CCR

Vicriviroc Malate is a second generation orally active CCR5 antagonist, which is also a potent inhibitor of HIV-1 entry into target cells, with a mean IC50 =0.46 nM and IC50 =1~10 nM to HIV isolates (n=52).

MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2 on human monocytes and low nM in the chemotaxis assay. It has good PK profiles in preclinical species and demonstrated efficacy in animal models.

INCB8761(PF-4136309) is a potent, selective, and orally bioavailable CCR2 antagonist.

INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.

GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96??0.11.

Teijin compound 1 is a specific CCR 2 antagonist with IC50s of 24 and 180 nM in chemotaxis and binding assay, respectively.

TAK-779 is a novel, potent and selective small-molecule antagonists of CCR5 with the IC50 value of 1.4nM in binding assay.

RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 98 nM and > 100 uM for inhibition of human recombinant CCR2b and CCR1 receptors respectively).

Vicriviroc maleate is a CCR5 antagonist with IC50 of 0.91 nM in clinical development for the treatment of HIV-1.

NSC5844 is a bisquinoline compound with C-C chemokine receptor type 1 (CCR1)-agonistic properties.

AZ084 is a potent, selective, allosteric and oral active CCR8 antagonist, with a Ki of 0.9 nM. Has potential to treat asthma.

TAK-220 is a selective and orally bioavailable CCR5 antagonist.

RS102895 hydrochloride is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.

BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.