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Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.
Swanson DM, Savall BM, Coe KJ, Schoetens F, Koudriakova T, Skaptason J, Wall J, Rech J, Deng X, De Angelis M, Everson A, Lord B, Wang Q, Ao H, Scott B, Sepassi K, Lovenberg TW, Carruthers NI, Bhattacharya A, Letavic MA. Swanson DM, et al. Among authors: skaptason j. J Med Chem. 2016 Sep 22;59(18):8535-48. doi: 10.1021/acs.jmedchem.6b00989. Epub 2016 Sep 8. J Med Chem. 2016. PMID: 27548392
Characterization of JNJ-2482272 [4-(4-Methyl-2-(4-(Trifluoromethyl)Phenyl)Thiazole-5-yl) Pyrimidine-2-Amine] As a Strong Aryl Hydrocarbon Receptor Activator in Rat and Human.
Coe KJ, Feinstein M, Higgins JW, Leung P, Scott BP, Skaptason J, Tam Y, Volak LP, Kinong J, Bittner A, McAllister H, Lim NM, Hack M, Koudriakova T. Coe KJ, et al. Among authors: skaptason j. Drug Metab Dispos. 2022 Aug;50(8):1064-1076. doi: 10.1124/dmd.121.000825. Epub 2022 Jun 9. Drug Metab Dispos. 2022. PMID: 35680134
Prolyl hydroxylase inhibition corrects functional iron deficiency and inflammation-induced anaemia in rats.
Barrett TD, Palomino HL, Brondstetter TI, Kanelakis KC, Wu X, Yan W, Merton KP, Schoetens F, Ma JY, Skaptason J, Gao J, Tran DT, Venkatesan H, Rosen MD, Shankley NP, Rabinowitz MH. Barrett TD, et al. Among authors: skaptason j. Br J Pharmacol. 2015 Aug;172(16):4078-88. doi: 10.1111/bph.13188. Epub 2015 Jun 26. Br J Pharmacol. 2015. PMID: 25988595 Free PMC article.