Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 4, 2012, Pages 1655-1659

  Cumming, John G ^a   Tucker, Howard ^a   Oldfield, John ^a   Fielding, Colin ^a   Highton, Adrian ^a   Faull, Alan ^a   Wild, Martin ^a   Brown, Dearg ^a   Wells, Stuart ^a   Shaw, John ^a  

^a ASTRAZENECA   (United Kingdom)

Author keywords

CCR5 antagonist; Chemokine receptor; HERG

Indexed keywords

1 (3,3 DIPHENYLPROPYL)PIPERIDINE PHENYLACETAMIDE; 4 [(4 BROMOPHENYL)(ETHOXYIMINO)METHYL] 1' [(2,4 DIMETHYL 3 PYRIDINYL)CARBONYL] 4' METHYL 1,4' BIPIPERIDINE; AZD 5672; CHEMOKINE RECEPTOR CCR5 ANTAGONIST; CYTOCHROME P450; ION CHANNEL; MACROPHAGE INFLAMMATORY PROTEIN 1BETA; MARAVIROC; POTASSIUM CHANNEL HERG; UNCLASSIFIED DRUG;

ARTICLE; CHEMICAL STRUCTURE; CHEMOTAXIS; DRUG ABSORPTION; DRUG ANTAGONISM; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DEVELOPMENT; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SAFETY; DRUG SOLUBILITY; DRUG STABILITY; ENANTIOMER; EX VIVO STUDY; HUMAN; IC 50; IN VITRO STUDY; LIPOPHILICITY; MOLECULAR WEIGHT; NONHUMAN; OXIDATION; PHARMACODYNAMICS; PHARMACOKINETICS; PHASE 2 CLINICAL TRIAL (TOPIC); PHYSICAL CHEMISTRY; PLASMA CLEARANCE; QT PROLONGATION; RAT; RHEUMATOID ARTHRITIS;

EID: 84863398102     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.12.117     Document Type: Article

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