Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 5, 2011, Pages 1442-1446

  Zheng, Changsheng ^a   Cao, Ganfeng ^a   Xia, Michael ^a   Feng, Hao ^a   Glenn, Joseph ^a   Anand, Rajan ^a   Zhang, Ke ^a   Huang, Taisheng ^a   Wang, Anlai ^a   Kong, Ling ^a   Li, Mei ^a   Galya, Laurine ^a   Hughes, Robert O ^b   Devraj, Rajesh ^b   Morton, Phillip A ^b   Rogier, D Joseph ^b   Covington, Maryanne ^a   Baribaud, Fred ^a   Shin, Niu ^a   Scherle, Peggy ^a   Diamond, Sharon ^a   Yeleswaram, Swamy ^a   Vaddi, Kris ^a   Newton, Robert ^a   Hollis, Greg ^a   Friedman, Steven ^a   Metcalf, Brian ^a   Xue, Chu Biao ^a   more..

^a Experimental Station   (United States)

^b PFIZER INC   (United States)

Author keywords

Antagonist; CCR2; CCR5; Chemokine

Indexed keywords

CHEMOKINE RECEPTOR CCR2 ANTAGONIST; CHEMOKINE RECEPTOR CCR5 ANTAGONIST; INCB 10820; N 3 ISOPROPYL 3[[4 (4 (TRIFLUOROMETHYL)PYRIDIN 2 YL]PIPERAZIN 1 YL)CARBONYL]CYCLOPENTYL] 3 METHOXYTETRAHYDRO 2H PYRAN 4 AMINE; PF 4178903; UNCLASSIFIED DRUG;

ARTICLE; DRUG BIOAVAILABILITY; DRUG SCREENING;

BIOLOGICAL AVAILABILITY; CACO-2 CELLS; DRUG DISCOVERY; HUMANS; INHIBITORY CONCENTRATION 50; MOLECULAR STRUCTURE; PIPERAZINES; PYRANS; RECEPTORS, CCR2; RECEPTORS, CCR5;

EID: 79951725766     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.01.015     Document Type: Article

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29. 80. The human trough concentration was obtained from the projected human PK by an allometric scaling of the rat PK.