Ontology highlight
ABSTRACT:
SUBMITTER: Yang MG
PROVIDER: S-EPMC6421546 | biostudies-literature | 2019 Mar
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20190116 3
We encountered a dilemma in the course of studying a series of antagonists of the G-protein coupled receptor CC chemokine receptor-2 (CCR2): compounds with polar C3 side chains exhibited good ion channel selectivity but poor oral bioavailability, whereas compounds with lipophilic C3 side chains exhibited good oral bioavailability in preclinical species but poor ion channel selectivity. Attempts to solve this through the direct modulation of physicochemical properties failed. However, the install ...[more]