| S3383 |
RS102895
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RS 102895 is a small molecule antagonist of CCR2 with an IC50 of 360 nM.
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Exp Mol Med, 2024, 56(2):408-421.
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Theranostics, 2022, 12(17):7351-7370
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| S0085 |
BMS-813160
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BMS-813160 is a potent, well-absorbed dual CCR2 and CCR5 chemokine antagonist. This compound inhibits inflammatory processes, angiogenesis, tumor cell migration, tumor cell proliferation and invasion.
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Commun Biol, 2024, 7(1):1304
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Mater Today (Kidlington), 2023, 62:33-50
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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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明海歯学, 2023, S19
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Neuro-Oncology Advances, 2022, vdab194
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Neurooncol Adv, 2022, 4(1):vdab194
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| S3494 |
Vicriviroc maleate
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Vicriviroc maleate(SCH-417690 maleate,SCH-D maleate) is a potent, selective, oral 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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| 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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Journal of the American Heart Association, December 17, 2025, e039153
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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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| 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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| E6879New |
Carboxyethylgermanium sesquioxide
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Carboxyethylgermanium sesquioxide(Repagermanium, DMX-200) is an orally active small‑molecule inhibitor of the C‑C chemokine receptor type 2 (CCR2) pathway and is used in combination with an angiotensin receptor blocker (ARB) to reduce proteinuria and slow kidney function decline in proteinuric chronic kidney diseases such as focal segmental glomerulosclerosis (FSGS).
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| E0486 |
C-021
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C-021 is a potent CCR4 antagonist with IC50 values are 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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| E5955 |
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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| E1584New |
CCR6 inhibitor 1
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CCR6 inhibitor-1 is a potent and selective inhibitor of CCR6 with IC50 of 0.45 nM and 6 nM for monkey and human CCR6, respectively. It potently inhibits human B-cell migration and ERK phosphorylation, exhibiting potential as a treatment for autoimmune diseases.
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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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International Journal of Biological Sciences, 2025, 21(14):6113-6131
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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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| 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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Insects, 2026, 17(3)300
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American Journal of Physiology-Renal Physiology, 2024, F202-F218
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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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