Vercirnon is an orally bioavailable, selective, and potent antagonist of CCR9, with an IC50 of 10 nM, used in the research of inflammatory bowel diseases.
Plozalizumab (MLN-1202) is a specific humanized anti-CCR2 antibody. Plozalizumab can be used for malignant melanoma research[1].
PF-232798 is an orally active CCR5 antagonist with anti-HIV effects[1].
CCR2 antagonist 5 is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). CCR2 antagonist 5 displays a Ki of 9.6 µM for mCCR2 binding. CCR2 antagonist 5 can be used in the research of inflammatory disease[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].
Bertilimumab (CAT 213; iCo-008) is a human monoclonal antibody targeting eotaxin-1 (CCL11). Bertilimumab has the potential for allergic disorders research[1].
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca2+ flux [1][2][3].
CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity[1].
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).
Ophiobolin C inhibits CCR5 binding to the envelop protein gp120 and CD4, which is responsible for mediating the entry of HIV-1 into cells[1]. Ophiobolin C is also cytotoxic to chronic lymphocytic leukemia cells[2].
MLN 3897 is a potent, specific and orally active antagonist of CCR1 with IC50 of 0.8 nM in competition binding assays, 500-fold selectivity over CCR5; inhibits osteoclastogenesis and OC activity by impairing multinucleation and by down-regulation of c-fos signaling, inhibits osteoclastogenesis and OC activity by impairing multinucleation and by down-regulation of c-Fos signaling; demonstrates potential for the treatment of multiple sclerosis and rheumatoid arthritis. Multiple Sclerosis Phase 1 Discontinued
Cosalane (NSC 658586) is a potent inhibitor of HIV replication. Cosalane has an intrinsic ability to block human and murine CCR7 function in vitro in response to both of its natural ligands, CCL19 and CCL21, with the IC50 of 0.207/2.66 μM in human for CCL19/CCL21 and 0.193/1.98 μM in murine, respectively[1][2].
SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC50 of 4.5 nM[1].
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].
Met-RANTES (human) is a partial antagonist of CCR5. Met-RANTES (human) reduces the infiltration of blood monocytes into the liver[1].
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively[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].
AZ084 is a potent, selective, allosteric and oral active CCR8 antagonist, with a Ki of 0.9 nM. Has potential to treat asthma[1].
ZK756326 is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.
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.
BAY-3153 is a selective CCR1 (C-C motif chemokine receptor 1) antagonist (human IC50=3 nM; rat IC50=11 nM; mice IC50=81 nM)[1].
BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM)[1][2].
MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research[1].
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
ZK756326 dihydrochloride is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.
CCX140 is a potent CCR2 antagonist.
AZD 1678 is a potent, selective orally bioavailable CCR4 receptor antagonist with pIC50 of 8.6 for hCCR4, pIC50 of 9.0 for rCCR4; shows no significant activity against a panel of chemokine receptors (CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, CCR8; inactive at 10 uM); inhibits Th2 cell CCL22 driven chemotaxis in 0.3% HSA with pIC50 of 6.8. Asthma Phase 1 Clinical
CCR5 antagonist 2 (Compound 25) is a CCR5 antagonist with an IC50 of 8.34 nM. CCR5 antagonist 2 shows broad-spectrum anti-HIV-1 activities[1].
BMS-813160 is the first dual CCR2/CCR5 antagonist to enter clinical development for cardiovascular.
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].