Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability BEL Lauffer, R Mintzer, R Fong, S Mukund, C Tam, I Zilberleyb, B Flicke, ... Journal of Biological Chemistry 288 (37), 26926-26943, 2013 | 429 | 2013 |
Structural basis of Nav1. 7 inhibition by an isoform-selective small-molecule antagonist S Ahuja, S Mukund, L Deng, K Khakh, E Chang, H Ho, S Shriver, C Young, ... Science 350 (6267), aac5464, 2015 | 328 | 2015 |
Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects AR Johnson, AG Pavlovsky, DF Ortwine, F Prior, CF Man, DA Bornemeier, ... Journal of Biological Chemistry 282 (38), 27781-27791, 2007 | 252 | 2007 |
Discovery of GDC-0853: a potent, selective, and noncovalent Bruton’s tyrosine kinase inhibitor in early clinical development JJ Crawford, AR Johnson, DL Misner, LD Belmont, G Castanedo, R Choy, ... Journal of medicinal chemistry 61 (6), 2227-2245, 2018 | 233 | 2018 |
Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl) ethyl]-2H-pyran 2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing … BD Roth, CJ Blankley, AW Chucholowski, E Ferguson, ML Hoefle, ... Journal of medicinal chemistry 34 (1), 357-366, 1991 | 219 | 1991 |
X-ray structure of a hydroxamate inhibitor complex of stromelysin catalytic domain and its comparison with members of the zinc metalloproteinase superfamily V Dhanaraj, QZ Ye, LL Johnson, DJ Hupe, DF Ortwine, JB Dunbar Jr, ... Structure 4 (4), 375-386, 1996 | 163 | 1996 |
Recent advances in the synthetic chemistry of bicyclo [1.1. 1] pentane J Kanazawa, M Uchiyama Synlett 30 (01), 1-11, 2019 | 151 | 2019 |
Substituted 2-benzothiazolamines as sodium flux inhibitors: quantitative structure-activity relationships and anticonvulsant activity SJ Hays, MJ Rice, DF Ortwine, G Johnson, RD Schwarz, DK Boyd, ... Journal of pharmaceutical sciences 83 (10), 1425-1432, 1994 | 149 | 1994 |
Battling Btk mutants with noncovalent inhibitors that overcome Cys481 and Thr474 mutations AR Johnson, PB Kohli, A Katewa, E Gogol, LD Belmont, R Choy, ... ACS chemical biology 11 (10), 2897-2907, 2016 | 147 | 2016 |
Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors DL Flynn, TR Belliotti, AM Boctor, DT Connor, CR Kostlan, DE Nies, ... Journal of medicinal chemistry 34 (2), 518-525, 1991 | 143 | 1991 |
Structure− activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors PM O'Brien, DF Ortwine, AG Pavlovsky, JA Picard, DR Sliskovic, BD Roth, ... Journal of medicinal chemistry 43 (2), 156-166, 2000 | 136 | 2000 |
4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione Inhibitors of the Checkpoint Kinase Wee1. Structure−Activity Relationships for Chromophore Modification and … BD Palmer, AM Thompson, RJ Booth, EM Dobrusin, AJ Kraker, HH Lee, ... Journal of medicinal chemistry 49 (16), 4896-4911, 2006 | 130 | 2006 |
N6-[2-(3, 5-dimethoxyphenyl)-2-(2-methylphenyl) ethyl] adenosine and its uronamide derivatives. Novel adenosine agonists with both high affinity and high selectivity for the … AJ Bridges, RF Bruns, DF Ortwine, SR Priebe, DL Szotek, BK Trivedi Journal of medicinal chemistry 31 (7), 1282-1285, 1988 | 128 | 1988 |
Synthesis and structure-activity relationships of pyrazolo [4, 3-d] pyrimidin-7-ones as adenosine receptor antagonists HW Hamilton, DF Ortwine, DF Worth, JA Bristol Journal of medicinal chemistry 30 (1), 91-96, 1987 | 109 | 1987 |
Novel series of achiral, low molecular weight, and potent HIV-1 protease inhibitors JVNV Prasad, KS Para, EA Lunney, DF Ortwine, JB Dunbar, D Ferguson, ... Journal of the American Chemical Society 116 (15), 6989-6990, 1994 | 108 | 1994 |
X-ray structure of gelatinase A catalytic domain complexed with a hydroxamate inhibitor V Dhanaraj, MG Williams, QZ Ye, F Molina, LL Johnson, DF Ortwine, ... Croatica chemica acta 72 (2-3), 575-591, 1999 | 104 | 1999 |
Novel series of achiral, low molecular weight, and potent HIV-1 protease inhibitors JVN Vara Prasad, KS Para, EA Lunney, DF Ortwine, JB Dunbar Jr, ... Journal of the American Chemical Society 116 (15), 6989-6990, 1994 | 103 | 1994 |
GDC-9545 (giredestrant): a potent and orally bioavailable selective estrogen receptor antagonist and degrader with an exceptional preclinical profile for ER+ breast cancer J Liang, JR Zbieg, RA Blake, JH Chang, S Daly, AG DiPasquale, ... Journal of Medicinal Chemistry 64 (16), 11841-11856, 2021 | 99 | 2021 |
A rationalization of the acidic pH dependence for stromelysin-1 (matrix metalloproteinase-3) catalysis and inhibition LL Johnson, AG Pavlovsky, AR Johnson, JA Janowicz, CF Man, ... Journal of Biological Chemistry 275 (15), 11026-11033, 2000 | 98 | 2000 |
Quinazolinones and Pyrido[3,4-d]pyrimidin-4-ones as Orally Active and Specific Matrix Metalloproteinase-13 Inhibitors for the Treatment of Osteoarthritis JJ Li, J Nahra, AR Johnson, A Bunker, P O’Brien, WS Yue, DF Ortwine, ... Journal of medicinal chemistry 51 (4), 835-841, 2008 | 94 | 2008 |