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The translational efficacy of a nonsteroidal progesterone receptor antagonist, 4-[3-cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy,-2,6-dimethylbenzonitrile (PF-02413873), on endometrial growth in macaque and human.
Howe DC, Mount NM, Bess K, Brown A, Bungay P, Gibson KR, Hawcock T, Richard J, Jones G, Walley R, McLeod A, Apfeldorfer C, Ramsey S, Tweedy S, Pullen N. Howe DC, et al. Among authors: gibson kr. J Pharmacol Exp Ther. 2011 Nov;339(2):642-53. doi: 10.1124/jpet.111.183848. Epub 2011 Aug 17. J Pharmacol Exp Ther. 2011. PMID: 21849626 Clinical Trial.
The Discovery of a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor (PF-06273340) for the Treatment of Pain.
Skerratt SE, Andrews M, Bagal SK, Bilsland J, Brown D, Bungay PJ, Cole S, Gibson KR, Jones R, Morao I, Nedderman A, Omoto K, Robinson C, Ryckmans T, Skinner K, Stupple P, Waldron G. Skerratt SE, et al. Among authors: gibson kr. J Med Chem. 2016 Nov 23;59(22):10084-10099. doi: 10.1021/acs.jmedchem.6b00850. Epub 2016 Nov 4. J Med Chem. 2016. PMID: 27766865
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.
Bagal SK, Bungay PJ, Denton SM, Gibson KR, Glossop MS, Hay TL, Kemp MI, Lane CA, Lewis ML, Maw GN, Million WA, Payne CE, Poinsard C, Rawson DJ, Stammen BL, Stevens EB, Thompson LR. Bagal SK, et al. Among authors: gibson kr. ACS Med Chem Lett. 2015 Apr 29;6(6):650-4. doi: 10.1021/acsmedchemlett.5b00059. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101568 Free PMC article.
Discovery of a First-in-Class Potent Small Molecule Antagonist against the Adrenomedullin-2 Receptor.
Avgoustou P, Jailani ABA, Zirimwabagabo JO, Tozer MJ, Gibson KR, Glossop PA, Mills JEJ, Porter RA, Blaney P, Bungay PJ, Wang N, Shaw AP, Bigos KJA, Holmes JL, Warrington JI, Skerry TM, Harrity JPA, Richards GO. Avgoustou P, et al. Among authors: gibson kr. ACS Pharmacol Transl Sci. 2020 Jun 25;3(4):706-719. doi: 10.1021/acsptsci.0c00032. eCollection 2020 Aug 14. ACS Pharmacol Transl Sci. 2020. PMID: 32832872 Free PMC article.
Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865).
Owen RM, Blakemore D, Cao L, Flanagan N, Fish R, Gibson KR, Gurrell R, Huh CW, Kammonen J, Mortimer-Cassen E, Nickolls SA, Omoto K, Owen D, Pike A, Pryde DC, Reynolds DS, Roeloffs R, Rose C, Stead C, Takeuchi M, Warmus JS, Watson C. Owen RM, et al. Among authors: gibson kr. J Med Chem. 2019 Jun 27;62(12):5773-5796. doi: 10.1021/acs.jmedchem.9b00322. Epub 2019 Apr 26. J Med Chem. 2019. PMID: 30964988
Novel Amino-pyrazole Ureas with Potent In Vitro and In Vivo Antileishmanial Activity.
Mowbray CE, Braillard S, Speed W, Glossop PA, Whitlock GA, Gibson KR, Mills JE, Brown AD, Gardner JM, Cao Y, Hua W, Morgans GL, Feijens PB, Matheeussen A, Maes LJ. Mowbray CE, et al. Among authors: gibson kr. J Med Chem. 2015 Dec 24;58(24):9615-24. doi: 10.1021/acs.jmedchem.5b01456. Epub 2015 Dec 4. J Med Chem. 2015. PMID: 26571076 Free article.
Discovery of a First-In-Class Small Molecule Antagonist against the Adrenomedullin-2 Receptor: Structure-Activity Relationships and Optimization.
Zirimwabagabo JO, Jailani ABA, Avgoustou P, Tozer MJ, Gibson KR, Glossop PA, Mills JEJ, Porter RA, Blaney P, Wang N, Skerry TM, Richards GO, Harrity JPA. Zirimwabagabo JO, et al. Among authors: gibson kr. J Med Chem. 2021 Mar 25;64(6):3299-3319. doi: 10.1021/acs.jmedchem.0c02191. Epub 2021 Mar 5. J Med Chem. 2021. PMID: 33666424 Free PMC article.
46 results