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Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists.
Carpenter J, Wang Y, Wu G, Feng J, Ye XY, Morales CL, Broekema M, Rossi KA, Miller KJ, Murphy BJ, Wu G, Malmstrom SE, Azzara AV, Sher PM, Fevig JM, Alt A, Bertekap RL Jr, Cullen MJ, Harper TM, Foster K, Luk E, Xiang Q, Grubb MF, Robl JA, Wacker DA. Carpenter J, et al. Among authors: fevig jm. J Med Chem. 2017 Jul 27;60(14):6166-6190. doi: 10.1021/acs.jmedchem.7b00385. Epub 2017 Jul 7. J Med Chem. 2017. PMID: 28635286
Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa.
Li YL, Fevig JM, Cacciola J, Buriak J Jr, Rossi KA, Jona J, Knabb RM, Luettgen JM, Wong PC, Bai SA, Wexler RR, Lam PY. Li YL, et al. Among authors: fevig jm. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5176-82. doi: 10.1016/j.bmcl.2006.07.002. Epub 2006 Jul 25. Bioorg Med Chem Lett. 2006. PMID: 16870435
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.
Lam PY, Clark CG, Li R, Pinto DJ, Orwat MJ, Galemmo RA, Fevig JM, Teleha CA, Alexander RS, Smallwood AM, Rossi KA, Wright MR, Bai SA, He K, Luettgen JM, Wong PC, Knabb RM, Wexler RR. Lam PY, et al. Among authors: fevig jm. J Med Chem. 2003 Oct 9;46(21):4405-18. doi: 10.1021/jm020578e. J Med Chem. 2003. PMID: 14521405
Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).
Devasthale P, Wang Y, Wang W, Fevig J, Feng J, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Moulin F, Li YX, Zahler R, Kirby MS, Hamann LG. Devasthale P, et al. J Med Chem. 2013 Sep 26;56(18):7343-57. doi: 10.1021/jm4008906. Epub 2013 Sep 9. J Med Chem. 2013. PMID: 23964740
Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Wang S, Fevig JM, Quan ML, Amparo E, Cacciola J, Rossi KA, Alexander RS, Smallwood AM, Luettgen JM, Liang L, Aungst BJ, Wright MR, Knabb RM, Wong PC, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: fevig jm. J Med Chem. 2001 Feb 15;44(4):566-78. doi: 10.1021/jm000409z. J Med Chem. 2001. PMID: 11170646
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