ML 145 is a selective GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM, but not for the related GPR55 orphan receptor. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic target in inflammatory disease.
IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein.
PF-04634817 is an orally administered CCR2 and CCR5 chemokine receptor antagonist, for the treatment of diabetic nephropathies and diabetic macular oedema.
AMD-070 hydrochloride is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.
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).
UNBS5162 is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers; the mean antiproliferative activity IC50 value is 17.9 uM for 9 cancer cell lines; hydrolysis product of UNBS3157.
