(1S)-CCR2 antagonist 1

Names

[ Name ]:
(1S)-CCR2 antagonist 1

Biological Activity

[Description]:

(1S)-CCR2 antagonist 1 is a left-handed chiral body of CCR2 antagonist 1 (HY-112792). CCR2 antagonist 1 is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> CCR

Research Areas >> Endocrinology

Signaling Pathways >> Immunology/Inflammation >> CCR

[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₈H₃₂BrF₃N₂O

[ Molecular Weight ]:
549.47

Related Compounds

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