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Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
Palucki BL, Park MK, Nargund RP, Ye Z, Sebhat IK, Pollard PG, Kalyani RN, Tang R, Macneil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, McGowan E, Martin WJ, Metzger JM, Shepherd CA, Strack AM, Macintyre DE, Van der Ploeg LH, Patchett AA. Palucki BL, et al. Among authors: shepherd ca. Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5. doi: 10.1016/j.bmcl.2004.10.020. Bioorg Med Chem Lett. 2005. PMID: 15582434
Soluble guanylate cyclase stimulators for the treatment of hypertension: Discovery of MK-2947.
Brockunier L, Stelmach J, Guo J, Spencer T, Rosauer K, Bansal A, Cai SJ, Chen N, Cummings J, Huang L, Johnson T, Levesque S, Luo L, Maloney K, Metzger J, Mortko C, Ortega K, Pai LY, Pereira A, Salituro G, Shang J, Shepherd C, Sherrie Xu S, Yang Q, Cui J, Roy S, Parmee E, Raghavan S. Brockunier L, et al. Bioorg Med Chem Lett. 2020 Nov 1;30(21):127574. doi: 10.1016/j.bmcl.2020.127574. Epub 2020 Sep 24. Bioorg Med Chem Lett. 2020. PMID: 32980512
VPA-985, a nonpeptide orally active and selective vasopressin V2 receptor antagonist.
Chan PS, Coupet J, Park HC, Lai F, Hartupee D, Cervoni P, Dusza JP, Albright JD, Ru X, Mazandarani H, Tanikella T, Shepherd C, Ochalski L, Bailey T, Lock TY, Ning X, Taylor JR, Spinelli W. Chan PS, et al. Adv Exp Med Biol. 1998;449:439-43. doi: 10.1007/978-1-4615-4871-3_55. Adv Exp Med Biol. 1998. PMID: 10026835 Review. No abstract available.
Fragment screening by SPR and advanced application to GPCRs.
Shepherd CA, Hopkins AL, Navratilova I. Shepherd CA, et al. Prog Biophys Mol Biol. 2014 Nov-Dec;116(2-3):113-23. doi: 10.1016/j.pbiomolbio.2014.09.008. Epub 2014 Oct 6. Prog Biophys Mol Biol. 2014. PMID: 25301577 Free article. Review.
21 results