| Year |
Citation |
Score |
| 2020 |
Vadukoot AK, Sharma S, Aretz CD, Kumar S, Gautam N, Alnouti Y, Aldrich AL, Heim CE, Kielian T, Hopkins CR. Synthesis and SAR Studies of 1-Pyrrolo[2,3-]pyridine-2-carboxamides as Phosphodiesterase 4B (PDE4B) Inhibitors. Acs Medicinal Chemistry Letters. 11: 1848-1854. PMID 33062163 DOI: 10.1021/Acsmedchemlett.9B00369 |
0.371 |
|
| 2020 |
Aretz C, Kharade SV, Chronister K, Trigueros RR, Rodriguez EM, Piermarini PM, Denton JS, Hopkins CR. Further SAR on the (phenylsulfonyl)piperazine scaffold as inhibitors of the Aedes aegypti Kir1 (AeKir) channel and larvicides. Chemmedchem. PMID 32926544 DOI: 10.1002/Cmdc.202000598 |
0.346 |
|
| 2020 |
Engers DW, Bollinger SR, Felts AS, Vadukoot AK, Williams CH, Blobaum AL, Lindsley CW, Hong CC, Hopkins CR. Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors. Bioorganic & Medicinal Chemistry Letters. 30: 127418. PMID 32750526 DOI: 10.1016/J.Bmcl.2020.127418 |
0.304 |
|
| 2020 |
Antonio-Tolentino K, Hopkins CR. Selective α7 nicotinic receptor agonists and positive allosteric modulators for the treatment of schizophrenia - a review. Expert Opinion On Investigational Drugs. 1-7. PMID 32396418 DOI: 10.1080/13543784.2020.1764938 |
0.33 |
|
| 2019 |
Aretz CD, Vadukoot AK, Hopkins CR. Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics. Journal of Medicinal Chemistry. PMID 31034224 DOI: 10.1021/Acs.Jmedchem.8B01891 |
0.334 |
|
| 2019 |
Sharma S, Hopkins CR. A review of transient receptor potential channel (TRPC) modulators and diseases. Journal of Medicinal Chemistry. PMID 30943030 DOI: 10.1021/Acs.Jmedchem.8B01954 |
0.352 |
|
| 2019 |
Vo BN, Abney KK, Anderson A, Marron Fernandez de Velasco E, Benneyworth MA, Daniels JS, Morrison RD, Hopkins CR, Weaver CD, Wickman K. VU0810464, a non-urea GIRK channel activator, exhibits enhanced selectivity for neuronal GIRK channels and reduces stress-induced hyperthermia in mice. British Journal of Pharmacology. PMID 30924523 DOI: 10.1111/Bph.14671 |
0.31 |
|
| 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, ... ... Hopkins CR, 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 |
0.332 |
|
| 2019 |
Aretz C, Morwitzer MJ, Sanford A, Hogan AM, Portillo M, Kharade SV, Kramer M, Mcarthey J, Trigueros RR, Piermarini PM, Denton JS, Hopkins CR. Discovery and characterization of 2-nitro-5-(4-(phenylsulfonyl)piperazin-1-yl)-N-(pyridin-4-ylmethyl)anilines as novel inhibitors of the Aedes aegypti Kir1 (AeKir1) channel. Acs Infectious Diseases. PMID 30832472 DOI: 10.1021/Acsinfecdis.8B00368 |
0.361 |
|
| 2019 |
Sharma S, Kozek KA, Abney KK, Kumar S, Gautam N, Alnouti Y, David Weaver C, Hopkins CR. Discovery, synthesis and characterization of a series of (1-alkyl-3-methyl-1H-pyrazol-5-yl)-2-(5-aryl-2H-tetrazol-2-yl)acetamides as novel GIRK1/2 potassium channel activators. Bioorganic & Medicinal Chemistry Letters. PMID 30718161 DOI: 10.1016/J.Bmcl.2019.01.027 |
0.353 |
|
| 2019 |
Sharma SH, Pablo JL, Montesinos MS, Greka A, Hopkins CR. Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903. Bioorganic & Medicinal Chemistry Letters. 29: 155-159. PMID 30538066 DOI: 10.1016/J.Bmcl.2018.12.007 |
0.402 |
|
| 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, ... ... Hopkins CR, 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 |
0.322 |
|
| 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 |
0.318 |
|
| 2018 |
Rusconi Trigueros R, Hopkins CR, Denton JS, Piermarini PM. Pharmacological Inhibition of Inward Rectifier Potassium Channels Induces Lethality in Larval . Insects. 9. PMID 30445675 DOI: 10.3390/Insects9040163 |
0.345 |
|
| 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 |
0.347 |
|
| 2018 |
Piermarini PM, Inocente EA, Acosta N, Hopkins CR, Denton JS, Michel AP. Inward rectifier potassium (Kir) channels in the soybean aphid Aphis glycines: Functional characterization, pharmacology, and toxicology. Journal of Insect Physiology. 110: 57-65. PMID 30196125 DOI: 10.1016/J.Jinsphys.2018.09.001 |
0.325 |
|
| 2018 |
Kozek KA, Du Y, Sharma S, Prael FJ, Spitznagel BD, Kharade SV, Denton JS, Hopkins CR, Weaver CD. Discovery and Characterization of VU0529331, a Synthetic Small-Molecule Activator of Homomeric G Protein-gated, Inwardly-rectifying, Potassium (GIRK) Channels. Acs Chemical Neuroscience. PMID 30136838 DOI: 10.1021/Acschemneuro.8B00287 |
0.339 |
|
| 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, ... Hopkins CR, 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 |
0.373 |
|
| 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 |
0.382 |
|
| 2017 |
Zhou Y, Castonguay P, Sidhom EH, Clark AR, Dvela-Levitt M, Kim S, Sieber J, Wieder N, Jung JY, Andreeva S, Reichardt J, Dubois F, Hoffmann SC, Basgen JM, Montesinos MS, ... ... Hopkins CR, et al. A small-molecule inhibitor of TRPC5 ion channels suppresses progressive kidney disease in animal models. Science (New York, N.Y.). 358: 1332-1336. PMID 29217578 DOI: 10.1126/Science.Aal4178 |
0.318 |
|
| 2017 |
Wieting JM, Vadukoot AK, Sharma SH, Abney KK, Bridges TM, Daniels JS, Morrison RD, Wickman K, Weaver CD, Hopkins CR. Discovery and characterization of 1H-pyrazol-5-yl-2-phenylacetamides as novel, non-urea containing GIRK1/2 potassium channel activators. Acs Chemical Neuroscience. PMID 28697302 DOI: 10.1021/Acschemneuro.7B00217 |
0.369 |
|
| 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 |
0.321 |
|
| 2016 |
Swale DR, Engers DW, Bollinger SR, Gross A, Inocente EA, Days E, Kanga F, Johnson RM, Yang L, Bloomquist JR, Hopkins CR, Piermarini PM, Denton JS. An insecticide resistance-breaking mosquitocide targeting inward rectifier potassium channels in vectors of Zika virus and malaria. Scientific Reports. 6: 36954. PMID 27849039 DOI: 10.1038/Srep36954 |
0.329 |
|
| 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 |
0.348 |
|
| 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 |
0.354 |
|
| 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, ... ... Hopkins CR, 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 |
0.325 |
|
| 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 |
0.378 |
|
| 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 |
0.339 |
|
| 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 |
0.32 |
|
| 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, ... ... Hopkins CR, 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 |
0.363 |
|
| 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 |
0.339 |
|
| 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 |
0.381 |
|
| 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 |
0.311 |
|
| 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 |
0.331 |
|
| 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 |
0.352 |
|
| 2014 |
Raphemot R, Rouhier MF, Swale DR, Days E, Weaver CD, Lovell KM, Konkel LC, Engers DW, Bollinger SR, Bollinger SF, Hopkins C, Piermarini PM, Denton JS. Discovery and characterization of a potent and selective inhibitor of Aedes aegypti inward rectifier potassium channels. Plos One. 9: e110772. PMID 25375326 DOI: 10.1371/Journal.Pone.0110772 |
0.408 |
|
| 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 |
0.304 |
|
| 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, ... ... Hopkins CR, 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 |
0.34 |
|
| 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 |
0.318 |
|
| 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 |
0.324 |
|
| 2013 |
Raphemot R, Rouhier MF, Hopkins CR, Gogliotti RD, Lovell KM, Hine RM, Ghosalkar D, Longo A, Beyenbach KW, Denton JS, Piermarini PM. Eliciting renal failure in mosquitoes with a small-molecule inhibitor of inward-rectifying potassium channels. Plos One. 8: e64905. PMID 23734226 DOI: 10.1371/Journal.Pone.0064905 |
0.336 |
|
| 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 |
0.315 |
|
| 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 |
0.378 |
|
| 2013 |
Sheffler DJ, Sevel C, Le U, Lovell KM, Tarr JC, Carrington SJ, Cho HP, Digby GJ, Niswender CM, Conn PJ, Hopkins CR, Wood MR, Lindsley CW. Further exploration of Mâ‚ allosteric agonists: subtle structural changes abolish Mâ‚ allosteric agonism and result in pan-mAChR orthosteric antagonism. Bioorganic & Medicinal Chemistry Letters. 23: 223-7. PMID 23200253 DOI: 10.1016/J.Bmcl.2012.10.132 |
0.301 |
|
| 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, ... ... Hopkins CR, 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 |
0.362 |
|
| 2012 |
Potet F, Lorinc AN, Chaigne S, Hopkins CR, Venkataraman R, Stepanovic SZ, Lewis LM, Days E, Sidorov VY, Engers DW, Zou B, Afshartous D, George AL, Campbell CM, Balser JR, et al. Identification and characterization of a compound that protects cardiac tissue from human Ether-Ã -go-go-related gene (hERG)-related drug-induced arrhythmias. The Journal of Biological Chemistry. 287: 39613-25. PMID 23033485 DOI: 10.1074/Jbc.M112.380162 |
0.35 |
|
| 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 |
0.343 |
|
| 2012 |
Neely MD, Litt MJ, Tidball AM, Li GG, Aboud AA, Hopkins CR, Chamberlin R, Hong CC, Ess KC, Bowman AB. DMH1, a highly selective small molecule BMP inhibitor promotes neurogenesis of hiPSCs: comparison of PAX6 and SOX1 expression during neural induction. Acs Chemical Neuroscience. 3: 482-91. PMID 22860217 DOI: 10.1021/Cn300029T |
0.307 |
|
| 2012 |
Hopkins CR. ACS chemical neuroscience molecule spotlight on BMS-708163. Acs Chemical Neuroscience. 3: 149-50. PMID 22860183 DOI: 10.1021/Cn3000179 |
0.301 |
|
| 2012 |
Hopkins CR. ACS chemical neuroscience molecule spotlight on Begacestat (GSI-953). Acs Chemical Neuroscience. 3: 3-4. PMID 22860177 DOI: 10.1021/Cn200124U |
0.32 |
|
| 2012 |
Cheung YY, Yu H, Xu K, Zou B, Wu M, McManus OB, Li M, Lindsley CW, Hopkins CR. Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor. Journal of Medicinal Chemistry. 55: 6975-9. PMID 22793372 DOI: 10.1021/Jm300700V |
0.376 |
|
| 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 |
0.316 |
|
| 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 |
0.353 |
|
| 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 |
0.32 |
|
| 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 |
0.332 |
|
| 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, ... Hopkins CR, 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 |
0.307 |
|
| 2012 |
Potet F, Lorinc A, Hopkins C, Venkataraman R, Chaigne S, Stepanovic S, Lindsley C, Baudenbacher F, Kupershmidt S. Characterization of a Compound that Reduces Sensitivity to HERG Inhibitors and Prevents hERG-Related, Drug-Induced Arrhythmias in Isolated Rabbit Hearts Biophysical Journal. 102: 14a. DOI: 10.1016/J.Bpj.2011.11.101 |
0.336 |
|
| 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 |
0.351 |
|
| 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 |
0.386 |
|
| 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 |
0.349 |
|
| 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 |
0.324 |
|
| 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, ... ... Hopkins CR, 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 |
0.362 |
|
| 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 |
0.372 |
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| 2011 |
Wood MR, Hopkins CR, Brogan JT, Conn PJ, Lindsley CW. "Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology. Biochemistry. 50: 2403-10. PMID 21341760 DOI: 10.1021/Bi200129S |
0.326 |
|
| 2011 |
Cheung YY, Zamorano R, Blobaum AL, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGluâ‚„. Acs Combinatorial Science. 13: 159-65. PMID 21338051 DOI: 10.1021/Co1000508 |
0.33 |
|
| 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 |
0.341 |
|
| 2010 |
Hopkins CR. ACS chemical neuroscience molecule spotlight on semagacestat (LY450139). Acs Chemical Neuroscience. 1: 533-4. PMID 22778845 DOI: 10.1021/Cn1000606 |
0.301 |
|
| 2010 |
Hopkins CR. ACS chemical neuroscience molecule spotlight on savella. Acs Chemical Neuroscience. 1: 345. PMID 22778830 DOI: 10.1021/Cn1000233 |
0.322 |
|
| 2010 |
Hopkins CR. ACS chemical neuroscience molecule spotlight on Valdoxen. Acs Chemical Neuroscience. 1: 772-3. PMID 22778814 DOI: 10.1021/Cn100062J |
0.304 |
|
| 2010 |
Hopkins CR. ACS chemical neuroscience molecule spotlight on Lorcaserin. Acs Chemical Neuroscience. 1: 718-9. PMID 22778808 DOI: 10.1021/Cn100059U |
0.31 |
|
| 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 |
0.331 |
|
| 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 |
0.354 |
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| 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 |
0.319 |
|
| 2010 |
Wipf P, Hopkins CR. ChemInform Abstract: Enantioselective Synthesis of the AB-Ring System of the Antitumor Antibiotic Tetrazomine. Cheminform. 32: no-no. DOI: 10.1002/chin.200137226 |
0.332 |
|
| 2010 |
Wipf P, Hopkins CR. ChemInform Abstract: Efficient Synthesis of 1,4-Dihydro-2H-isoquinoline-3,5,8-triones via Cyclobutene Ring Expansion. Cheminform. 31: no-no. DOI: 10.1002/chin.200002165 |
0.347 |
|
| 2009 |
Hopkins CR, Lindsley CW, Niswender CM. mGluR4-positive allosteric modulation as potential treatment for Parkinson's disease. Future Medicinal Chemistry. 1: 501-13. PMID 20161443 DOI: 10.4155/Fmc.09.38 |
0.31 |
|
| 2009 |
Lindsley CW, Niswender CM, Engers DW, Hopkins CR. Recent progress in the development of mGluR4 positive allosteric modulators for the treatment of Parkinson's disease. Current Topics in Medicinal Chemistry. 9: 949-63. PMID 19754407 DOI: 10.2174/156802609789378272 |
0.361 |
|
| 2009 |
Williams R, Johnson KA, Gentry PR, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4). Bioorganic & Medicinal Chemistry Letters. 19: 4967-70. PMID 19640716 DOI: 10.1016/J.Bmcl.2009.07.072 |
0.374 |
|
| 2009 |
Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). Journal of Medicinal Chemistry. 52: 4115-8. PMID 19469556 DOI: 10.1021/Jm9005065 |
0.334 |
|
| 2006 |
Hopkins CR, O'neil SV, Laufersweiler MC, Wang Y, Pokross M, Mekel M, Evdokimov A, Walter R, Kontoyianni M, Petrey ME, Sabatakos G, Roesgen JT, Richardson E, Demuth TP. Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-gamma binding agents with potential application to the treatment of osteoporosis. Bioorganic & Medicinal Chemistry Letters. 16: 5659-63. PMID 16919947 DOI: 10.1016/J.Bmcl.2006.08.003 |
0.33 |
|
| 2006 |
Maier JA, Brugel TA, Sabat M, Golebiowski A, Laufersweiler MJ, VanRens JC, Hopkins CR, De B, Hsieh LC, Brown KK, Easwaran V, Janusz MJ. Development of N-4,6-pyrimidine-N-alkyl-N'-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase. Bioorganic & Medicinal Chemistry Letters. 16: 3646-50. PMID 16682201 DOI: 10.1016/J.Bmcl.2006.04.072 |
0.3 |
|
| 2005 |
Hopkins CR, Czekaj M, Kaye SS, Gao Z, Pribish J, Pauls H, Liang G, Sides K, Cramer D, Cairns J, Luo Y, Lim HK, Vaz R, Rebello S, Maignan S, et al. Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase. Bioorganic & Medicinal Chemistry Letters. 15: 2734-7. PMID 15911249 DOI: 10.1016/J.Bmcl.2005.04.002 |
0.359 |
|
| 2004 |
Hopkins C, Neuenschwander K, Scotese A, Jackson S, Nieduzak T, Pauls H, Liang G, Sides K, Cramer D, Cairns J, Maignan S, Mathieu M. Novel pyrazinone inhibitors of mast cell tryptase: Synthesis and SAR evaluation Bioorganic and Medicinal Chemistry Letters. 14: 4819-4823. PMID 15341931 DOI: 10.1016/J.Bmcl.2004.07.051 |
0.312 |
|
| 2002 |
Wipf P, Hopkins CR, Phillips EO, Lazo JS. Separation of Cdc25 dual specificity phosphatase inhibition and DNA cleaving activities in a focused library of analogs of the antitumor antibiotic Dnacin Tetrahedron. 58: 6367-6372. DOI: 10.1016/S0040-4020(02)00636-1 |
0.429 |
|
| 2001 |
Wipf P, Hopkins CR. Enantioselective synthesis of the AB-ring system of the antitumor antibiotic tetrazomine. The Journal of Organic Chemistry. 66: 3133-9. PMID 11325279 DOI: 10.1021/Jo015512Q |
0.42 |
|
| 1999 |
Wipf P, Hopkins CR. Efficient Synthesis of 1,4-Dihydro-2H-isoquinoline-3,5,8-triones via Cyclobutene Ring Expansion. The Journal of Organic Chemistry. 64: 6881-6887. PMID 11674700 DOI: 10.1021/Jo990089V |
0.424 |
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