Craig W. Lindsley, Ph.D. - Publications

Affiliations: 
2006- Pharmacology Vanderbilt University, Nashville, TN 
Website:
http://www.mc.vanderbilt.edu/labs/lindsley/lindsleycw.html

365 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2019 Presley CC, Perry CK, Childress ES, Mulder MJ, Luscombe VB, Rodriguez AL, Niswender CM, Conn PJ, Lindsley CW. Evaluation of Synthetic Cytochrome P-Mimetic Metalloporphyrins To Facilitate "Biomimetic" Biotransformation of a Series of mGlu Allosteric Ligands. Acs Omega. 4: 12782-12789. PMID 31460402 DOI: 10.1021/acsomega.9b02017  0.64
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  0.32
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  0.96
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  0.48
2019 Xiang Z, Lv X, Maksymetz J, Stansley BJ, Ghoshal A, Gogliotti RG, Niswender CM, Lindsley CW, Conn PJ. mGlu Positive Allosteric Modulators Facilitate Long-Term Potentiation via Disinhibition Mediated by mGlu-Endocannabinoid Signaling. Acs Pharmacology & Translational Science. 2: 198-209. PMID 31259318 DOI: 10.1021/acsptsci.9b00017  0.64
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  0.68
2019 Kharade SV, Sanchez-Andres JV, Fulton MG, Shelton EJ, Blobaum AL, Engers DW, Hofmann CS, Dadi PK, Lantier L, Jacobson DA, Lindsley CW, Denton JS. Structure-activity relationships, pharmacokinetics, and pharmacodynamics of the Kir6.2/SUR1-specific channel opener, VU0071063. The Journal of Pharmacology and Experimental Therapeutics. PMID 31201216 DOI: 10.1124/jpet.119.257204  0.6
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  0.64
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  0.8
2019 Iwaki Y, Yashiro K, Kokubo M, Mori T, Wieting JM, McGowan KM, Bridges TM, Engers DW, Denton JS, Kurata H, Lindsley CW. Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249. Bioorganic & Medicinal Chemistry Letters. PMID 31072652 DOI: 10.1016/j.bmcl.2019.04.048  0.48
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  0.64
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  0.64
2019 Abney KK, Bubser M, Du Y, Kozek KA, Bridges TM, Lindsley CW, Daniels JS, Morrison RD, Wickman K, Hopkins CR, Jones CK, Weaver CD. Correction to Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models. Acs Chemical Neuroscience. PMID 30912639 DOI: 10.1021/acschemneuro.9b00165  0.6
2019 Reed CW, Washecheck JP, Quitlag MC, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Jeffrey Conn P, Niswender CM, Lindsley CW. Surveying heterocycles as amide bioisosteres within a series of mGlu NAMs: Discovery of VU6019278. Bioorganic & Medicinal Chemistry Letters. PMID 30910459 DOI: 10.1016/j.bmcl.2019.03.016  0.6
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  0.64
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  0.64
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  0.32
2018 Fisher NM, Seto M, Lindsley CW, Niswender CM. Corrigendum: Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental Disorders. Frontiers in Molecular Neuroscience. 11: 444. PMID 30588231 DOI: 10.3389/fnmol.2018.00444  0.48
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  0.48
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  0.6
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  0.6
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  0.6
2018 Abney KK, Bubser M, Du Y, Kozek KA, Bridges TM, Lindsley CW, Daniels JS, Morrison RD, Wickman K, Hopkins CR, Jones CK, Weaver CD. Analgesic effects of the GIRK Activator, VU0466551, alone and in combination with morphine in acute and persistent pain models. Acs Chemical Neuroscience. PMID 30474955 DOI: 10.1021/acschemneuro.8b00370  0.6
2018 Friggeri L, Hargrove TY, Rachakonda G, Blobaum AL, Fisher P, de Oliveira GM, da Silva CF, Soeiro MNC, Nes WD, Lindsley CW, Villalta F, Guengerich FP, Lepesheva GI. Sterol 14α-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae. Journal of Medicinal Chemistry. PMID 30451500 DOI: 10.1021/acs.jmedchem.8b01671  0.6
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  0.6
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  0.48
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  0.68
2018 Joffe ME, Santiago CI, Stansley BJ, Maksymetz J, Gogliotti RG, Engers JL, Nicoletti F, Lindsley CW, Conn PJ. Mechanisms underlying prelimbic prefrontal cortex mGlu/mGlu-dependent plasticity and reversal learning deficits following acute stress. Neuropharmacology. PMID 30326237 DOI: 10.1016/j.neuropharm.2018.10.013  0.64
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  0.68
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  0.64
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  0.68
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  0.68
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  0.68
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  0.64
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  0.6
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  0.6
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  0.48
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  0.68
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  0.64
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  0.68
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  0.64
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  0.68
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  0.68
2018 Turner BD, Rook JM, Lindsley CW, Conn PJ, Grueter BA. mGlu and mGlu modulate distinct excitatory inputs to the nucleus accumbens shell. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 29654259 DOI: 10.1038/s41386-018-0049-1  0.64
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  0.68
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  0.68
2018 Berizzi AE, Perry CJ, Shackleford DM, Lindsley CW, Jones CK, Chen NA, Sexton PM, Christopoulos A, Langmead CJ, Lawrence AJ. Muscarinic Mreceptors modulate ethanol seeking in rats. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 29483658 DOI: 10.1038/s41386-017-0007-3  0.32
2018 Daniels AB, Froehler MT, Pierce JM, Nunnally AH, Calcutt MW, Bridges TM, LaNeve DC, Williams PE, Boyd KL, Reyzer ML, Lindsley CW, Friedman DL, Richmond A. Pharmacokinetics, Tissue Localization, Toxicity, and Treatment Efficacy in the First Small Animal (Rabbit) Model of Intra-Arterial Chemotherapy for Retinoblastoma. Investigative Ophthalmology & Visual Science. 59: 446-454. PMID 29368001 DOI: 10.1167/iovs.17-22302  0.48
2017 Joffe ME, Santiago CI, Engers JL, Lindsley CW, Conn PJ. Metabotropic glutamate receptor subtype 3 gates acute stress-induced dysregulation of amygdalo-cortical function. Molecular Psychiatry. PMID 29269844 DOI: 10.1038/s41380-017-0015-z  0.64
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  0.64
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  0.64
2017 Stansley BJ, Fisher NM, Gogliotti RG, Lindsley CW, Conn PJ, Niswender CM. Contextual Fear Extinction Induces Hippocampal Metaplasticity Mediated by Metabotropic Glutamate Receptor 5. Cerebral Cortex (New York, N.Y. : 1991). 1-14. PMID 29136107 DOI: 10.1093/cercor/bhx282  0.64
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  0.68
2017 Di Menna L, Joffe ME, Iacovelli L, Orlando R, Lindsley CW, Mairesse J, Gressèns P, Cannella M, Caraci F, Copani A, Bruno V, Battaglia G, Conn PJ, Nicoletti F. Functional partnership between mGlu3 and mGlu5 metabotropic glutamate receptors in the central nervous system. Neuropharmacology. PMID 29079293 DOI: 10.1016/j.neuropharm.2017.10.026  0.64
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  0.64
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  0.32
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  0.68
2017 Bender AM, Chopko TC, Bridges TM, Lindsley CW. Preparation of Unsymmetrical 1,2,4,5-Tetrazines via a Mild Suzuki Cross-Coupling Reaction. Organic Letters. PMID 28976768 DOI: 10.1021/acs.orglett.7b02868  0.48
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  0.64
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  0.64
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  0.68
2017 Crouch RD, Blobaum AL, Felts AS, Conn PJ, Lindsley CW. Species-specific involvement of aldehyde oxidase and xanthine oxidase in the metabolism of the pyrimidine-containing mGlu5 negative allosteric modulator VU0424238 (auglurant). Drug Metabolism and Disposition: the Biological Fate of Chemicals. PMID 28939686 DOI: 10.1124/dmd.117.077552  0.64
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  0.68
2017 Gogliotti RG, Senter RK, Fisher NM, Adams J, Zamorano R, Walker AG, Blobaum AL, Engers DW, Hopkin CR, Daniels JS, Jones CK, Lindsley CW, Xiang Z, Conn PJ, Niswender CM. mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome. Science Translational Medicine. 9. PMID 28814546 DOI: 10.1126/scitranslmed.aai7459  0.64
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  0.64
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  0.64
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  0.64
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  0.68
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  0.64
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  0.68
2017 Lindsley CW, Hopkins CR. The Return of D4 Dopamine Receptor Antagonists in Drug Discovery. Journal of Medicinal Chemistry. PMID 28489950 DOI: 10.1021/acs.jmedchem.7b00151  0.6
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  0.68
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  0.68
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  0.48
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  0.48
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  0.64
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  0.68
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  0.64
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  0.4
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  0.64
2017 Bender AM, Jones CK, Lindsley CW. Classics in Chemical Neuroscience: Xanomeline. Acs Chemical Neuroscience. PMID 28141924 DOI: 10.1021/acschemneuro.7b00001  0.32
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  0.68
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  0.64
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  0.68
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  0.64
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  0.68
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  0.6
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  0.6
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  0.6
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  0.64
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  0.68
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  0.6
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  0.96
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  0.96
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  0.96
2016 Garcia-Barrantes PM, Lindsley CW. Total Synthesis of Gombamide A. Organic Letters. PMID 27442228 DOI: 10.1021/acs.orglett.6b01825  0.48
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  0.6
2016 Shen W, Plotkin JL, Francardo V, Ko WK, Xie Z, Li Q, Fieblinger T, Wess J, Neubig RR, Lindsley CW, Conn PJ, Greengard P, Bezard E, Cenci MA, Surmeier DJ. M4 Muscarinic Receptor Signaling Ameliorates Striatal Plasticity Deficits in Models of L-DOPA-Induced Dyskinesia. Neuron. 90: 1139. PMID 27253449 DOI: 10.1016/j.neuron.2016.05.017  0.64
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  0.6
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  0.96
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  0.6
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  0.96
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  0.96
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  0.6
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  0.6
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  0.96
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  0.6
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  0.96
2016 Gogliotti RG, Klar R, Rook JM, Ghoshal A, Zamorano R, Malosh C, Stauffer SR, Bridges TM, Bartolome JM, Daniels JS, Jones C, Lindsley CW, Conn PJ, Niswender CM. mGlu5 Positive Allosteric Modulation Normalizes Synaptic Plasticity Defects and Motor Phenotypes in a Mouse Model of Rett Syndrome. Human Molecular Genetics. PMID 26936821 DOI: 10.1093/hmg/ddw074  0.64
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  0.96
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  0.96
2016 Balu DT, Li Y, Takagi S, Presti KT, Ramikie TS, Rook JM, Jones CK, Lindsley CW, Conn PJ, Bolshakov VY, Coyle JT. An mGlu5 Positive Allosteric Modulator Rescues the Neuroplasticity Deficits in a Genetic Model of NMDA Receptor Hypofunction in Schizophrenia. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 26741285 DOI: 10.1038/npp.2016.2  0.6
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  0.92
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  0.96
2015 Kharade SV, Flores D, Lindsley CW, Satlin LM, Denton JS. ROMK Inhibitor Actions in the Nephron Probed with Diuretics. American Journal of Physiology. Renal Physiology. ajprenal.00423.2015. PMID 26661652 DOI: 10.1152/ajprenal.00423.2015  0.6
2015 Gould RW, Nedelcovych MT, Gong X, Tsai E, Bubser M, Bridges TM, Wood MR, Duggan ME, Brandon NJ, Dunlop J, Wood MW, Ivarsson M, Noetzel MJ, Daniels JS, Niswender CM, ... Lindsley CW, et al. State-Dependent Alterations in Sleep/wake Architecture Elicited by the M4 PAM VU0467154- Relation to Antipsychotic-like Drug Effects. Neuropharmacology. PMID 26617071 DOI: 10.1016/j.neuropharm.2015.11.016  0.6
2015 Shen W, Plotkin JL, Francardo V, Ko WK, Xie Z, Li Q, Fieblinger T, Wess J, Neubig RR, Lindsley CW, Conn PJ, Greengard P, Bezard E, Cenci MA, Surmeier DJ. M4 Muscarinic Receptor Signaling Ameliorates Striatal Plasticity Deficits in Models of L-DOPA-Induced Dyskinesia. Neuron. 88: 762-773. PMID 26590347 DOI: 10.1016/j.neuron.2015.10.039  0.64
2015 Devergnas A, Chen E, Ma Y, Hamada I, Pittard D, Kammermeier S, Mullin AP, Faundez V, Lindsley CW, Jones C, Smith Y, Wichmann T. Anatomical Localization of CaV3.1 Calcium Channels and Electrophysiological Effects of T-type Calcium Channel Blockade in the Thalamus of MPTP-Treated Monkeys. Journal of Neurophysiology. jn.00858.2015. PMID 26538609 DOI: 10.1152/jn.00858.2015  0.6
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  0.6
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  0.6
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  0.64
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  0.96
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  0.6
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  0.4
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  0.96
2015 Ahowesso C, Black PN, Saini N, Montefusco D, Chekal J, Malosh C, Lindsley CW, Stauffer SR, DiRusso CC. Chemical inhibition of fatty acid absorption and cellular uptake limits lipotoxic cell death. Biochemical Pharmacology. 98: 167-81. PMID 26394026 DOI: 10.1016/j.bcp.2015.09.004  0.4
2015 Mitchener MM, Hermanson DJ, Shockley EM, Brown HA, Lindsley CW, Reese J, Rouzer CA, Lopez CF, Marnett LJ. Competition and allostery govern substrate selectivity of cyclooxygenase-2. Proceedings of the National Academy of Sciences of the United States of America. 112: 12366-71. PMID 26392530 DOI: 10.1073/pnas.1507307112  0.44
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  0.6
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  0.6
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  0.6
2015 Duvernay MT, Matafonov A, Lindsley CW, Hamm HE. Platelet Lipidomic Profiling: Novel Insight into Cytosolic Phospholipase A2α Activity and Its Role in Human Platelet Activation. Biochemistry. 54: 5578-88. PMID 26295742 DOI: 10.1021/acs.biochem.5b00549  0.4
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  0.64
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  0.96
2015 Gould RW, Dencker D, Grannan M, Bubser M, Zhan X, Wess J, Xiang Z, Locuson C, Lindsley CW, Conn PJ, Jones CK. A role for the M1 muscarinic acetylcholine receptor in top-down cognitive processing using a touchscreen visual discrimination task in mice. Acs Chemical Neuroscience. PMID 26176846 DOI: 10.1021/acschemneuro.5b00123  0.6
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  0.64
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  0.6
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  0.56
2015 Halambage UD, Wong JP, Melancon BJ, Lindsley CW, Aiken C. A Microplate-Based Assay for Identifying Small Molecules that Bind a Specific Intersubunit Interface Within the Assembled HIV-1 Capsid. Antimicrobial Agents and Chemotherapy. PMID 26077250 DOI: 10.1128/AAC.00646-15  0.6
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  0.96
2015 Taylor HE, Simmons GE, Mathews TP, Khatua AK, Popik W, Lindsley CW, D'Aquila RT, Brown HA. Phospholipase D1 Couples CD4+ T Cell Activation to c-Myc-Dependent Deoxyribonucleotide Pool Expansion and HIV-1 Replication. Plos Pathogens. 11: e1004864. PMID 26020637 DOI: 10.1371/journal.ppat.1004864  0.96
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  0.96
2015 Klar R, Walker AG, Ghose D, Grueter BA, Engers DW, Hopkins CR, Lindsley CW, Xiang Z, Conn PJ, Niswender CM. Activation of Metabotropic Glutamate Receptor 7 Is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the Hippocampus. The Journal of Neuroscience : the Official Journal of the Society For Neuroscience. 35: 7600-15. PMID 25972184 DOI: 10.1523/JNEUROSCI.4543-14.2015  0.96
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  0.96
2015 Du Y, Days E, Romaine I, Abney KK, Kaufmann K, Sulikowski G, Stauffer S, Lindsley CW, Weaver CD. Development and Validation of a Thallium Flux-Based Functional Assay for the Sodium Channel NaV1.7 and Its Utility for Lead Discovery and Compound Profiling. Acs Chemical Neuroscience. 6: 871-8. PMID 25879403 DOI: 10.1021/acschemneuro.5b00004  0.96
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  0.96
2015 Lindsley CW. 2014 global prescription medication statistics: strong growth and CNS well represented. Acs Chemical Neuroscience. 6: 505-6. PMID 25873191 DOI: 10.1021/acschemneuro.5b00098  0.96
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  0.96
2015 Burket JA, Benson AD, Green TL, Rook JM, Lindsley CW, Conn PJ, Deutsch SI. Effects of VU0410120, a novel GlyT1 inhibitor, on measures of sociability, cognition and stereotypic behaviors in a mouse model of autism. Progress in Neuro-Psychopharmacology & Biological Psychiatry. 61: 10-7. PMID 25784602 DOI: 10.1016/j.pnpbp.2015.03.003  0.6
2015 Lindsley CW. 2013 trends and statistics for prescription medications in the United States: CNS highest ranked and record number of prescriptions dispensed. Acs Chemical Neuroscience. 6: 356-7. PMID 25783498 DOI: 10.1021/acschemneuro.5b00049  0.96
2015 Iderberg H, Maslava N, Thompson AD, Bubser M, Niswender CM, Hopkins CR, Lindsley CW, Conn PJ, Jones CK, Cenci MA. Pharmacological stimulation of metabotropic glutamate receptor type 4 in a rat model of Parkinson's disease and l-DOPA-induced dyskinesia: Comparison between a positive allosteric modulator and an orthosteric agonist. Neuropharmacology. 95: 121-9. PMID 25749357 DOI: 10.1016/j.neuropharm.2015.02.023  0.96
2015 Lindsley CW. Momentum is building. Acs Chemical Neuroscience. 6: 207. PMID 25689884 DOI: 10.1021/acschemneuro.5b00039  0.96
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  0.96
2015 Mathews TP, Hill S, Rose KL, Ivanova PT, Lindsley CW, Brown HA. Human phospholipase D activity transiently regulates pyrimidine biosynthesis in malignant gliomas. Acs Chemical Biology. 10: 1258-68. PMID 25646564 DOI: 10.1021/cb500772c  0.96
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  0.96
2015 Nedelcovych MT, Gould RW, Zhan X, Bubser M, Gong X, Grannan M, Thompson AT, Ivarsson M, Lindsley CW, Conn PJ, Jones CK. A rodent model of traumatic stress induces lasting sleep and quantitative electroencephalographic disturbances. Acs Chemical Neuroscience. 6: 485-93. PMID 25581551 DOI: 10.1021/cn500342u  0.96
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  0.96
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  0.96
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  0.6
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  0.96
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  0.96
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  0.96
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  0.96
2015 Lindsley CW. 2014 Prescription Medications in the United States: Tremendous Growth, Specialty/Orphan Drug Expansion, and Dispensed Prescriptions Continue to Increase Acs Chemical Neuroscience. 6: 811-812. DOI: 10.1021/acschemneuro.5b00148  0.96
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  0.96
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  0.96
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  0.96
2014 Lindsley CW. Elevating standards for discoveries reported in ACS Chemical Neuroscience: new criteria to enhance reproducibility, experimental transparency, reliability, and the value of negative data. Acs Chemical Neuroscience. 5: 868-9. PMID 25315492 DOI: 10.1021/cn500208g  0.96
2014 Lindsley CW. Pharmacoeconomics and the medicinal chemist. Acs Medicinal Chemistry Letters. 5: 1066-8. PMID 25313315 DOI: 10.1021/ml500351u  0.96
2014 Tsugawa D, Oya Y, Masuzaki R, Ray K, Engers DW, Dib M, Do N, Kuramitsu K, Ho K, Frist A, Yu PB, Bloch KD, Lindsley CW, Hopkins CR, Hong CC, et al. Specific activin receptor-like kinase 3 inhibitors enhance liver regeneration. The Journal of Pharmacology and Experimental Therapeutics. 351: 549-58. PMID 25271257 DOI: 10.1124/jpet.114.216903  0.96
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  0.96
2014 Bruntz RC, Lindsley CW, Brown HA. Phospholipase D signaling pathways and phosphatidic acid as therapeutic targets in cancer. Pharmacological Reviews. 66: 1033-79. PMID 25244928 DOI: 10.1124/pr.114.009217  0.4
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2014 Oguin TH, Sharma S, Stuart AD, Duan S, Scott SA, Jones CK, Daniels JS, Lindsley CW, Thomas PG, Brown HA. Phospholipase D facilitates efficient entry of influenza virus, allowing escape from innate immune inhibition. The Journal of Biological Chemistry. 289: 25405-17. PMID 25065577 DOI: 10.1074/jbc.M114.558817  0.96
2014 Bates BS, Rodriguez AL, Felts AS, Morrison RD, Venable DF, Blobaum AL, Byers FW, Lawson KP, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorganic & Medicinal Chemistry Letters. 24: 3307-14. PMID 24969015 DOI: 10.1016/j.bmcl.2014.06.003  0.96
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  0.96
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, Martín-Martín 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  0.96
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  0.96
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  0.96
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  0.96
2014 Foster DJ, Gentry PR, Lizardi-Ortiz JE, Bridges TM, Wood MR, Niswender CM, Sulzer D, Lindsley CW, Xiang Z, Conn PJ. M5 receptor activation produces opposing physiological outcomes in dopamine neurons depending on the receptor's location. The Journal of Neuroscience : the Official Journal of the Society For Neuroscience. 34: 3253-62. PMID 24573284 DOI: 10.1523/JNEUROSCI.4896-13.2014  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2014 Scott SA, Mathews TP, Ivanova PT, Lindsley CW, Brown HA. Chemical modulation of glycerolipid signaling and metabolic pathways. Biochimica Et Biophysica Acta. 1841: 1060-84. PMID 24440821 DOI: 10.1016/j.bbalip.2014.01.009  0.96
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  0.96
2014 Bruntz RC, Taylor HE, Lindsley CW, Brown HA. Phospholipase D2 mediates survival signaling through direct regulation of Akt in glioblastoma cells. The Journal of Biological Chemistry. 289: 600-16. PMID 24257753 DOI: 10.1074/jbc.M113.532978  0.4
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  0.96
2014 Saunders C, Siuta M, Robertson SD, Davis AR, Sauer J, Matthies HJ, Gresch PJ, Airey DC, Lindsley CW, Schetz JA, Niswender KD, Veenstra-Vanderweele JM, Galli A. Neuronal ablation of p-Akt at Ser473 leads to altered 5-HT1A/2A receptor function. Neurochemistry International. 73: 113-21. PMID 24090638 DOI: 10.1016/j.neuint.2013.09.015  0.96
2014 Cipriano R, Bryson BL, Miskimen KL, Bartel CA, Hernandez-Sanchez W, Bruntz RC, Scott SA, Lindsley CW, Brown HA, Jackson MW. Hyperactivation of EGFR and downstream effector phospholipase D1 by oncogenic FAM83B. Oncogene. 33: 3298-306. PMID 23912460 DOI: 10.1038/onc.2013.293  0.96
2014 Lindsley CW. ACS chemical neuroscience in 2014 Acs Chemical Neuroscience. 5: 81. DOI: 10.1021/cn500011r  0.96
2014 Wenthur CJ, Bennett MR, Lindsley CW. Classics in chemical neuroscience: Fluoxetine (Prozac) Acs Chemical Neuroscience. 5: 14-23. DOI: 10.1021/cn400186j  0.96
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  0.96
2013 Lindsley CW. The end of an era and new beginnings for the editorial leadership of ACS Chemical Neuroscience. Acs Chemical Neuroscience. 4: 1415. PMID 24256220 DOI: 10.1021/cn400198c  0.96
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  0.4
2013 Schaldecker T, Kim S, Tarabanis C, Tian D, Hakroush S, Castonguay P, Ahn W, Wallentin H, Heid H, Hopkins CR, Lindsley CW, Riccio A, Buvall L, Weins A, Greka A. Inhibition of the TRPC5 ion channel protects the kidney filter. The Journal of Clinical Investigation. 123: 5298-309. PMID 24231357 DOI: 10.1172/JCI71165  0.96
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  0.96
2013 Schmitz Y, Castagna C, Mrejeru A, Lizardi-Ortiz JE, Klein Z, Lindsley CW, Sulzer D. Glycine transporter-1 inhibition promotes striatal axon sprouting via NMDA receptors in dopamine neurons. The Journal of Neuroscience : the Official Journal of the Society For Neuroscience. 33: 16778-89. PMID 24133278 DOI: 10.1523/JNEUROSCI.3041-12.2013  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2013 Wenthur CJ, Lindsley CW. Classics in chemical neuroscience: clozapine. Acs Chemical Neuroscience. 4: 1018-25. PMID 24047509 DOI: 10.1021/cn400121z  0.96
2013 Storaska AJ, Mei JP, Wu M, Li M, Wade SM, Blazer LL, Sjögren B, Hopkins CR, Lindsley CW, Lin Z, Babcock JJ, McManus OB, Neubig RR. Reversible inhibitors of regulators of G-protein signaling identified in a high-throughput cell-based calcium signaling assay. Cellular Signalling. 25: 2848-55. PMID 24041654 DOI: 10.1016/j.cellsig.2013.09.007  0.96
2013 O'Reilly MC, Lindsley CW. A general, enantioselective synthesis of β- and γ-fluoroamines. Tetrahedron Letters. 54: 3627-3629. PMID 24039308 DOI: 10.1016/j.tetlet.2013.04.116  0.96
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  0.96
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  0.96
2013 Lindsley CW. 2012 trends and statistics for prescription medications in the United States: CNS therapeutics continue to hold leading positions. Acs Chemical Neuroscience. 4: 1133-5. PMID 23962293 DOI: 10.1021/cn400127u  0.96
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  0.96
2013 Bartolomé-Nebreda JM, Conde-Ceide S, Delgado F, Iturrino L, Pastor J, Pena MÁ, 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  0.96
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  0.96
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  0.96
2013 Xu J, Zhu Y, Kraniotis S, He Q, Marshall JJ, Nomura T, Stauffer SR, Lindsley CW, Conn PJ, Contractor A. Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning. Learning & Memory (Cold Spring Harbor, N.Y.). 20: 438-45. PMID 23869026 DOI: 10.1101/lm.031666.113  0.96
2013 Lindsley CW. A new impact factor and new directions for ACS Chemical Neuroscience. Acs Chemical Neuroscience. 4: 1016. PMID 23859765 DOI: 10.1021/cn4001268  0.96
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  0.96
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  0.96
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  0.96
2013 Kaufmann K, Romaine I, Days E, Pascual C, Malik A, Yang L, Zou B, Du Y, Sliwoski G, Morrison RD, Denton J, Niswender CM, Daniels JS, Sulikowski GA, Xie XS, ... Lindsley CW, et al. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. Acs Chemical Neuroscience. 4: 1278-86. PMID 23730969 DOI: 10.1021/cn400062a  0.96
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  0.96
2013 Scott SA, Xiang Y, Mathews TP, Cho HP, Myers DS, Armstrong MD, Tallman KA, O'Reilly MC, Lindsley CW, Brown HA. Regulation of phospholipase D activity and phosphatidic acid production after purinergic (P2Y6) receptor stimulation. The Journal of Biological Chemistry. 288: 20477-87. PMID 23723068 DOI: 10.1074/jbc.M113.451708  0.96
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  0.96
2013 Amato RJ, Felts AS, Rodriguez AL, Venable DF, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Jones CK, Emmitte KA. Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction. Acs Chemical Neuroscience. 4: 1217-28. PMID 23682684 DOI: 10.1021/cn400070k  0.96
2013 Yu H, Lin Z, Mattmann ME, Zou B, Terrenoire C, Zhang H, Wu M, McManus OB, Kass RS, Lindsley CW, Hopkins CR, Li M. Dynamic subunit stoichiometry confers a progressive continuum of pharmacological sensitivity by KCNQ potassium channels. Proceedings of the National Academy of Sciences of the United States of America. 110: 8732-7. PMID 23650380 DOI: 10.1073/pnas.1300684110  0.96
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  0.96
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  0.96
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  0.96
2013 Lindsley CW. New hope for multiple sclerosis patients Acs Chemical Neuroscience. 4: 368. PMID 23509970 DOI: 10.1021/cn400059g  0.96
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  0.96
2013 O'Reilly MC, Scott SA, Brown KA, Oguin TH, Thomas PG, Daniels JS, Morrison R, Brown HA, Lindsley CW. Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. Journal of Medicinal Chemistry. 56: 2695-9. PMID 23445448 DOI: 10.1021/jm301782e  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2013 D'Amore V, Santolini I, van Rijn CM, Biagioni F, Molinaro G, Prete A, Conn PJ, Lindsley CW, Zhou Y, Vinson PN, Rodriguez AL, Jones CK, Stauffer SR, Nicoletti F, van Luijtelaar G, et al. Potentiation of mGlu5 receptors with the novel enhancer, VU0360172, reduces spontaneous absence seizures in WAG/Rij rats. Neuropharmacology. 66: 330-8. PMID 22705340 DOI: 10.1016/j.neuropharm.2012.05.044  0.96
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 to mGlu5 signaling (Molecular Pharmacology (2013) 83, (835-847)) Molecular Pharmacology. 84: 654. DOI: 10.1124/mol.113.10er13  0.96
2013 Free RB, Conroy JL, Roof RA, Doyle T, Han Y, Donthamsetti P, Javitch JA, Southall N, Emmitte K, Lindsley C, Ferrer M, Sibley DR. High-Throughput Screening for Modulators of the D2 Dopamine Receptor Yields Unique and Selective Pharmacological Chemotypes Catecholamine Research in the 21st Century: Abstracts and Graphical Abstracts, 10th International Catecholamine Symposium, 2012. 115. DOI: 10.1016/B978-0-12-800044-1.00101-X  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2012 Lindsley CW. Alzheimers disease: Development of disease-modifying treatments is the challenge for our generation Acs Chemical Neuroscience. 3: 804-805. PMID 23173063 DOI: 10.1021/cn300190f  0.96
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 mGluâ‚… 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  0.96
2012 Panarese JD, Lindsley CW. Biomimetic synthesis and biological evaluation of aplidiopsamine A Organic Letters. 14: 5808-5810. PMID 23106227 DOI: 10.1021/ol3024665  0.96
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 M₁ antagonists. Bioorganic & Medicinal Chemistry Letters. 22: 6923-8. PMID 23062550 DOI: 10.1016/j.bmcl.2012.09.011  0.96
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  0.96
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  0.96
2012 Voss J, Ebert A, Wolfe M, Lindsley C, Cookson M, Deane R. The future of neurodegenerative diseases: emerging targets, treatments and technologies. Future Medicinal Chemistry. 4: 1661-9. PMID 22924504 DOI: 10.4155/fmc.12.118  0.96
2012 Mattmann ME, Yu H, Lin Z, Xu K, Huang X, Long S, Wu M, McManus OB, Engers DW, Le UM, Li M, Lindsley CW, Hopkins CR. Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator. Bioorganic & Medicinal Chemistry Letters. 22: 5936-41. PMID 22910039 DOI: 10.1016/j.bmcl.2012.07.060  0.96
2012 Lindsley CW. The top prescription drugs of 2011 in the United States: Antipsychotics and antidepressants once again lead CNS therapeutics Acs Chemical Neuroscience. 3: 630-631. PMID 22896807 DOI: 10.1021/cn3000923  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2012 Conrad KL, Davis AR, Silberman Y, Sheffler DJ, Shields AD, Saleh SA, Sen N, Matthies HJ, Javitch JA, Lindsley CW, Winder DG. Yohimbine depresses excitatory transmission in BNST and impairs extinction of cocaine place preference through orexin-dependent, norepinephrine-independent processes. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 37: 2253-66. PMID 22617356 DOI: 10.1038/npp.2012.76  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2012 Senter TJ, Fadeyi OO, Lindsley CW. Enantioselective total synthesis of (+)-amabiline. Organic Letters. 14: 1869-71. PMID 22432912 DOI: 10.1021/ol300466a  0.96
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 (mGluâ‚…): from an artificial neural network virtual screen to an in vivo tool compound. Chemmedchem. 7: 406-14. PMID 22267125 DOI: 10.1002/cmdc.201100510  0.96
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  0.96
2012 Theriault JR, Felts AS, Bates BS, Perez JR, Palmer M, Gilbert SR, Dawson ES, Engers JL, Lindsley CW, Emmitte KA. Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway. Bioorganic & Medicinal Chemistry Letters. 22: 76-81. PMID 22172704 DOI: 10.1016/j.bmcl.2011.11.077  0.96
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  0.96
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  0.96
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  0.96
2012 Jones CK, Bubser M, Thompson AD, Dickerson JW, Turle-Lorenzo N, Amalric M, Blobaum AL, Bridges TM, Morrison RD, Jadhav S, Engers DW, Italiano K, Bode J, Daniels JS, Lindsley CW, et al. The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease. The Journal of Pharmacology and Experimental Therapeutics. 340: 404-21. PMID 22088953 DOI: 10.1124/jpet.111.187443  0.96
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  0.96
2012 Lindsley CW. Call for papers! A special thematic compilation/special issue crossover with the journal of medicinal chemistry and ACS medicinal chemistry letters focused on Alzheimer's disease Acs Chemical Neuroscience. 3: 147. DOI: 10.1021/cn300021c  0.96
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. DOI: 10.1021/cn200102d  0.96
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  0.96
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  0.96
2012 Lindsley CW, Weaver D, Bridges TM, Kennedy JP. Lead Optimization in Drug Discovery Chemical Biology: Approaches to Drug Discovery and Development to Targeting Disease. 65-81. DOI: 10.1002/9781118435762.ch4  0.96
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  0.96
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  0.96
2011 Lindsley CW. The top prescription drugs of 2010 in the United States: Antipsychotics show strong growth Acs Chemical Neuroscience. 2: 276-277. PMID 22778870 DOI: 10.1021/cn200050c  0.96
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  0.96
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  0.96
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  0.96
2011 Yu H, Wu M, Townsend SD, Zou B, Long S, Daniels JS, McManus OB, Li M, Lindsley CW, Hopkins CR. Discovery, Synthesis, and Structure Activity Relationship of a Series of N-Aryl- bicyclo[2.2.1]heptane-2-carboxamides: Characterization of ML213 as a Novel KCNQ2 and KCNQ4 Potassium Channel Opener. Acs Chemical Neuroscience. 2: 572-577. PMID 22125664 DOI: 10.1021/cn200065b  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2011 Wang HR, Wu M, Yu H, Long S, Stevens A, Engers DW, Sackin H, Daniels JS, Dawson ES, Hopkins CR, Lindsley CW, Li M, McManus OB. Selective inhibition of the K(ir)2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR, and pharmacological characterization of ML133. Acs Chemical Biology. 6: 845-56. PMID 21615117 DOI: 10.1021/cb200146a  0.96
2011 Norton LJ, Zhang Q, Saqib KM, Schrewe H, Macura K, Anderson KE, Lindsley CW, Brown HA, Rudge SA, Wakelam MJO. PLD1 rather than PLD2 regulates phorbol-ester-, adhesion-dependent and Fcγ-receptor-stimulated ROS production in neutrophils Journal of Cell Science. 124: 1973-1983. PMID 21610093 DOI: 10.1242/jcs.082008  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2011 Lindsley CW. A special "reviews" issue on the chemical senses Acs Chemical Neuroscience. 2: 1. DOI: 10.1021/cn1001073  0.96
2011 Lindsley CW, Hopkins CR, Sulikowski GA. Biomimetic Synthesis of Lignans Biomimetic Organic Synthesis. 2: 677-693. DOI: 10.1002/9783527634606.ch18  0.96
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  0.96
2010 Lindsley CW. (S)-(+)-mecamylamine (TC-5214): A neuronal nicotinic receptor modulator enters phase III trials as an adjunct treatment for major depressive disorder (MDD) Acs Chemical Neuroscience. 1: 530-531. PMID 22778844 DOI: 10.1021/cn100070s  0.96
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  0.96
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  0.96
2010 Lindsley CW. Horners syndrome and neuroblastoma: Our familys odyssey with disorders of the sympathetic nervous system Acs Chemical Neuroscience. 1: 649-651. PMID 22778806 DOI: 10.1021/cn100091k  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2010 Engers DW, Gentry PR, Williams R, Bolinger JD, Weaver CD, Menon UN, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorganic & Medicinal Chemistry Letters. 20: 5175-8. PMID 20667732 DOI: 10.1016/j.bmcl.2010.07.007  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2010 Lindsley CW. The last issue of our inaugural year: Reflections and a view to the future Acs Chemical Neuroscience. 1: 770-771. DOI: 10.1021/cn1001057  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2009 Fadeyi OO, Lindsley CW. Total synthesis of brevisamide. Organic Letters. 11: 3950-2. PMID 19639953 DOI: 10.1021/ol9015755  0.96
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  0.68
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
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  0.96
2007 Daniels RN, Lindsley CW. A new, non-SSRI mechanism of action for Prozac. Current Topics in Medicinal Chemistry. 7: 1039. PMID 17563945  0.96
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  0.96
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