| DC70219 |
AstraZeneca CCR4 antagonist |
AstraZeneca CCR4 antagonist is a potent, selective CCR4 antagonist, inhibits CCR4 ligand macrophage-derived chemokine (MDC/CCL22) in CCR4+CD4+ T cells. |
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| DC70261 |
BMS-570520 |
BMS-570520 is a potent, selective CCR3 antagonist with IC50 of 1.9 nM, inhibits eotaxin-induced chemotaxis with IC50 of 0.068 nM.BMS-570520 displays reduced inhibition on CYP2D6 (IC50=1300 nM) compared with DPC168 (IC50=30 nM), also possesses >100-fold selectivity over 5-HT2a, DAT and NET.BMS-570520 showed good activity in murine models of CCR3 antagonism and greater in vitro potency and in vivo in the mouse intranasal eotaxin challenge mode. |
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| DC70278 |
BX471 hydrochloride |
BX471 is a potent, selective, orally available CCR1 antagonist with Ki of 1 nM for hCCR1, displays 100 times less affinity for rat CCR1; shows 10,000-fold selectivity for CCR1 compared with 28 GPCRs (); displays CCR1 ligands MIP-1α, RANTES, and MCP-3 with high affinity (Ki=1-5.5 nM), inhibits a number of CCR1-mediated effects including Ca(2+) mobilization, increase in extracellular acidification rate, CD11b expression; effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis. |
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| DC70290 |
CCR2 Covalent-IN-14 |
CCR2 covalent-IN-14 is a covalent, negative allosteric modulator (NAM) of CCR2, binds to intracellularly pocket of CCR2 with Ki of 4 nM.CCR2 covalent-IN-14 is more potent than non-covalent analogue and wash-resistant in functional assays (IC50=33 nM in GTPγS binding assay on U2OS-CCR2 cell membranes, IC50=4 nM in β-arrestin recruitment assays).CCR2 covalent-IN-14 displays little to no inhibitory potency on CCR1 and CCR5.The affinity of CCR2 covalent-IN-14 for both the C70S and C75S CCR2 mutants is significantly decreased compared to WT CCR2. |
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| DC70291 |
CCR2 inhibitor SD-24 |
CCR2 inhibitor SD-24 is a potent selective CCR2 antagonist with pKi of 8.5. |
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| DC70292 |
CCR4-IN-38
Featured
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CCR4-IN-38 (CCR4-351) is a potent, selective, orally bioavailable CCR4 antagonist with IC50 of 50 nM (Chemotaxis inhibition).CCR4-IN-38 inhibits the recruitment of Treg into the tumor microenvironment (TME).CCR4-IN-38 elicits antitumor responses as a single agent or in combination with an immune checkpoint blockade. |
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| DC70293 |
CCR7 inhibitor Cmp1205 |
CCR7 inhibitor Cmp1205 is an allosteric ligand and antagonist for human CC chemokine receptor 7 (CCR7) with Kd of 3 nM, suppresses arrestin binding in response to activation by CCL19 with IC50 of 7.3 uM.Cmp1205 binds to a pocket at the intracellular part of CCR7 between the ends of TM1, TM2, TM3, and TM6 and the loop between TM7 and H8.Cmp1205 allosterically inhibits binding of the native chemokine CCL19 ligand in a membrane-based competition binding experiment with IC50 of 35 nM. |
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| DC70295 |
CCX-6239 |
CCX-6239 is a novel potent, orally available CCR4 inhibitor with potential utility in the treatment of allergic airways disease. |
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| DC70333 |
CXCR6 inhibitor 81
Featured
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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. |
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| DC70334 |
CXCR7 modulator 20 |
CXCR7 modulator 20 is a small molecule modulator of the atypical chemokine receptor CXCR7 with Ki of 52 nM. |
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| DC70366 |
DPC168 |
DPC168 (DPC-168) is a highly potent, selective CC chemokine receptor-3 (CCR3) antagonist with IC50 of 2.0 nM, inhibits eotaxin-induced chemotaxis with IC50 of 0.034 nM.DPC168 demonstrates potency for mouse CCR3 (chemotaxis IC50=41 nM) and oral bioavailability in mice (20% F).DPC168 reduced eosinophil recruitment into the lungs in a dose-dependent manner in these animal models. |
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| DC70384 |
EMU-116 |
EMU-116 (EMU-000116) is a potent, selective CXCR4 antagonist with IC50 29.6 nM in Ca2+ flux assay. |
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| DC70415 |
FLX-475 |
FLX-475 is a novel CCR4 antagonist for the treatment of cancer. |
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| DC70454 |
GSK-2239633 |
GSK-2239633 is a potent, selective, allosteric CCR4 antagonist with pIC50 of 7.96; also inhibits TARC-induced increases in the F-actin content of isolated human CD4+ CCR4+ T-cells with pA2 of 7.1. |
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| DC70472 |
GSK812397 |
GSK812397 is a potent, selective, noncompetitive, orally available antagonist of CXCR4 receptor, inhibits entry of X4-tropic strains of HIV-1 with IC50 of 4.60 nM and 1.50 nM in PBMCs and HOS assays, respectively; does not block CCR5-mediated viral entry in the R5 viral HOS assay (IC50>25 uM); produces a concentration-dependent decrease in both an SDF-1-mediated chemotaxis and intracellular calcium release (IC50=0.34 nM and 2.41 nM, respectively) in cell-based functional assays; demonstrates antiviral activity against a broad range of X4-utilizing strains of HIV-1. |
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| DC70482 |
HF50731 |
HF50731 (HF-50731) is a novel potent, selective CXCR4 antagonist with Ki of 19.8 nM in the CXCR4 competitive binding assay.HF50731 significantly inhibited SDF-1α-induced calcium mobilization (IC50=621 nM) and cell migration, and blocked HIV-1 infection via antagonizing CXCR4 coreceptor function (IC50=1.5 uM).The structure-activity relationship analysis demonstrated that HF50731 could primarily occupy the minor subpocket of CXCR4 and partially bind in the major subpocket by interacting with residues W94, D97, D171, and E288. |
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| DC70517 |
IS811 |
IS811 is a potent, selective CCR3 antagonist with IC50 of 2.0 nM, potently inhibits chemotaxis with EC50 of 19 nM.IS811 displays >100-fold selectivity over 5-HT2a, DAT and NET.IS811 (0-20 mg/kg) dose-dependently inhibited eotaxin-induced eosinophil influx to the lung in vivo. |
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| DC70559 |
Lazucirnon |
Lazucirnon (KST4290, ALK4290) is a small molecule, orally active inhibitor against CCR3, the natural receptor for chemokine eotaxin, decreases inflammatory cytokines in preclinical models.Lazucirnon (KST4290, ALK4290) blocks eotaxin from binding to its G-protein coupled receptor (GPCR) CCR3.CCR3 plays an important modulatory role in inflammation, immune cell recruitment, and neovascularization, processes important for the pathogenesis of wet age-related macular degeneration (wet AMD) and other neurological and immunological diseases. |
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| DC70602 |
ML339
Featured
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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. |
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| DC70745 |
RS-1269 |
RS-1269 is a highly potent, selective CCR4 antagonist, inhibits [125I]CCL17 binding to human CCR4 with IC50 of 27.7 nM.RS-1269 also has strong affinity to displace the CCL17 binding with IC50 of 27.0 nM in CCR4-expressing CHO cells.RS-1269 displays no competitive displacement in the binding of [125I]CCL3 (MIP-1α) to CCR1 and [125I]CCL2 (MCP-1) to CCR2b.RS-1269 dose-dependently inhibited CCL17-induced migration of Th2 cells with IC50 of 5.5 nM.Orally administered RS-1269 (30 mg/kg) ameliorates ovalbumin-induced ear swelling in mice.RS-1269 also inhibited LPS-induced TNF-α production in vivo. |
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| DC70746 |
RS-1748 |
RS-1748 is a highly potent, selective, orallu active CCR4 antagonist, inhibits [125I]CCL17 binding to human CCR4 with IC50 of 59.9 nM.RS-1748 displays no competitive displacement in the binding of [125I]CCL3 (MIP-1α) to CCR1 and [125I]CCL2 (MCP-1) to CCR2b. dose-dependently inhibited 50 nM CCL22-induced [Ca2+]i mobilization with IC50 of 28.3 nM, inhibited the binding of [35S]GTPgS to human CCR4-expressing CHO cells with IC50 of 18.4 nM.Orally administered RS-1748 (30 mg/kg) significantly lowered the total cell numbers and the eosinophils numbers in ovalbumin-sensitized guinea pigs. |
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| DC70817 |
SX-682
Featured
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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. |
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| DC70881 |
Vercirnon |
Vercirnon (GSK1605786A, CCX282-B) is a potent, selective, orally bioavailable antagonist of CCR9, inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 of 5.4 and 3.4 nM, respectively.Vercirnon (GSK1605786A, CCX282-B) displays high selectivity for CCR9 over CCR1-12 and CX3CR1-7 (IC50>10 uM).Vercirnon (GSK1605786A, CCX282-B) is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.CCX282-B also inhibited mouse and rat CCR9-mediated chemotaxis.Inhibition of CCR9 with CCX282-B results in normalization of Crohn's disease such as histopathology associated with the TNF(ΔARE) mice. |
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| DC71662 |
CXCR4 probe 1 |
CXCR4 probe 1 (compound 5) is a potent and specific CXCR4-targeted PET tracer with an IC50 value of 6.9 nM against CXCR4-specific antagonist peptide, TN14003. CXCR4 probe 1 has potential to be used as CXCR4-specific imaging probe to diagnose and monitor the prognosis of inflammatory diseases, CXCR4-positive tumors, and metastatic cancers. |
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| DC72110 |
RPT193
Featured
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RPT193 is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. RPT193 can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research. |
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| DC72117 |
ACT-660602 |
ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research. |
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| DC72523 |
BAY-3153 |
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). |
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| DC72524 |
FLX475
Featured
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FLX475 is a potent CCR4 antagonist that blocks regulatory T cells that interfere with effective antitumor immune responses and has antitumor activity. |
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| DC72766 |
PF-07054894
Featured
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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. |
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| DC72882 |
MR120 |
MR120 (CCR6 antagonist 1b) is a potent, selective CCR6 antagonist, disrupts the CCL20-induced chemotaxis of CCR6+CD4+ T cells. |
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