ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.

BL5923 (BL-5923) is a potent, highly specific, orally available inhibitor of CCR1 with IC50 of 20.4 and 22.8 nM for human and mouse CCR1, resepctively.

AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis.

SX-682 (SX682) is a potent, allosteric, orally bioavailable inhibitor of CXCR1 and CXCR2.SX-682 enhances tumor infiltration, activation, and the therapeutic efficacy of adoptively transferred NK cells.SX-682 significantly inhibits trafficking of PMN-MDSCs without altering CXCR2 ligand expression.SX-682 enhances T cell-based immunotherapeutic efficacy.

IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.

YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM.

YM-355179 is a potent selective, and orally available antagonist of CC chemokine receptor 3 (CCR3) with binding IC50 of 7.6 nM (CCL5).

YM-344484 (YM344484) is a potent, selective dual antagonist of chemokine CCR3 receptor and histamine H1 receptor, potently inhibits both the CCL11-induced Ca2+ influx in human CCR3-expressing cells (Kb=1.8 nM) and histamine-induced Ca2+ influx in histamin

VUF15485 is a small-molecule agonist of the atypical chemokine receptor ACKR3 with binding pIC50 of 8.3, and pEC50 of 7.6 in BRET-based β-arrestin2 recruitment assay.

UCUF-965 (UCUF965) is a potent partial agonist and positive allosteric modulator of CXCR4 with EC50 of 0.02 uM, Emax=44% for CXCR4/CXCL12 signaling for β-arrestin-2 recruitment.

UCB35625 is a potent, selective inhibitor of CCR1 and CCR3, inhibits MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants with IC50 of 9.57 and 93.8 nM respectively.

SCH-479833 is a potent, specific and orally active CXCR1 and CXCR2 antagonist with Ki of 0.17 and 7 nM, respectively.

RAP-103 is an orally active, stabilized pentapeptide analog of DAPTA (D-ala-peptide T-amide), and multi-chemokine receptor antagonist.

NUCC-390 dihydrochloride (NUCC390) is a small molecule agonist of CXCR4, recapitulates the activity of CXCL12α.

LN6023 (LN-6023) a potent, selective and first-in-class inhibitor of the atypical chemokine receptor 3 (ACKR3, CXCR7) with β-arrestin EC50 of 3.5 uM.

Ki19003 (Ki 19003) is a potent, specific CCR3 antagonist, inhibits the CCL11-induced migration of CCR3-expressing L1.2 cells with IC50 of 20 nM.

GW782415W (GW782415) is a potent, specific CCR3 antagonist, inhibits chemotaxis of human and murine eosinophils pKi of 8.08 and 7.85, respectively.

DF2755A is a selective, allosteric, orally acting inhibitor of CXCR1/2 (Kd=2.24/0.94 nM), inhibits human PMN (hPMN) migration induced by CXCL8 and CXCL1 with IC50 of 4.2 and 2.1 nM, respectively.

A potent and specific CCR6 antagonist.

BPRCX807 (BPRCX-807) is a highly selective and potent CXCR4 antagonist with binding IC50 of 40.4 nM and EC50 of 48.1 nM for cell-mobility activity in the chemotaxis assays, inhibits CXCL12-mediated cell signaling pathway.

BPRCX714 (BPRCX 714) is a highly selective and potent CXCR4 antagonist with binding IC50 of 34.2 nM, effectively inhibits CXCL12-induced movement of CCRF-CEM cells with EC50 of 13.7 nM.

AZD3778 (AZD-3778) is a dual CCR3 and H1-receptor antagonistwith Ki of 54 nM for guinea-pig H1-receptor, inhibits binding of CR3 radioligand 125I-eotaxin to human CCR3-receptor expressed on CHO-cells with IC50 of 8 nM.

AZ12436092 (AZ 12436092) is a potent, selective CCR3 antagonist with binding pKi value of 9.2.

alpha-NETA (α-NETA) is a small molecule antagonist of chemerin receptor chemokine-like receptor 1 (CMKLR1), inhibits chemerin-stimulated β-arrestin2 association with CMKLR1 with IC50 of 4.9 uM.

ACT-672125 (ACT672125) is a potent, selective CXCR3 antagonist with IC50 of 239 nM in human blood.

ML 339 is a potent and selective hCXCR6 antagonist (IC50 = 140 nM), 100-fold less active at the murine CXCR6 receptor (IC50 = 18 uM); ML 339 exhibits selectivity over CXCR5, CXCR4, CCR6 and APJ receptors.

CXCR6 inhibitor 81 is a potent (EC50=40 nM) and selective orally bioavailable small molecule antagonist of human CXCR6 receptor; Compound 81 displays >10-fold improvement in potency in both the β-arrestin and cAMP assays (IC50 =40 and 540 nM, respectively) compared to ML339. CXCR6 inhibitor 81 inhibits migration of SK-HEP-1 hepatoma cells in a dose dependent manner. Compound 81 has promising oral DMPK data, significantly decreases tumor growth in a 30-day mouse xenograft model of HCC.

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

PF-07054894 is a potent CCR6 antagonist. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease.

FLX475 is a potent CCR4 antagonist that blocks regulatory T cells that interfere with effective antitumor immune responses and has antitumor activity.