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Page 1
Development of small molecule inhibitors of natural killer group 2D receptor (NKG2D).
Wang J, Nakafuku KM, Ziff J, Gelin CF, Gholami H, Thompson AA, Karpowich NK, Limon L, Coate HR, Damm-Ganamet KL, Shih AY, Grant JC, Côte M, Mak PA, Pascual HA, Rives ML, Edwards JP, Venable JD, Venkatesan H, Shi Z, Allen SJ, Sharma S, Kung PP, Shireman BT. Wang J, et al. Among authors: coate hr. Bioorg Med Chem Lett. 2023 Nov 15;96:129492. doi: 10.1016/j.bmcl.2023.129492. Epub 2023 Sep 29. Bioorg Med Chem Lett. 2023. PMID: 37778428
Discovery of a Series of Substituted 1H-((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators.
Gelin CF, Stenne B, Coate H, Hiscox A, Soyode-Johnson A, Wall JL, Lord B, Schoellerman J, Coe KJ, Wang K, Alcázar J, Chrovian CC, Dvorak CA, Carruthers NI, Koudriakova T, Balana B, Letavic MA. Gelin CF, et al. J Med Chem. 2023 Feb 23;66(4):2877-2892. doi: 10.1021/acs.jmedchem.2c01916. Epub 2023 Feb 9. J Med Chem. 2023. PMID: 36757100
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.
Préville C, Bonaventure P, Koudriakova T, Lord B, Nepomuceno D, Rizzolio M, Mani N, Coe KJ, Ndifor A, Dugovic C, Dvorak CA, Coate H, Pippel DJ, Fitzgerald A, Allison B, Lovenberg TW, Carruthers NI, Shireman BT. Préville C, et al. ACS Med Chem Lett. 2020 Apr 27;11(10):2002-2009. doi: 10.1021/acsmedchemlett.0c00085. eCollection 2020 Oct 8. ACS Med Chem Lett. 2020. PMID: 33062185 Free PMC article.
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
Stearns BA, Baccei C, Bain G, Broadhead A, Clark RC, Coate H, Evans JF, Fagan P, Hutchinson JH, King C, Lee C, Lorrain DS, Prasit P, Prodanovich P, Santini A, Scott JM, Stock NS, Truong YP. Stearns BA, et al. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51. doi: 10.1016/j.bmcl.2009.06.085. Epub 2009 Jun 25. Bioorg Med Chem Lett. 2009. PMID: 19608418
Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.
Crew AP, Bhagwat SV, Dong H, Bittner MA, Chan A, Chen X, Coate H, Cooke A, Gokhale PC, Honda A, Jin M, Kahler J, Mantis C, Mulvihill MJ, Tavares-Greco PA, Volk B, Wang J, Werner DS, Arnold LD, Pachter JA, Wild R, Gibson NW. Crew AP, et al. Bioorg Med Chem Lett. 2011 Apr 1;21(7):2092-7. doi: 10.1016/j.bmcl.2011.01.139. Epub 2011 Feb 3. Bioorg Med Chem Lett. 2011. PMID: 21353551
GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.
Liu C, Bonaventure P, Lee G, Nepomuceno D, Kuei C, Wu J, Li Q, Joseph V, Sutton SW, Eckert W, Yao X, Yieh L, Dvorak C, Carruthers N, Coate H, Yun S, Dugovic C, Harrington A, Lovenberg TW. Liu C, et al. Mol Pharmacol. 2015 Nov;88(5):911-25. doi: 10.1124/mol.115.100412. Epub 2015 Sep 8. Mol Pharmacol. 2015. PMID: 26349500
Pharmacology of JNJ-28583113: A novel TRPM2 antagonist.
Fourgeaud L, Dvorak C, Faouzi M, Starkus J, Sahdeo S, Wang Q, Lord B, Coate H, Taylor N, He Y, Qin N, Wickenden A, Carruthers N, Lovenberg TW, Penner R, Bhattacharya A. Fourgeaud L, et al. Eur J Pharmacol. 2019 Jun 15;853:299-307. doi: 10.1016/j.ejphar.2019.03.043. Epub 2019 Apr 6. Eur J Pharmacol. 2019. PMID: 30965058
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.
Mulvihill MJ, Ji QS, Coate HR, Cooke A, Dong H, Feng L, Foreman K, Rosenfeld-Franklin M, Honda A, Mak G, Mulvihill KM, Nigro AI, O'Connor M, Pirrit C, Steinig AG, Siu K, Stolz KM, Sun Y, Tavares PA, Yao Y, Gibson NW. Mulvihill MJ, et al. Among authors: coate hr. Bioorg Med Chem. 2008 Feb 1;16(3):1359-75. doi: 10.1016/j.bmc.2007.10.061. Epub 2007 Oct 23. Bioorg Med Chem. 2008. PMID: 17983756
13 results