CCR2 antagonist 1

CCR2 antagonist 1 is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM.

Signaling Pathways >> GPCR/G Protein >> CCR

Signaling Pathways >> Immunology/Inflammation >> CCR

Research Areas >> Others

CCR2:2.4 nM (Ki)

The combination of SAR and SKR in the hit-to-lead process results in the discovery of a new higheaffinity and longeresidenceetime CCR2 antagonist (CCR2 antagonist 1 (compound 15a), Ki=2.4 nM; RT=714 min)[1].

[1]. Vilums M, et al. When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists. Eur J Med Chem. 2015 Mar 26;93:121-34.

INCB3344 | Cenicriviroc | INCB8761(PF-4136309) | RS504393 | RS-102895 hydrochloride | BX 471 | TAK-779 | Vercirnon | MK-0812 Succinate | AZD 2098 | CCX140 | INCB 3284 | ZK 756326 | CCR2-RA-[R] | BMS-813160