Meiler J, Rodriguez AL, Chauder BA, Bates BS, Felts AS, Lamb JP, Menon UN, Jadhav SB, Kane AS, Jones CK, Gregory KJ, Niswender CM, Conn PJ, ... ... Lindsley CW, et al. Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound. Chemmedchem. 7: 406-14. PMID 22267125 DOI: 10.1002/Cmdc.201100510 |
0.332 |
|
| 2012 |
Reed JC, White EL, Aub́ J, Lindsley C, Li M, Sklar L, Schreiber S. The NIH's role in accelerating translational sciences Nature Biotechnology. 30: 16-19. PMID 22231085 DOI: 10.1038/Nbt.2087 |
0.396 |
|
| 2012 |
Melancon BJ, Lamers AP, Bridges TM, Sulikowski GA, Utley TJ, Sheffler DJ, Noetzel MJ, Morrison RD, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Wood MR. Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012. Bioorganic & Medicinal Chemistry Letters. 22: 1044-8. PMID 22197142 DOI: 10.1016/J.Bmcl.2011.11.110 |
0.384 |
|
| 2012 |
Lindsley CW, Brown HA. Phospholipase D as a therapeutic target in brain disorders Neuropsychopharmacology. 37: 301-302. PMID 22157867 DOI: 10.1038/Npp.2011.178 |
0.312 |
|
| 2012 |
Melancon BJ, Hopkins CR, Wood MR, Emmitte KA, Niswender CM, Christopoulos A, Conn PJ, Lindsley CW. Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. Journal of Medicinal Chemistry. 55: 1445-64. PMID 22148748 DOI: 10.1021/Jm201139R |
0.331 |
|
| 2012 |
Xiang Z, Thompson AD, Jones CK, Lindsley CW, Conn PJ. Roles of the M1 muscarinic acetylcholine receptor subtype in the regulation of basal ganglia function and implications for the treatment of Parkinson's disease Journal of Pharmacology and Experimental Therapeutics. 340: 595-603. PMID 22135383 DOI: 10.1124/Jpet.111.187856 |
0.377 |
|
| 2012 |
Noetzel MJ, Rook JM, Vinson PN, Cho HP, Days E, Zhou Y, Rodriguez AL, Lavreysen H, Stauffer SR, Niswender CM, Xiang Z, Daniels JS, Jones CK, Lindsley CW, Weaver CD, et al. Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function. Molecular Pharmacology. 81: 120-33. PMID 22021324 DOI: 10.1124/Mol.111.075184 |
0.343 |
|
| 2012 |
Thomsen M, Lindsley CW, Conn PJ, Wessell JE, Fulton BS, Wess J, Caine SB. Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice Psychopharmacology. 220: 673-685. PMID 21964721 DOI: 10.1007/S00213-011-2516-9 |
0.306 |
|
| 2012 |
O'Reilly MC, Lindsley CW. Enantioselective synthesis of C2-functionalized, N-protected morpholines and orthogonally N,N′-protected piperazines via organocatalysis Tetrahedron Letters. 53: 1539-1542. DOI: 10.1016/J.Tetlet.2011.12.063 |
0.302 |
|
| 2012 |
Potet F, Lorinc A, Hopkins C, Venkataraman R, Chaigne S, Stepanovic S, Lindsley C, Baudenbacher F, Kupershmidt S. Characterization of a Compound that Reduces Sensitivity to HERG Inhibitors and Prevents hERG-Related, Drug-Induced Arrhythmias in Isolated Rabbit Hearts Biophysical Journal. 102: 14a. DOI: 10.1016/J.Bpj.2011.11.101 |
0.32 |
|
| 2012 |
Fadeyi OO, Lindsley CW. The discovery and synthesis of brevisamide Studies in Natural Products Chemistry. 38: 37-51. DOI: 10.1016/B978-0-444-59530-0.00002-2 |
0.793 |
|
| 2011 |
Robichaud AJ, Engers DW, Lindsley CW, Hopkins CR. Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics. Acs Chemical Neuroscience. 2: 433-49. PMID 22860170 DOI: 10.1021/Cn200043E |
0.365 |
|
| 2011 |
Lindsley CW. Special issue on the pharmacology and medicinal chemistry of allosteric modulators of metabotropic glutamate receptors (mGluRs) Acs Chemical Neuroscience. 2: 379. PMID 22860165 DOI: 10.1021/Cn200069D |
0.337 |
|
| 2011 |
Xiang Z, Thompson AD, Brogan JT, Schulte ML, Melancon BJ, Mi D, Lewis LM, Zou B, Yang L, Morrison R, Santomango T, Byers F, Brewer K, Aldrich JS, Yu H, ... ... Lindsley CW, et al. The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease. Acs Chemical Neuroscience. 2: 730-742. PMID 22368764 DOI: 10.1021/Cn200090Z |
0.609 |
|
| 2011 |
Raphemot R, Lonergan DF, Nguyen TT, Utley T, Lewis LM, Kadakia R, Weaver CD, Gogliotti R, Hopkins C, Lindsley CW, Denton JS. Discovery, characterization, and structure-activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.x, and Kir7.1. Frontiers in Pharmacology. 2: 75. PMID 22275899 DOI: 10.3389/Fphar.2011.00075 |
0.315 |
|
| 2011 |
Brogan JT, Stoops SL, Crews BC, Marnett LJ, Lindsley CW. Total Synthesis (+)-7-Bromotrypargine and Unnatural Analogs: Biological Evaluation Uncovers Activity at CNS Targets of Therapeutic Relevance. Acs Chemical Neuroscience. 2: 633-639. PMID 22247792 DOI: 10.1021/Cn200075N |
0.805 |
|
| 2011 |
Utley T, Haddenham D, Salovich JM, Zamorano R, Vinson PN, Lindsley CW, Hopkins CR, Niswender CM. Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator. Bioorganic & Medicinal Chemistry Letters. 21: 6955-9. PMID 22030026 DOI: 10.1016/J.Bmcl.2011.09.131 |
0.322 |
|
| 2011 |
Speed N, Saunders C, Davis AR, Owens WA, Matthies HJ, Saadat S, Kennedy JP, Vaughan RA, Neve RL, Lindsley CW, Russo SJ, Daws LC, Niswender KD, Galli A. Impaired striatal Akt signaling disrupts dopamine homeostasis and increases feeding. Plos One. 6: e25169. PMID 21969871 DOI: 10.1371/Journal.Pone.0025169 |
0.381 |
|
| 2011 |
Jones CK, Engers DW, Thompson AD, Field JR, Blobaum AL, Lindsley SR, Zhou Y, Gogliotti RD, Jadhav S, Zamorano R, Bogenpohl J, Smith Y, Morrison R, Daniels JS, Weaver CD, ... ... Lindsley CW, et al. Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model. Journal of Medicinal Chemistry. 54: 7639-47. PMID 21966889 DOI: 10.1021/Jm200956Q |
0.364 |
|
| 2011 |
Schulte ML, Lindsley CW. Highly diastereoselective and general synthesis of primary β-fluoroamines. Organic Letters. 13: 5684-7. PMID 21942742 DOI: 10.1021/ol202415j |
0.599 |
|
| 2011 |
Selvy PE, Lavieri RR, Lindsley CW, Brown HA. Phospholipase D: enzymology, functionality, and chemical modulation. Chemical Reviews. 111: 6064-119. PMID 21936578 DOI: 10.1021/Cr200296T |
0.707 |
|
| 2011 |
Lebois EP, Digby GJ, Sheffler DJ, Melancon BJ, Tarr JC, Cho HP, Miller NR, Morrison R, Bridges TM, Xiang Z, Daniels JS, Wood MR, Conn PJ, Lindsley CW. Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071. Bioorganic & Medicinal Chemistry Letters. 21: 6451-5. PMID 21930376 DOI: 10.1016/J.Bmcl.2011.08.084 |
0.809 |
|
| 2011 |
Lindsley CW, Bates BS, Menon UN, Jadhav SB, Kane AS, Jones CK, Rodriguez AL, Conn PJ, Olsen CM, Winder DG, Emmitte KA. (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction. Acs Chemical Neuroscience. 2: 471-482. PMID 21927650 DOI: 10.1021/Cn100099N |
0.366 |
|
| 2011 |
Miller M, Shi J, Zhu Y, Kustov M, Tian JB, Stevens A, Wu M, Xu J, Long S, Yang P, Zholos AV, Salovich JM, Weaver CD, Hopkins CR, Lindsley CW, et al. Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels. The Journal of Biological Chemistry. 286: 33436-46. PMID 21795696 DOI: 10.1074/Jbc.M111.274167 |
0.315 |
|
| 2011 |
Mattmann ME, Stoops SL, Lindsley CW. Inhibition of Akt with small molecules and biologics: historical perspective and current status of the patent landscape. Expert Opinion On Therapeutic Patents. 21: 1309-38. PMID 21635152 DOI: 10.1517/13543776.2011.587959 |
0.775 |
|
| 2011 |
Wolkenberg SE, Zhao Z, Thut C, Maxwell JW, McDonald TP, Kinose F, Reilly M, Lindsley CW, Hartman GD. Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2. Journal of Medicinal Chemistry. 54: 2351-8. PMID 21395312 DOI: 10.1021/Jm101501B |
0.343 |
|
| 2011 |
Wood MR, Hopkins CR, Brogan JT, Conn PJ, Lindsley CW. "Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology. Biochemistry. 50: 2403-10. PMID 21341760 DOI: 10.1021/Bi200129S |
0.326 |
|
| 2011 |
Cheung YY, Zamorano R, Blobaum AL, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGluâ‚„. Acs Combinatorial Science. 13: 159-65. PMID 21338051 DOI: 10.1021/Co1000508 |
0.341 |
|
| 2011 |
Williams R, Manka JT, Rodriguez AL, Vinson PN, Niswender CM, Weaver CD, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold. Bioorganic & Medicinal Chemistry Letters. 21: 1350-3. PMID 21315585 DOI: 10.1016/J.Bmcl.2011.01.044 |
0.379 |
|
| 2011 |
Lebois EP, Jones CK, Lindsley CW. The Evolution of Histamine H 3 Antagonists/Inverse Agonists Current Topics in Medicinal Chemistry. 11: 648-660. PMID 21261594 DOI: 10.2174/1568026611109060648 |
0.798 |
|
| 2011 |
Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. Journal of Medicinal Chemistry. 54: 1106-10. PMID 21247167 DOI: 10.1021/Jm101271S |
0.339 |
|
| 2011 |
Stoops SL, Pearson AS, Weaver C, Waterson AG, Days E, Farmer C, Brady S, Weaver CD, Beauchamp RD, Lindsley CW. Identification and optimization of small molecules that restore E-cadherin expression and reduce invasion in colorectal carcinoma cells. Acs Chemical Biology. 6: 452-65. PMID 21241068 DOI: 10.1021/Cb100305H |
0.771 |
|
| 2011 |
Reid PR, Bridges TM, Sheffler DJ, Cho HP, Lewis LM, Days E, Daniels JS, Jones CK, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Wood MR. Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe. Bioorganic & Medicinal Chemistry Letters. 21: 2697-701. PMID 21194936 DOI: 10.1016/J.Bmcl.2010.12.015 |
0.384 |
|
| 2011 |
Lamb JP, Engers DW, Niswender CM, Rodriguez AL, Venable DF, Conn PJ, Lindsley CW. Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists. Bioorganic & Medicinal Chemistry Letters. 21: 2711-4. PMID 21183344 DOI: 10.1016/J.Bmcl.2010.11.119 |
0.375 |
|
| 2011 |
Bhave G, Chauder BA, Liu W, Dawson ES, Kadakia R, Nguyen TT, Lewis LM, Meiler J, Weaver CD, Satlin LM, Lindsley CW, Denton JS. Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel. Molecular Pharmacology. 79: 42-50. PMID 20926757 DOI: 10.1124/Mol.110.066928 |
0.326 |
|
| 2011 |
Stoops SL, Beauchamp RD, Lindsley CW. Abstract B197: Understanding the mechanism of action of small molecules that restore E-cadherin expression. Molecular Cancer Therapeutics. 10. DOI: 10.1158/1535-7163.Targ-11-B197 |
0.78 |
|
| 2010 |
Zhou Y, Manka JT, Rodriguez AL, Weaver CD, Days EL, Vinson PN, Jadhav S, Hermann EJ, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity. Acs Medicinal Chemistry Letters. 1: 433-438. PMID 23308336 DOI: 10.1021/Ml100181A |
0.376 |
|
| 2010 |
Speed NK, Matthies HJ, Kennedy JP, Vaughan RA, Javitch JA, Russo SJ, Lindsley CW, Niswender K, Galli A. Akt-dependent and isoform-specific regulation of dopamine transporter cell surface expression. Acs Chemical Neuroscience. 1: 476-81. PMID 22778840 DOI: 10.1021/Cn100031T |
0.394 |
|
| 2010 |
Lindsley CW. The top prescription drugs of 2009 in the US: CNS therapeutics rank among highest grossing Acs Chemical Neuroscience. 1: 407-408. PMID 22778834 DOI: 10.1021/Cn1000556 |
0.31 |
|
| 2010 |
Lebois EP, Bridges TM, Lewis LM, Dawson ES, Kane AS, Xiang Z, Jadhav SB, Yin H, Kennedy JP, Meiler J, Niswender CM, Jones CK, Conn PJ, Weaver CD, Lindsley CW. Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system. Acs Chemical Neuroscience. 1: 104-121. PMID 21961051 DOI: 10.1021/Cn900003H |
0.818 |
|
| 2010 |
Hammond AS, Rodriguez AL, Townsend SD, Niswender CM, Gregory KJ, Lindsley CW, Conn PJ. Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology. Acs Chemical Neuroscience. 1: 702-716. PMID 20981342 DOI: 10.1021/Cn100051M |
0.344 |
|
| 2010 |
Rodriguez AL, Grier MD, Jones CK, Herman EJ, Kane AS, Smith RL, Williams R, Zhou Y, Marlo JE, Days EL, Blatt TN, Jadhav S, Menon UN, Vinson PN, Rook JM, ... ... Lindsley CW, et al. Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Molecular Pharmacology. 78: 1105-23. PMID 20923853 DOI: 10.1124/Mol.110.067207 |
0.379 |
|
| 2010 |
Davis AA, Heilman CJ, Brady AE, Miller NR, Fuerstenau-Sharp M, Hanson BJ, Lindsley CW, Conn PJ, Lah JJ, Levey AI. Differential effects of allosteric M(1) muscarinic acetylcholine receptor agonists on receptor activation, arrestin 3 recruitment, and receptor downregulation. Acs Chemical Neuroscience. 1: 542-551. PMID 20835371 DOI: 10.1021/Cn100011E |
0.535 |
|
| 2010 |
Bridges TM, Kennedy JP, Hopkins CR, Conn PJ, Lindsley CW. Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators. Bioorganic & Medicinal Chemistry Letters. 20: 5617-22. PMID 20801651 DOI: 10.1016/J.Bmcl.2010.08.042 |
0.483 |
|
| 2010 |
Robertson SD, Matthies HJ, Owens WA, Sathananthan V, Christianson NS, Kennedy JP, Lindsley CW, Daws LC, Galli A. Insulin reveals Akt signaling as a novel regulator of norepinephrine transporter trafficking and norepinephrine homeostasis. The Journal of Neuroscience : the Official Journal of the Society For Neuroscience. 30: 11305-16. PMID 20739551 DOI: 10.1523/Jneurosci.0126-10.2010 |
0.393 |
|
| 2010 |
Lavieri RR, Scott SA, Selvy PE, Kim K, Jadhav S, Morrison RD, Daniels JS, Brown HA, Lindsley CW. Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor. Journal of Medicinal Chemistry. 53: 6706-19. PMID 20735042 DOI: 10.1021/Jm100814G |
0.74 |
|
| 2010 |
Aldrich LN, Stoops SL, Crews BC, Marnett LJ, Lindsley CW. Total synthesis and biological evaluation of tambjamine K and a library of unnatural analogs. Bioorganic & Medicinal Chemistry Letters. 20: 5207-11. PMID 20655217 DOI: 10.1016/J.Bmcl.2010.06.154 |
0.772 |
|
| 2010 |
Felts AS, Lindsley SR, Lamb JP, Rodriguez AL, Menon UN, Jadhav S, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. 3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats. Bioorganic & Medicinal Chemistry Letters. 20: 4390-4. PMID 20598884 DOI: 10.1016/J.Bmcl.2010.06.064 |
0.333 |
|
| 2010 |
Williams R, Zhou Y, Niswender CM, Luo Q, Conn PJ, Lindsley CW, Hopkins CR. Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4. Acs Chemical Neuroscience. 1: 411-419. PMID 20582156 DOI: 10.1021/Cn9000318 |
0.348 |
|
| 2010 |
Fadeyi OO, Schulte ML, Lindsley CW. General access to chiral N-alkyl terminal aziridines via organocatalysis. Organic Letters. 12: 3276-8. PMID 20552963 DOI: 10.1021/ol101276x |
0.774 |
|
| 2010 |
Siuta MA, Robertson SD, Kocalis H, Saunders C, Gresch PJ, Khatri V, Shiota C, Kennedy JP, Lindsley CW, Daws LC, Polley DB, Veenstra-Vanderweele J, Stanwood GD, Magnuson MA, Niswender KD, et al. Dysregulation of the norepinephrine transporter sustains cortical hypodopaminergia and schizophrenia-like behaviors in neuronal rictor null mice. Plos Biology. 8: e1000393. PMID 20543991 DOI: 10.1371/Journal.Pbio.1000393 |
0.397 |
|
| 2010 |
Bridges TM, LeBois EP, Hopkins CR, Wood MR, Jones CK, Conn PJ, Lindsley CW. The antipsychotic potential of muscarinic allosteric modulation. Drug News & Perspectives. 23: 229-40. PMID 20520852 DOI: 10.1358/Dnp.2010.23.4.1416977 |
0.803 |
|
| 2010 |
Mueller R, Rodriguez AL, Dawson ES, Butkiewicz M, Nguyen TT, Oleszkiewicz S, Bleckmann A, Weaver CD, Lindsley CW, Conn PJ, Meiler J. Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening. Acs Chemical Neuroscience. 1: 288-305. PMID 20414370 DOI: 10.1021/Cn9000389 |
0.346 |
|
| 2010 |
Miller NR, Daniels RN, Lee D, Conn PJ, Lindsley CW. Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists. Bioorganic & Medicinal Chemistry Letters. 20: 2174-7. PMID 20202841 DOI: 10.1016/J.Bmcl.2010.02.041 |
0.781 |
|
| 2010 |
Lindsley CW. The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation: a 2009 update. Current Topics in Medicinal Chemistry. 10: 458-77. PMID 20180757 DOI: 10.2174/156802610790980602 |
0.31 |
|
| 2010 |
Aldrich LN, Dawson ES, Lindsley CW. Evaluation of the biosynthetic proposal for the synthesis of marineosins A and B. Organic Letters. 12: 1048-51. PMID 20141121 DOI: 10.1021/Ol100034P |
0.78 |
|
| 2010 |
Hao J, Ho JN, Lewis JA, Karim KA, Daniels RN, Gentry PR, Hopkins CR, Lindsley CW, Hong CC. In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. Acs Chemical Biology. 5: 245-53. PMID 20020776 DOI: 10.1021/Cb9002865 |
0.742 |
|
| 2010 |
Bridges TM, Kennedy JP, Cho HP, Breininger ML, Gentry PR, Hopkins CR, Conn PJ, Lindsley CW. Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorganic & Medicinal Chemistry Letters. 20: 558-62. PMID 20004578 DOI: 10.1016/J.Bmcl.2009.11.089 |
0.475 |
|
| 2010 |
Yang FV, Shipe WD, Bunda JL, Nolt MB, Wisnoski DD, Zhao Z, Barrow JC, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Hartman GD, Lindsley CW. Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators. Bioorganic & Medicinal Chemistry Letters. 20: 531-6. PMID 20004574 DOI: 10.1016/J.Bmcl.2009.11.100 |
0.382 |
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| 2010 |
Thomsen M, Conn PJ, Lindsley C, Wess J, Boon JY, Fulton BS, Fink-Jensen A, Caine SB. Attenuation of cocaine's reinforcing and discriminative stimulus effects via muscarinic M1 acetylcholine receptor stimulation Journal of Pharmacology and Experimental Therapeutics. 332: 959-969. PMID 19996296 DOI: 10.1124/Jpet.109.162057 |
0.308 |
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| 2010 |
Smith BJ, Qu T, Mulder M, Noetzel MJ, Lindsley CW, Sulikowski GA. Synthesis and bioactivity of (±)-tetrahydrohaliclonacyclamine A Tetrahedron. 66: 4805-4810. DOI: 10.1016/J.Tet.2010.03.117 |
0.348 |
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| 2010 |
Denton JS, Chauder BA, Kadakia R, Dawson ES, Lindsley C, Weaver CD, Bhave G. Chemical Synthesis of a Highly Selective Probe of the Renal Outer Medullary Potassium Channel (ROMK) Biophysical Journal. 98: 755a. DOI: 10.1016/J.Bpj.2009.12.4144 |
0.334 |
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| 2010 |
Bridges TM, Kennedy JP, Cho HP, Breininger ML, Gentry PR, Hopkins CR, Conn PJ, Lindsley CW. ChemInform Abstract: Chemical Lead Optimization of a Pan Gq mAChR M1, M3, M5 Positive Allosteric Modulator (PAM) Lead. Part 1. Development of the First Highly Selective M5 PAM (I). Cheminform. 41: no-no. DOI: 10.1002/chin.201023112 |
0.387 |
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| 2010 |
LIPSHUTZ BH, MOLLARD P, LINDSLEY C, CHANG V. ChemInform Abstract: Cyclo-SEM: A New Carbonyl Protecting Group. Cheminform. 28: no-no. DOI: 10.1002/chin.199727069 |
0.482 |
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| 2010 |
LIPSHUTZ BH, BHANDARI A, LINDSLEY C, KEIL R, WOOD MR. ChemInform Abstract: New Synthetic Methods Based on Organozirconium and Organocopper Chemistry Cheminform. 25: no-no. DOI: 10.1002/chin.199442296 |
0.387 |
|
| 2009 |
Aldrich LN, Lebois EP, Lewis LM, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW. MAOS ls for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines. Tetrahedron Letters. 50: 212-215. PMID 22090663 DOI: 10.1016/J.Tetlet.2008.10.127 |
0.805 |
|
| 2009 |
Miller TW, Forbes JT, Shah C, Wyatt SK, Manning HC, Olivares MG, Sanchez V, Dugger TC, de Matos Granja N, Narasanna A, Cook RS, Kennedy JP, Lindsley CW, Arteaga CL. Inhibition of mammalian target of rapamycin is required for optimal antitumor effect of HER2 inhibitors against HER2-overexpressing cancer cells. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 15: 7266-76. PMID 19934303 DOI: 10.1158/1078-0432.Ccr-09-1665 |
0.609 |
|
| 2009 |
Daniels RN, Melancon BJ, Wang EA, Crews BC, Marnett LJ, Sulikowski GA, Lindsley CW. Progress toward the total synthesis of lucentamycin A: total synthesis and biological evaluation of 8-epi-lucentamycin A. The Journal of Organic Chemistry. 74: 8852-5. PMID 19908916 DOI: 10.1021/Jo902115S |
0.752 |
|
| 2009 |
Shirey JK, Brady AE, Jones PJ, Davis AA, Bridges TM, Kennedy JP, Jadhav SB, Menon UN, Xiang Z, Watson ML, Christian EP, Doherty JJ, Quirk MC, Snyder DH, Lah JJ, ... ... Lindsley CW, et al. A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning. The Journal of Neuroscience : the Official Journal of the Society For Neuroscience. 29: 14271-86. PMID 19906975 DOI: 10.1523/Jneurosci.3930-09.2009 |
0.618 |
|
| 2009 |
Zhou Y, Rodriguez AL, Williams R, Weaver CD, Conn PJ, Lindsley CW. Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS. Bioorganic & Medicinal Chemistry Letters. 19: 6502-6. PMID 19875287 DOI: 10.1016/J.Bmcl.2009.10.059 |
0.326 |
|
| 2009 |
Felts AS, Saleh SA, Le U, Rodriguez AL, Weaver CD, Conn PJ, Lindsley CW, Emmitte KA. Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Bioorganic & Medicinal Chemistry Letters. 19: 6623-6. PMID 19854049 DOI: 10.1016/J.Bmcl.2009.10.024 |
0.369 |
|
| 2009 |
Weaver CD, Sheffler DJ, Lewis LM, Bridges TM, Williams R, Nalywajko NT, Kennedy JP, Mulder MM, Jadhav S, Aldrich LA, Jones CK, Marlo JE, Niswender CM, Mock MM, Zheng F, ... ... Lindsley CW, et al. Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe. Current Topics in Medicinal Chemistry. 9: 1217-26. PMID 19807667 DOI: 10.2174/156802609789753635 |
0.521 |
|
| 2009 |
Lindsley CW, Niswender CM, Engers DW, Hopkins CR. Recent progress in the development of mGluR4 positive allosteric modulators for the treatment of Parkinson's disease. Current Topics in Medicinal Chemistry. 9: 949-63. PMID 19754407 DOI: 10.2174/156802609789378272 |
0.334 |
|
| 2009 |
Ma L, Seager MA, Seager M, Wittmann M, Jacobson M, Bickel D, Burno M, Jones K, Graufelds VK, Xu G, Pearson M, McCampbell A, Gaspar R, Shughrue P, Danziger A, ... ... Lindsley CW, et al. Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation. Proceedings of the National Academy of Sciences of the United States of America. 106: 15950-5. PMID 19717450 DOI: 10.1073/Pnas.0900903106 |
0.382 |
|
| 2009 |
Lewis LM, Bhave G, Chauder BA, Banerjee S, Lornsen KA, Redha R, Fallen K, Lindsley CW, Weaver CD, Denton JS. High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1. Molecular Pharmacology. 76: 1094-103. PMID 19706730 DOI: 10.1124/Mol.109.059840 |
0.301 |
|
| 2009 |
Kennedy JP, Bridges TM, Gentry PR, Brogan JT, Kane AS, Jones CK, Brady AE, Shirey JK, Conn PJ, Lindsley CW. Synthesis and structure-activity relationships of allosteric potentiators of the m(4) muscarinic acetylcholine receptor. Chemmedchem. 4: 1600-7. PMID 19705385 DOI: 10.1002/Cmdc.200900231 |
0.413 |
|
| 2009 |
Fadeyi OO, Lindsley CW. Total synthesis of brevisamide. Organic Letters. 11: 3950-2. PMID 19639953 DOI: 10.1021/Ol9015755 |
0.784 |
|
| 2009 |
Sharma S, Kedrowski J, Rook JM, Smith RL, Jones CK, Rodriguez AL, Conn PJ, Lindsley CW. Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines. Journal of Medicinal Chemistry. 52: 4103-6. PMID 19537763 DOI: 10.1021/Jm900654C |
0.393 |
|
| 2009 |
Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). Journal of Medicinal Chemistry. 52: 4115-8. PMID 19469556 DOI: 10.1021/Jm9005065 |
0.341 |
|
| 2009 |
Rodriguez AL, Williams R, Zhou Y, Lindsley SR, Le U, Grier MD, Weaver CD, Conn PJ, Lindsley CW. Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype. Bioorganic & Medicinal Chemistry Letters. 19: 3209-13. PMID 19443219 DOI: 10.1016/J.Bmcl.2009.04.110 |
0.352 |
|
| 2009 |
Kennedy JP, Conn PJ, Lindsley CW. A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin. Bioorganic & Medicinal Chemistry Letters. 19: 3204-8. PMID 19443215 DOI: 10.1016/J.Bmcl.2009.04.106 |
0.453 |
|
| 2009 |
Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. Journal of Medicinal Chemistry. 52: 3445-8. PMID 19438238 DOI: 10.1021/Jm900286J |
0.371 |
|
| 2009 |
Miller TW, Pérez-Torres M, Narasanna A, Guix M, Stål O, Pérez-Tenorio G, Gonzalez-Angulo AM, Hennessy BT, Mills GB, Kennedy JP, Lindsley CW, Arteaga CL. Loss of Phosphatase and Tensin homologue deleted on chromosome 10 engages ErbB3 and insulin-like growth factor-I receptor signaling to promote antiestrogen resistance in breast cancer. Cancer Research. 69: 4192-201. PMID 19435893 DOI: 10.1158/0008-5472.Can-09-0042 |
0.4 |
|
| 2009 |
Sheffler DJ, Williams R, Bridges TM, Xiang Z, Kane AS, Byun NE, Jadhav S, Mock MM, Zheng F, Lewis LM, Jones CK, Niswender CM, Weaver CD, Lindsley CW, Conn PJ. A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Molecular Pharmacology. 76: 356-68. PMID 19407080 DOI: 10.1124/Mol.109.056531 |
0.401 |
|
| 2009 |
Lavieri R, Scott SA, Lewis JA, Selvy PE, Armstrong MD, Alex Brown H, Lindsley CW. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity. Bioorganic & Medicinal Chemistry Letters. 19: 2240-3. PMID 19299128 DOI: 10.1016/J.Bmcl.2009.02.125 |
0.743 |
|
| 2009 |
Lewis JA, Scott SA, Lavieri R, Buck JR, Selvy PE, Stoops SL, Armstrong MD, Brown HA, Lindsley CW. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorganic & Medicinal Chemistry Letters. 19: 1916-20. PMID 19268584 DOI: 10.1016/J.Bmcl.2009.02.057 |
0.798 |
|
| 2009 |
Conn PJ, Jones CK, Lindsley CW. Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders Trends in Pharmacological Sciences. 30: 148-155. PMID 19201489 DOI: 10.1016/J.Tips.2008.12.002 |
0.387 |
|
| 2009 |
Engers DW, Rodriguez AL, Williams R, Hammond AS, Venable D, Oluwatola O, Sulikowski GA, Conn PJ, Lindsley CW. Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273. Chemmedchem. 4: 505-11. PMID 19197923 DOI: 10.1002/Cmdc.200800357 |
0.361 |
|
| 2009 |
Wolkenberg SE, Zhao Z, Wisnoski DD, Leister WH, O'Brien J, Lemaire W, Williams DL, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Gibson C, Ma BK, ... ... Lindsley CW, et al. Discovery of GlyT1 inhibitors with improved pharmacokinetic properties. Bioorganic & Medicinal Chemistry Letters. 19: 1492-5. PMID 19181525 DOI: 10.1016/J.Bmcl.2009.01.015 |
0.323 |
|
| 2009 |
Zhao Z, Leister WH, O'Brien JA, Lemaire W, Williams DL, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Hartman GD, Lindsley CW, Wolkenberg SE. Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors. Bioorganic & Medicinal Chemistry Letters. 19: 1488-91. PMID 19179073 DOI: 10.1016/J.Bmcl.2008.12.115 |
0.352 |
|
| 2009 |
Fadeyi OO, Lindsley CW. Rapid, general access to chiral beta-fluoroamines and beta,beta-difluoroamines via organocatalysis. Organic Letters. 11: 943-6. PMID 19159275 DOI: 10.1021/Ol802930Q |
0.749 |
|
| 2009 |
Scott SA, Selvy PE, Buck JR, Cho HP, Criswell TL, Thomas AL, Armstrong MD, Arteaga CL, Lindsley CW, Brown HA. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nature Chemical Biology. 5: 108-17. PMID 19136975 DOI: 10.1038/Nchembio.140 |
0.358 |
|
| 2009 |
Conn PJ, Christopoulos A, Lindsley CW. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nature Reviews. Drug Discovery. 8: 41-54. PMID 19116626 DOI: 10.1038/Nrd2760 |
0.339 |
|
| 2009 |
Williams R, Niswender CM, Luo Q, Le U, Conn PJ, Lindsley CW. Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead. Bioorganic & Medicinal Chemistry Letters. 19: 962-6. PMID 19097893 DOI: 10.1016/J.Bmcl.2008.11.104 |
0.351 |
|
| 2009 |
Marlo JE, Niswender CM, Days EL, Bridges TM, Xiang Y, Rodriguez AL, Shirey JK, Brady AE, Nalywajko T, Luo Q, Austin CA, Williams MB, Kim K, Williams R, Orton D, ... ... Lindsley CW, et al. Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity. Molecular Pharmacology. 75: 577-88. PMID 19047481 DOI: 10.1124/Mol.108.052886 |
0.416 |
|
| 2009 |
Phillip Kennedy J, Breininger ML, Lindsley CW. Total synthesis of Eudistomins Y1–Y6 Tetrahedron Letters. 50: 7067-7069. DOI: 10.1016/J.Tetlet.2009.09.180 |
0.315 |
|
| 2009 |
Fadeyi OO, Nathan Daniels R, DeGuire SM, Lindsley CW. Total synthesis of polemannones B and C Tetrahedron Letters. 50: 3084-3087. DOI: 10.1016/J.Tetlet.2009.04.043 |
0.768 |
|
| 2009 |
Lebois EP, Bridges TM, Dawson ES, Kennedy JP, Xiang Z, Jadhav SB, Yin H, Meiler J, Jones CK, Conn PJ, Weaver CD, Lindsley CW. P2-256: Towards the treatment of Alzheimer's disease: Discovery and development of novel subtype-specific M1 allosteric agonists Alzheimer's & Dementia. 5: P335-P335. DOI: 10.1016/J.Jalz.2009.04.570 |
0.79 |
|
| 2009 |
Bridges TM, Marlo JE, Niswender CM, Gentry PR, Weaver CD, Conn PJ, Lindsley CW. P2-207: Discovery of a highly M5-preferring muscarinic acetylcholine receptor allosteric potentiator Alzheimer's & Dementia. 5: P321-P321. DOI: 10.1016/J.Jalz.2009.04.520 |
0.347 |
|
| 2009 |
Fadeyi OO, Lindsley CW. ChemInform Abstract: Rapid, General Access to Chiral β-Fluoroamines and β,β-Difluoroamines via Organocatalysis. Cheminform. 40. DOI: 10.1002/chin.200927039 |
0.732 |
|
| 2008 |
Conn PJ, Lindsley CW, Jones CK. Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia. Trends in Pharmacological Sciences. 30: 25-31. PMID 19058862 DOI: 10.1016/J.Tips.2008.10.006 |
0.335 |
|
| 2008 |
Jones CK, Brady AE, Davis AA, Xiang Z, Bubser M, Tantawy MN, Kane AS, Bridges TM, Kennedy JP, Bradley SR, Peterson TE, Ansari MS, Baldwin RM, Kessler RM, Deutch AY, ... ... Lindsley CW, et al. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. The Journal of Neuroscience : the Official Journal of the Society For Neuroscience. 28: 10422-33. PMID 18842902 DOI: 10.1523/Jneurosci.1850-08.2008 |
0.619 |
|
| 2008 |
Miller NR, Daniels RN, Bridges TM, Brady AE, Conn PJ, Lindsley CW. Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen. Bioorganic & Medicinal Chemistry Letters. 18: 5443-7. PMID 18829311 DOI: 10.1016/J.Bmcl.2008.09.032 |
0.778 |
|
| 2008 |
Yang ZQ, Barrow JC, Shipe WD, Schlegel KA, Shu Y, Yang FV, Lindsley CW, Rittle KE, Bock MG, Hartman GD, Uebele VN, Nuss CE, Fox SV, Kraus RL, Doran SM, et al. Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels. Journal of Medicinal Chemistry. 51: 6471-7. PMID 18817368 DOI: 10.1021/Jm800830N |
0.327 |
|
| 2008 |
Bridges TM, Brady AE, Kennedy JP, Daniels RN, Miller NR, Kim K, Breininger ML, Gentry PR, Brogan JT, Jones CK, Conn PJ, Lindsley CW. Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties. Bioorganic & Medicinal Chemistry Letters. 18: 5439-42. PMID 18805692 DOI: 10.1016/J.Bmcl.2008.09.023 |
0.796 |
|
| 2008 |
Kennedy JP, Brogan JT, Lindsley CW. Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential. Journal of Natural Products. 71: 1783-6. PMID 18800848 DOI: 10.1021/Np800339E |
0.491 |
|
| 2008 |
Niswender CM, Lebois EP, Luo Q, Kim K, Muchalski H, Yin H, Conn PJ, Lindsley CW. Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators. Bioorganic & Medicinal Chemistry Letters. 18: 5626-30. PMID 18793851 DOI: 10.1016/J.Bmcl.2008.08.087 |
0.801 |
|
| 2008 |
Lewis JA, Daniels RN, Lindsley CW. Total synthesis of Ciliatamides A-C: stereochemical revision and the natural product-guided synthesis of unnatural analogs. Organic Letters. 10: 4545-8. PMID 18788742 DOI: 10.1021/Ol801842V |
0.739 |
|
| 2008 |
Brady AE, Jones CK, Bridges TM, Kennedy JP, Thompson AD, Heiman JU, Breininger ML, Gentry PR, Yin H, Jadhav SB, Shirey JK, Conn PJ, Lindsley CW. Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. The Journal of Pharmacology and Experimental Therapeutics. 327: 941-53. PMID 18772318 DOI: 10.1124/Jpet.108.140350 |
0.529 |
|
| 2008 |
Daniels RN, Fadeyi OO, Lindsley CW. A new catalytic Cu(II)/sparteine oxidant system for beta,beta-phenolic couplings of styrenyl phenols: synthesis of carpanone and unnatural analogs. Organic Letters. 10: 4097-100. PMID 18729467 DOI: 10.1021/Ol801643T |
0.759 |
|
| 2008 |
Niswender CM, Johnson KA, Weaver CD, Jones CK, Xiang Z, Luo Q, Rodriguez AL, Marlo JE, de Paulis T, Thompson AD, Days EL, Nalywajko T, Austin CA, Williams MB, Ayala JE, ... ... Lindsley CW, et al. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Molecular Pharmacology. 74: 1345-58. PMID 18664603 DOI: 10.1124/Mol.108.049551 |
0.34 |
|
| 2008 |
Bridges TM, Lindsley CW. G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms. Acs Chemical Biology. 3: 530-41. PMID 18652471 DOI: 10.1021/Cb800116F |
0.306 |
|
| 2008 |
Sharma S, Rodriguez AL, Conn PJ, Lindsley CW. Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold. Bioorganic & Medicinal Chemistry Letters. 18: 4098-101. PMID 18550372 DOI: 10.1016/J.Bmcl.2008.05.091 |
0.395 |
|
| 2008 |
Zeng Z, O'Brien JA, Lemaire W, O'Malley SS, Miller PJ, Zhao Z, Wallace MA, Raab C, Lindsley CW, Sur C, Williams DL. A novel radioligand for glycine transporter 1: characterization and use in autoradiographic and in vivo brain occupancy studies. Nuclear Medicine and Biology. 35: 315-25. PMID 18355687 DOI: 10.1016/J.Nucmedbio.2007.12.002 |
0.337 |
|
| 2008 |
Lewis JA, Lebois EP, Lindsley CW. Allosteric modulation of kinases and GPCRs: design principles and structural diversity. Current Opinion in Chemical Biology. 12: 269-80. PMID 18342020 DOI: 10.1016/J.Cbpa.2008.02.014 |
0.781 |
|
| 2008 |
Lindsley CW, Barnett SF, Layton ME, Bilodeau MT. The PI3K/Akt pathway: recent progress in the development of ATP-competitive and allosteric Akt kinase inhibitors. Current Cancer Drug Targets. 8: 7-18. PMID 18288939 DOI: 10.2174/156800908783497096 |
0.626 |
|
| 2008 |
Kennedy JP, Williams L, Bridges TM, Daniels RN, Weaver D, Lindsley CW. Application of combinatorial chemistry science on modern drug discovery. Journal of Combinatorial Chemistry. 10: 345-54. PMID 18220367 DOI: 10.1021/Cc700187T |
0.749 |
|
| 2008 |
Lewis LM, Sheffler D, Williams R, Bridges TM, Kennedy JP, Brogan JT, Mulder MJ, Williams L, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW. Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. Bioorganic & Medicinal Chemistry Letters. 18: 885-90. PMID 18178088 DOI: 10.1016/J.Bmcl.2007.12.051 |
0.531 |
|
| 2008 |
Daniels RN, Kim K, Lebois EP, Muchalski H, Hughes M, Lindsley CW. Microwave-assisted protocols for the expedited synthesis of pyrazolo[1,5-a] and [3,4-d]pyrimidines Tetrahedron Letters. 49: 305-310. DOI: 10.1016/J.Tetlet.2007.11.054 |
0.794 |
|
| 2008 |
Ray WJ, Seager M, Ma L, Wittmann M, Getty K, Marlatt M, Crouthamel M, Wu G, Sankaranarayananan S, Simon A, Burno M, Jones K, Graufields VK, Bickel D, Posavec D, ... ... Lindsley C, et al. P4-305: Allosteric potentiation of the M1 muscarinic receptor provides unprecedented selectivity and a novel therapeutic strategy for the treatment of Alzheimer's disease Alzheimer's & Dementia. 4: T761-T761. DOI: 10.1016/J.Jalz.2008.05.2375 |
0.358 |
|
| 2008 |
Daniels RN, Kim K, Lebois EP, Muchalski H, Hughes M, Lindsley CW. ChemInform Abstract: Microwave-Assisted Protocols for the Expedited Synthesis of Pyrazolo[1,5-a] and [3,4-d]Pyrimidines. Cheminform. 39. DOI: 10.1002/chin.200816176 |
0.773 |
|
| 2007 |
Lindsley CW, Barnett SF, Yaroschak M, Bilodeau MT, Layton ME. Recent progress in the development of ATP-competitive and allosteric Akt kinase inhibitors. Current Topics in Medicinal Chemistry. 7: 1349-63. PMID 17692025 DOI: 10.2174/156802607781696864 |
0.614 |
|
| 2007 |
Daniels RN, Lindsley CW. A new, non-SSRI mechanism of action for Prozac. Current Topics in Medicinal Chemistry. 7: 1039. PMID 17563945 |
0.693 |
|
| 2007 |
Lindsley CW, Weaver D, Jones C, Marnett L, Conn PJ. Preclinical drug discovery research and training at Vanderbilt. Acs Chemical Biology. 2: 17-20. PMID 17243778 DOI: 10.1021/Cb6004867 |
0.304 |
|
| 2007 |
Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL, Jacobson MA, Wittman M, Ha SN, Schaffhauser H, Sur C, Pettibone DJ, Duggan ME, Conn PJ, Hartman GD, Lindsley CW. Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. Bioorganic & Medicinal Chemistry Letters. 17: 1386-91. PMID 17210250 DOI: 10.1016/J.Bmcl.2006.11.081 |
0.345 |
|
| 2007 |
Shipe WD, Yang F, Zhao Z, Wolkenberg SE, Nolt MB, Lindsley CW. Convenient and General Microwave-Assisted Protocols for the Expedient Synthesis of Heterocycles Cheminform. 38. DOI: 10.3987/Rev-06-Sr(W)1 |
0.319 |
|
| 2006 |
Lindsley CW, Wolkenberg SE, Kinney GG. Progress in the preparation and testing of glycine transporter type-1 (GlyT1) inhibitors. Current Topics in Medicinal Chemistry. 6: 1883-96. PMID 17017963 DOI: 10.2174/156802606778249784 |
0.312 |
|
| 2006 |
Zhao Z, O'Brien JA, Lemaire W, Williams DL, Jacobson MA, Sur C, Pettibone DJ, Tiller PR, Smith S, Hartman GD, Wolkenberg SE, Lindsley CW. Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides. Bioorganic & Medicinal Chemistry Letters. 16: 5968-72. PMID 16987662 DOI: 10.1016/J.Bmcl.2006.08.131 |
0.37 |
|
| 2006 |
Nanda KK, Nolt MB, Cato MJ, Kane SA, Kiss L, Spencer RH, Wang J, Lynch JJ, Regan CP, Stump GL, Li B, White R, Yeh S, Bogusky MJ, Bilodeau MT, ... ... Lindsley CW, et al. Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides. Bioorganic & Medicinal Chemistry Letters. 16: 5897-901. PMID 16949818 DOI: 10.1016/J.Bmcl.2006.08.054 |
0.349 |
|
| 2006 |
Lindsley CW, Zhao Z, Leister WH, O'Brien J, Lemaire W, Williams DL, Chen TB, Chang RS, Burno M, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, et al. Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides. Chemmedchem. 1: 807-11. PMID 16902933 DOI: 10.1002/Cmdc.200600097 |
0.308 |
|
| 2006 |
Wolkenberg SE, Zhao Z, Kapitskaya M, Webber AL, Petrukhin K, Tang YS, Dean DC, Hartman GD, Lindsley CW. Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand. Bioorganic & Medicinal Chemistry Letters. 16: 5001-4. PMID 16879962 DOI: 10.1016/J.Bmcl.2006.07.056 |
0.334 |
|
| 2006 |
Lindsley CW, Shipe WD, Wolkenberg SE, Theberge CR, Williams DL, Sur C, Kinney GG. Progress towards validating the NMDA receptor hypofunction hypothesis of schizophrenia. Current Topics in Medicinal Chemistry. 6: 771-85. PMID 16719816 DOI: 10.2174/156802606777057599 |
0.304 |
|
| 2006 |
Jesudason CD, Beavers LS, Cramer JW, Dill J, Finley DR, Lindsley CW, Stevens FC, Gadski RA, Oldham SW, Pickard RT, Siedem CS, Sindelar DK, Singh A, Watson BM, Hipskind PA. Synthesis and SAR of novel histamine H3 receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 16: 3415-8. PMID 16677814 DOI: 10.1016/J.Bmcl.2006.04.004 |
0.355 |
|
| 2005 |
Shipe WD, Wolkenberg SE, Lindsley CW. Accelerating lead development by microwave-enhanced medicinal chemistry. Drug Discovery Today. Technologies. 2: 155-61. PMID 24981843 DOI: 10.1016/J.Ddtec.2005.05.002 |
0.324 |
|
| 2005 |
Williams DL, Lindsley CW. Discovery of positive allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5). Current Topics in Medicinal Chemistry. 5: 825-46. PMID 16178729 DOI: 10.2174/1568026054750290 |
0.392 |
|
| 2005 |
Feuston BP, Chakravorty SJ, Conway JF, Culberson JC, Forbes J, Kraker B, Lennon PA, Lindsley C, McGaughey GB, Mosley R, Sheridan RP, Valenciano M, Kearsley SK. Web enabling technology for the design, enumeration, optimization and tracking of compound libraries. Current Topics in Medicinal Chemistry. 5: 773-83. PMID 16101417 DOI: 10.2174/1568026054637656 |
0.317 |
|
| 2005 |
Barnett SF, Bilodeau MT, Lindsley CW. The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation. Current Topics in Medicinal Chemistry. 5: 109-25. PMID 15853641 DOI: 10.2174/1568026053507714 |
0.305 |
|
| 2005 |
Zhao Z, Leister WH, Robinson RG, Barnett SF, Defeo-Jones D, Jones RE, Hartman GD, Huff JR, Huber HE, Duggan ME, Lindsley CW. Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors. Bioorganic & Medicinal Chemistry Letters. 15: 905-9. PMID 15686884 DOI: 10.1016/J.Bmcl.2004.12.062 |
0.318 |
|
| 2005 |
Lindsley CW, Zhao Z, Leister WH, Robinson RG, Barnett SF, Defeo-Jones D, Jones RE, Hartman GD, Huff JR, Huber HE, Duggan ME. Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorganic & Medicinal Chemistry Letters. 15: 761-4. PMID 15664853 DOI: 10.1016/J.Bmcl.2004.11.011 |
0.303 |
|
| 2005 |
Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, Smith S, Jacobson MA, Sur C, Duggan ME, Pettibone DJ, et al. A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models. The Journal of Pharmacology and Experimental Therapeutics. 313: 199-206. PMID 15608073 DOI: 10.1124/Jpet.104.079244 |
0.352 |
|
| 2005 |
Lindsley CW, Bogusky MJ, Leister WH, McClain RT, Robinson RG, Barnett SF, Defeo-Jones D, Ross CW, Hartman GD. Synthesis and biological evaluation of unnatural canthine alkaloids Tetrahedron Letters. 46: 2779-2782. DOI: 10.1016/J.Tetlet.2005.02.143 |
0.327 |
|
| 2004 |
Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, et al. Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. Journal of Medicinal Chemistry. 47: 5825-8. PMID 15537338 DOI: 10.1021/Jm049400D |
0.373 |
|
| 2004 |
Wolkenberg SE, Wisnoski DD, Leister WH, Wang Y, Zhao Z, Lindsley CW. Efficient synthesis of imidazoles from aldehydes and 1,2-diketones using microwave irradiation. Organic Letters. 6: 1453-6. PMID 15101765 DOI: 10.1021/Ol049682B |
0.318 |
|
| 2004 |
O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Schaffhauser HJ, Rowe B, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL. A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. The Journal of Pharmacology and Experimental Therapeutics. 309: 568-77. PMID 14747613 DOI: 10.1124/Jpet.103.061747 |
0.335 |
|
| 2004 |
Leister W, Strauss K, Wisnoski D, Zhao Z, Lindsley C. Development of a custom high-throughput preparative liquid chromatography/mass spectrometer platform for the preparative purification and analytical analysis of compound libraries. Journal of Combinatorial Chemistry. 5: 322-9. PMID 12739949 DOI: 10.1021/Cc0201041 |
0.322 |
|
| 2004 |
Ball DB, Wood M, Lindsley C, Mollard P, Buzard DJ, Vivian R, Mahoney M, Taft BR. Research, Teaching, and Professional Development at a Comprehensive University Journal of Chemical Education. 81: 1796. DOI: 10.1021/Ed081P1796 |
0.745 |
|
| 2003 |
O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Lindsley CW, Schaffhauser HJ, Sur C, Pettibone DJ, Conn PJ, Williams DL. A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Molecular Pharmacology. 64: 731-40. PMID 12920211 DOI: 10.1124/Mol.64.3.731 |
0.341 |
|
| 2001 |
Tallarico JA, Depew KM, Pelish HE, Westwood NJ, Lindsley CW, Shair MD, Schreiber SL, Foley MA. An alkylsilyl-tethered, high-capacity solid support amenable to diversity-oriented synthesis for one-bead, one-stock solution chemical genetics. Journal of Combinatorial Chemistry. 3: 312-8. PMID 11350255 DOI: 10.1021/Cc000107I |
0.779 |
|
| 2000 |
Lindsley CW, Chan LK, Goess BC, Joseph R, Shair MD. Solid-phase biomimetic synthesis of carpanone-like molecules Journal of the American Chemical Society. 122: 422-423. DOI: 10.1021/Ja993674M |
0.769 |
|
| 1998 |
Lipshutz BH, Ullman B, Lindsley C, Pecchi S, Buzard DJ, Dickson D. A New Bromo Trienyne: Synthesis of all-E, Conjugated Tetra-, Penta-, and Hexaenes Common to Oxo Polyene Macrolide Antibiotics. The Journal of Organic Chemistry. 63: 6092-6093. PMID 11672230 DOI: 10.1021/Jo981107W |
0.485 |
|
| 1997 |
Lipshutz BH, Lindsley C. A streamlined route to highly conjugated, all-E polyenes characteristic of oxo polyene macrolide antibiotics Journal of the American Chemical Society. 119: 4555-4556. DOI: 10.1021/Ja963930K |
0.503 |
|
| 1997 |
Lipshutz BH, Mollard P, Lindsley C, Chang V. Cyclo-SEM: A new carbonyl protecting group Tetrahedron Letters. 38: 1873-1876. DOI: 10.1016/S0040-4039(97)00239-6 |
0.635 |
|
| 1995 |
Lipshutz BH, Wood MR, Lindsley CW. Spectroscopic experiments on the role of Me3SiCl in lithium dialkylamide deprotonations Tetrahedron Letters. 36: 4385-4388. DOI: 10.1016/0040-4039(95)00856-8 |
0.445 |
|
| 1994 |
Lipshutz BH, Bhandari A, Lindsley C, Keil R, Wood MR. New synthetic methods based on organozirconium and organocopper chemistry Pure and Applied Chemistry. 66: 1493-1500. DOI: 10.1351/Pac199466071493 |
0.466 |
|
| 1994 |
Lipshutz BH, Lindsley C, Bhandari A. Expanding the versatility of Schwartz' reagent: Hydrozirconation of vinylic and acetylenic acyl silanes Tetrahedron Letters. 35: 4669-4672. DOI: 10.1016/S0040-4039(00)76937-1 |
0.484 |
|
| 1994 |
Lipshutz BH, Lindsley C, Susfalk R, Gross T. A convenient preparation of triisopropylsilyl acyl silanes Tetrahedron Letters. 35: 8999-9002. DOI: 10.1016/0040-4039(94)88410-2 |
0.453 |
|
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