ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca2+ concentrations[1][2].
MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2 on human monocytes.
YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively[1]. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo[3].
Mogamulizumab (KW-0761) is a defucosylated humanized recombinant anti-CCR4 monoclonal antibody (MAb). Mogamulizumab can eliminate tumor cells by antibody-dependent cellular cytotoxicity (ADCC). Mogamulizumab can be used in the research of cancers, adult T-cell leukemia/lymphoma (ATLL), cutaneous T-cell lymphoma (CTCL)[1][2][3].
CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM[1].
AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor, used for asthma research.
7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid isolated from Glycyrrhiza uralensis, the eotaxin/CCL11 inhibitor, has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production[1]. 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2.7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM[1].
C-021 is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor with an IC50 of 18 nM[1].
JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2[1].
PF-0463481, an oral CCR2/5 dual antagonist, with a favorable ocular safety profile versus intravitreal therapies[1]. PF-0463481 is safe and well-tolerated and being developed for the treatment of diabetic nephropathy[2].
RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).
CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM[1].
CCR1 antagonist 8 (compound 19n), a third azaindazole series compound, is a CCR1 antagonist clinical candidate, with an IC50 of 1.8 nM in Ca2+ flux assay[1].
R243 is a potent, small molecule CCR8 antagonist that inhibits CCR8 signaling and chemotaxis, inhibits CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation at 0.2 uM; attenuated secretion of TNF-α, IL-6, and most strikingly IL-10 from WT PMφ (peritoneal macrophages), but not BMMφ (bone marrow-derived macrophages); shows suppressed c-JNK activity and NF-κB signaling after LPS treatment, suppresses LPS-induced cytokine secretion; attenuates peritoneal adhesions in vivo in CCR8-/- mice, also prevents hapten-induced colitis.
MLN3126 (MLN 3126, MLN-3126) is a potent, selective, orally available CCR9 antagonist with IC50 of 6.3 nM (CCL25-induced calcium mobilization); shows no significant antagonistic activity for other 12 chemokine receptors (CCR1, -2b, -4, -6, -7, -8, -10,CX3CR1, CXCR1, -2, -3 and -4) at 10 uM; dose dependently inhibits CCL25-induced chemotaxis of mouse thymocytes (IC90=1.8 uM); ameliorates inflammation in a T cell mediated mouse colitis model. Other Indication Phase 1 Discontinued
CCR6 antagonist 1 is a CCR6 antagonist that inhibits the CCL20/CCR6 axis. CCR6 antagonist 1 can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs)[1].
J-113863 is a potentand selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 has no active against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect[1][2][3].
RS102895 hydrochloride is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.
PF-04634817 is a potent, orally bioavailble CCR2 and CCR5 chemokine receptor antagonist, for the treatment of diabetic nephropathies and diabetic macular oedema. Other Indication Phase 2 Discontinued
CCR1 inhibitor 19e is a novel potent, selective CCR1 antagonist with IC50 of 6.8 nM, inhibits CCR1chemotaxis in THP-1 cells with IC50 of 28 nM.
Cenicriviroc is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.