Structure-kinetic relationships - An overlooked parameter in hit-to-lead optimization: A case of cyclopentylamines as chemokine receptor 2 antagonists

Journal of Medicinal Chemistry

Volumn 56, Issue 19, 2013, Pages 7706-7714

  Vilums, Maris ^a   Zweemer, Annelien J M ^a   Yu, Zhiyi ^a   De Vries, Henk ^a   Hillger, Julia M ^a   Wapenaar, Hannah ^a   Bollen, Ilse A E ^a   Barmare, Farhana ^b   Gross, Raymond ^b   Clemens, Jeremy ^b   Krenitsky, Paul ^b   Brussee, Johannes ^a   Stamos, Dean ^b   Saunders, John ^b   Heitman, Laura H ^a   Ijzerman, Adriaan P ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

^b VERTEX PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CHEMOKINE RECEPTOR CCR2; CHEMOKINE RECEPTOR CCR2 ANTAGONIST; CYCLOPENTYLAMINE DERIVATIVE; N [2 [[1 [4 (1,3 BENZODIOXOL 5 YL) 4 HYDROXYCYCLOHEXYL] 4 ETHOXY 3 PYRROLIDINYL]AMINO] 2 OXOETHYL] 3 (TRIFLUOROMETHYL)BENZAMIDE; PENTYLAMINE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; BINDING KINETICS; DRUG COMPETITION; DRUG DETERMINATION; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN TISSUE; OSTEOSARCOMA; PROCESS OPTIMIZATION;

BINDING, COMPETITIVE; CELL LINE, TUMOR; CYCLOPENTANES; HUMANS; INDANS; INDENES; KINETICS; LIGANDS; RECEPTORS, CCR2; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TETRAHYDRONAPHTHALENES;

EID: 84885615252     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm4011737     Document Type: Article

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