| S0129 |
SB-297006
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SB-297006 is an antagonist of C-C chemokine receptor 3 (CCR3) that suppresses antigen-induced accumulation of T(h)2 as well as eosinophils in the lungs. This compound suppressed CCL11-induced Th2 chemotaxis with IC50 of 2.5 μM.
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JHEP Rep, 2023, 5(9):100805
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Cell Death Dis, 2022, 13(5):478
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| S3479 |
R243
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R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis.
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Cell Prolif, 2025, e70032.
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| S3494 |
Vicriviroc maleate
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Vicriviroc maleate (SCH-417690 maleate, SCH-D maleate) is a potent, selective, orally bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells.
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Breast Cancer Res, 2021, 23(1):11
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| S9738 |
RS504393
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RS504393, an extremely selective CC chemokine receptor (CCR) 2 antagonist with IC50 of 98 nM, also targets multiple receptors for inhibition of CCR2b and CCR1 receptors when administrated in higher concentration.
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Mol Psychiatry, 2024, 10.1038/s41380-024-02826-9
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| S6555 |
AZD2098
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AZD2098 is a potent and bioavailable CCR4 receptor antagonist with pIC50 of 7.8.
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Neurooncol Adv, 2022, 4(1):vdab194
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| S8361 |
PF-4136309
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PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2.
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Signal Transduct Target Ther, 2025, 10(1):81
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| E4715 |
SB-328437
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SB-328437 is a non-peptide small molecule, potent and selective antagonist of CCR3 with an IC50 of 4.5 nM. It is important for eosinophil recruitment, a process that is thought to be crucial in the pathology of several inflammatory diseases including asthma, allergic rhinitis, and eczema.
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| S7538 |
RS-102895 Hydrochloride
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RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.
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| E0486 |
C-021
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C-021 is a potent CCR4 antagonist with IC50 values of 0.14 μM and 39 nM for inhibition of chemotaxis in human and mouse respectively.
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| E0395 |
Vercirnon
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Vercirnon (GSK1605786A, CCX-282, Traficet-EN), an orally bioavailable, selective, and potent antagonist of CCR9, is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9.
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| E5955New |
CCR6 antagonist 1
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CCR6 antagonist 1 is a potent antagonist of CCR6 that inhibits the CCL20/CCR6 axis. It can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs).
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| S0438 |
TAK-779
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TAK-779 (Takeda 779), a nonpeptide compound, is a potent antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5. It also exhibits highly potent and selective inhibition of R5 HIV-1 replication with EC50 and EC90 of 1.2 and 5.7 nM, respectively. It also suppresses the development of the cytokine storm in the murine model of the SARS-CoV-2-related acute respiratory distress syndrome.
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| S3032 |
Bindarit (AF 2838)
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Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.
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Exp Mol Med, 2024, 56(2):408-421.
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PLoS Pathog, 2024, 20(11):e1012747
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J Biol Chem, 2023, S0021-9258(23)02393-1
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| S3205 |
Perillaldehyde
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Perillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway.
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Front Cell Dev Biol, 2025, 13:1598520
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| S0777 |
Isuzinaxib (APX-115 free base)
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Isuzinaxib (APX-115 free base, Ewha-18278 free base) is a potent, orally active inhibitor of pan NADPH-oxidase (pan-Nox) with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. This compound significantly suppresses the expression of inflammatory molecules including MCP-1/CCL2, IL-6, and TNFα in the diabetic kidney.
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