S2003 |
Maraviroc
|
Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively. Maraviroc is used in the treatment of HIV infection. |
-
Neuron, 2023, S0896-6273(23)00268-4
-
J Transl Med, 2023, 21(1):196
-
Neural Regen Res, 2023, 18(1):141-149
|
|
S2907 |
Pirfenidone
|
Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3. |
-
Eur Respir J, 2024, 2300580
-
Acta Pharmacol Sin, 2023, 10.1038/s41401-023-01156-w
-
Front Immunol, 2023, 14:1070196
|
|
S3032 |
Bindarit
|
Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8. |
-
Exp Mol Med, 2024, 56(2):408-421.
-
J Biol Chem, 2023, S0021-9258(23)02393-1
-
Cell Death Discov, 2022, 8(1):466
|
|
S8512 |
Cenicriviroc
|
Cenicriviroc is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity. |
-
Int J Biol Sci, 2023, 19(8):2572-2587
-
Stem Cells, 2023, 41(6):672-683
-
Life Science Alliance, 2023, 6(6)
|
|
S2004 |
Vicriviroc Malate
|
Vicriviroc is a potent CCR5 antagonist with IC50 of 0.91 nM, showing broad-spectrum activity against genetically diverse HIV-1 isolates, and also drug-resistant viruses with RTI, PRI, or MDR phenotypes. Phase 3. |
-
Nature, 2013, 493(7430):51-5
-
Cancer Res, 2012, 72(15):3839-50
-
J Antimicrob Chemot, 2011, 66(4):802-12
|
|
S8501 |
Adaptavir (DAPTA)
|
Adaptavir (DAPTA, D-Ala-peptide T-amide, peptide T) is a water soluble potent, selective CCR5 antagonist which potently inhibits specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5. |
-
Cell Death Dis, 2022, 13(5):478
-
Proc Natl Acad Sci U S A, 2021, 118(9)e2017282118
-
FEBS J, 2020, 287(11):2367-2385
|
|
S8324 |
ZK756326 2HCl
|
ZK756326 is a full agonist of CCR8(Chemokine receptor 8) with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. |
-
Cancer Immunol Immunother, 2022, 10.1007/s00262-022-03196-3
-
J Exp Med, 2019, 216(12):2763-2777
|
|
S0129 |
SB-297006
|
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. SB-297006 suppressed CCL11-induced Th2 chemotaxis with IC50 of 2.5 μM. |
-
JHEP Rep, 2023, 5(9):100805
-
Cell Death Dis, 2022, 13(5):478
|
|
S8220 |
INCB3344
|
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity. |
-
Cancer Res, 2023, 83(16):2690-2703
-
Research Square, 2023, 10.21203/rs.3.rs-3674324/v1
|
|
S3383 |
RS102895
|
RS 102895 is a small molecule antagonist of CCR2 with an IC50 of 360 nM. |
-
Exp Mol Med, 2024, 56(2):408-421.
-
Theranostics, 2022, 12(17):7351-7370
|
|
S3494 |
Vicriviroc maleate
|
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. |
-
Breast Cancer Res, 2021, 23(1):11
|
|
S6555 |
AZD2098
|
AZD2098 is a potent and bioavailable CCR4 receptor antagonist with pIC50 of 7.8. |
-
Neurooncol Adv, 2022, 4(1):vdab194
|
|
S3479 |
R243
|
R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis. |
|
|
S7604 |
BX471
|
BX471 (ZK811752, BAY 865047, SH T 04268H) is a potent nonpeptide CC chemokine receptor-1 (CCR1) antagonist with Ki values of 1 nM and 5.5 nM in both MIP-1α and MCP-3 binding to CCR1-transfected HEK293 cells, respectively.
|
|
|
S7538 |
RS-102895 Hydrochloride
|
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. |
|
|
E0486 |
C-021
|
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. |
|
|
S0777 |
Isuzinaxib (APX-115 free base)
|
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. APX-115 free base (Ewha-18278 free base) significantly suppresses the expression of inflammatory molecules including MCP-1/CCL2, IL-6, and TNFα in the diabetic kidney. |
|
|
S9738 |
RS504393
|
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. |
|
|
S0085 |
BMS-813160
|
BMS-813160 is a potent, well-absorbed dual CCR2 and CCR5 chemokine antagonist. BMS-813160 inhibits inflammatory processes, angiogenesis, tumor cell migration, tumor cell proliferation and invasion. |
|
|
E0395 |
Vercirnon
|
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. |
|
|
S8361 |
PF-4136309
|
PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2. |
|
|
S3205 |
Perillaldehyde
|
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. |
|
|
S2907 |
Pirfenidone
|
Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3. |
- Eur Respir J, 2024, 2300580
- Acta Pharmacol Sin, 2023, 10.1038/s41401-023-01156-w
- Front Immunol, 2023, 14:1070196
|
|
S3032 |
Bindarit
|
Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8. |
- Exp Mol Med, 2024, 56(2):408-421.
- J Biol Chem, 2023, S0021-9258(23)02393-1
- Cell Death Discov, 2022, 8(1):466
|
|
S8512 |
Cenicriviroc
|
Cenicriviroc is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity. |
- Int J Biol Sci, 2023, 19(8):2572-2587
- Stem Cells, 2023, 41(6):672-683
- Life Science Alliance, 2023, 6(6)
|
|
S2004 |
Vicriviroc Malate
|
Vicriviroc is a potent CCR5 antagonist with IC50 of 0.91 nM, showing broad-spectrum activity against genetically diverse HIV-1 isolates, and also drug-resistant viruses with RTI, PRI, or MDR phenotypes. Phase 3. |
- Nature, 2013, 493(7430):51-5
- Cancer Res, 2012, 72(15):3839-50
- J Antimicrob Chemot, 2011, 66(4):802-12
|
|
S3479 |
R243
|
R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis. |
|
|
S7604 |
BX471
|
BX471 (ZK811752, BAY 865047, SH T 04268H) is a potent nonpeptide CC chemokine receptor-1 (CCR1) antagonist with Ki values of 1 nM and 5.5 nM in both MIP-1α and MCP-3 binding to CCR1-transfected HEK293 cells, respectively.
|
|
|
S0777 |
Isuzinaxib (APX-115 free base)
|
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. APX-115 free base (Ewha-18278 free base) significantly suppresses the expression of inflammatory molecules including MCP-1/CCL2, IL-6, and TNFα in the diabetic kidney. |
|
|
S3205 |
Perillaldehyde
|
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. |
|
|
S2003 |
Maraviroc
|
Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively. Maraviroc is used in the treatment of HIV infection. |
- Neuron, 2023, S0896-6273(23)00268-4
- J Transl Med, 2023, 21(1):196
- Neural Regen Res, 2023, 18(1):141-149
|
|
S8501 |
Adaptavir (DAPTA)
|
Adaptavir (DAPTA, D-Ala-peptide T-amide, peptide T) is a water soluble potent, selective CCR5 antagonist which potently inhibits specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5. |
- Cell Death Dis, 2022, 13(5):478
- Proc Natl Acad Sci U S A, 2021, 118(9)e2017282118
- FEBS J, 2020, 287(11):2367-2385
|
|
S0129 |
SB-297006
|
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. SB-297006 suppressed CCL11-induced Th2 chemotaxis with IC50 of 2.5 μM. |
- JHEP Rep, 2023, 5(9):100805
- Cell Death Dis, 2022, 13(5):478
|
|
S8220 |
INCB3344
|
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity. |
- Cancer Res, 2023, 83(16):2690-2703
- Research Square, 2023, 10.21203/rs.3.rs-3674324/v1
|
|
S3383 |
RS102895
|
RS 102895 is a small molecule antagonist of CCR2 with an IC50 of 360 nM. |
- Exp Mol Med, 2024, 56(2):408-421.
- Theranostics, 2022, 12(17):7351-7370
|
|
S3494 |
Vicriviroc maleate
|
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. |
- Breast Cancer Res, 2021, 23(1):11
|
|
S6555 |
AZD2098
|
AZD2098 is a potent and bioavailable CCR4 receptor antagonist with pIC50 of 7.8. |
- Neurooncol Adv, 2022, 4(1):vdab194
|
|
S7538 |
RS-102895 Hydrochloride
|
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. |
|
|
E0486 |
C-021
|
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. |
|
|
S9738 |
RS504393
|
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. |
|
|
S0085 |
BMS-813160
|
BMS-813160 is a potent, well-absorbed dual CCR2 and CCR5 chemokine antagonist. BMS-813160 inhibits inflammatory processes, angiogenesis, tumor cell migration, tumor cell proliferation and invasion. |
|
|
E0395 |
Vercirnon
|
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. |
|
|
S8361 |
PF-4136309
|
PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2. |
|
|