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CCR

CC chemokine receptors (or beta chemokine receptors) are integral membrane proteins that specifically bind and respond to cytokines of the CC chemokine family. They represent one subfamily of chemokine receptors, a large family of G protein-linked receptors that are known as seven transmembrane (7-TM) proteins since they span the cell membrane seven times. To date, ten true members of the CC chemokine receptor subfamily have been described. These are named CCR1 to CCR10 according to the IUIS/WHO Subcommittee on Chemokine Nomenclature.

  • Maraviroc
    T6016376348-65-1
    Maraviroc (Selzentry) is a C-C Chemokine Receptor Type 5 (CCR5) antagonist, and for MIP-1α(IC50=3.3 nM), MIP-1β (IC50=7.2 nM) and RANTES(IC50=5.2 nM).Maraviroc inhibits HIV-1 entry via CCR5 coreceptor interaction.
    • $47
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  • Pirfenidone
    T238653179-13-8
    Pirfenidone (AMR69) inhibits the production of CCL2 and CCL12 in fibroblasts and also decreases TGF-β2 protein levels. Pirfenidone is an antifibrotic agent that is commonly used in studies related to pulmonary fibrosis and also has anti-inflammatory activity.
    • $30
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  • Bindarit
    T6413130641-38-2
    Bindarit (AF2838) displays specific inhibition against monocyte chemotactic proteins MCP-1 CCL2, MCP-3 CCL7 and MCP-2 CCL8.
    • $52
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  • CCX354
    T152531010073-75-2In house
    CCX354 (CCR1 antagonist 1) is a potent small molecule CCR1 antagonist with anti-inflammatory activity for the treatment of rheumatoid arthritis.
    • $290
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  • INCB3344
    TQ01031262238-11-8
    INCB3344 is an effective, specific and orally bioavailable CCR2 antagonist with IC50 values of 9.5 nM (mCCR2) and 5.1 nM (hCCR2) in binding antagonism and 7.8 nM (mCCR2) and in 3.8 nM (hCCR2) antagonism of chemotaxis activity.
    • $64
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  • Cenicriviroc
    TQ0297497223-25-3
    Cenicriviroc (TAK-652) is an orally active, dual CCR2 CCR5 antagonist that inhibits both HIV-1 and HIV-2, exhibiting potent anti-infective and anti-inflammatory activity.
    • $63
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  • BMS-817399
    T268611202400-18-7In house
    BMS-817399 is an orally active antagonist of CCR1 with IC50s of binding affinity and chemotaxis inhibition potencies and can be used in studies about rheumatoid arthritis.
    • $163
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  • K777
    T15641233277-99-1In house
    K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.
    • $78
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  • BX471
    T2375217645-70-0
    BX471 (BX 471) is a potent, selective non-peptide CCR1 antagonist.
    • $35
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  • AZ084
    T10425929300-19-6
    AZ084 is a potent, selective, allosteric, and orally active CCR8 antagonist (Ki: 0.9 nM) with potential to treat asthma.
    • $135
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  • RS 504393
    T5384300816-15-3
    RS 504393 is a highly selective CCR2 chemokine receptor antagonist (IC50s: 89 nM and > 100 μM for human recombinant CCR2 and CCR1).
    • $43
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  • R243
    T24700688352-84-3
    R243 is CCR8 signaling and chemotaxis inhibitor.
    • $36
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  • J-113863
    T11699353791-85-2
    J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.
    • $54
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  • Vercirnon
    T17225698394-73-9
    Vercirnon (Traficet-EN) is a selective and potent antagonist of CCR9 (IC50: 10 nM). It is also used in the research of inflammatory bowel diseases.
    • $107
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  • MK-0812 Succinate
    T16091851916-42-2
    MK-0812 Succinate is an effective and selective CCR2 antagonist. It also has a high affinity at CCR2.
    • $59
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  • CCR2 antagonist 3
    T107121380100-86-6
    CCR2 antagonist 3 (AZD-2927) is an antagonist of CCR2.
    • $107
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  • CCX140
    T149091100318-47-5
    CCX140 (CCX140-B) (CCX140-B) is an antagonist of CCR2.
    • $50
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  • AZD2098
    T4300566203-88-1
    AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor used for asthma research.
    • $30
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  • CCR2 antagonist 4
    T13114226226-39-7
    CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist with IC50 values of 180 nM and 24 nM for CCR2 inhibition and MCP-1-induced chemotaxis inhibition, respectively.
    • $48
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  • CCR6 inhibitor 1
    T107152437547-04-9
    CCR6 inhibitor 1 is an effective and selective inhibitor of CCR6 (IC50 of monkey and human CCR6 was 0.45 nM and 6 nM, respectively). CCR6 is associated with both autoimmune and non-autoimmune diseases, so CCR6 inhibitor 1 is useful for in vitro and in vivo pathophysiology studies as a small molecule inhibitor of CCR6.
    • $118
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  • RS102895
    TQ0283300815-41-2
    RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.
    • $37
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  • CCR8 antagonist 1
    T9983723304-76-5
    CCR8 antagonist 1 is an antagonist of C-C Motif Chemokine Receptor 8 (CCR8) with a Ki value of 1.6 nM.
    • $47
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  • SB 328437
    T23321247580-43-4
    SB 328437 ((S)-methyl 2-(1-naphthamido)-3-(4-nitrophenyl)propanoate) is an effective and selective antagonist of CCR3 (IC50 = 4.5 nM).
    • $35
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  • DAPTA
    T7624106362-34-9
    DAPTA (Adaptavir) is an inhibitor of CCR5, shows potent anti-HIV activities.
    • $47
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  • 7,4'-Dihydroxyflavone
    TN12732196-14-7
    7,4'-Dihydroxyflavone (4',7-Dihydroxyflavone) can induce transcription of nodulation (nod) genes in Rhizobium meliloti. It has inhibitory activities against COX-2.
    • $33
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  • PF-4136309
    T34301341224-83-6
    PF-4136309 (INCB8761) is a specific, effective, and orally bioavailable CCR2 antagonist.
    • $30
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  • RS102895 hydrochloride
    T127731173022-16-6
    RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).
    • $40
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  • TAK-779
    T7499229005-80-5
    TAK-779 (Takeda 779) is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).
    • $38
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  • C-021
    T21870864289-85-0In house
    C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. It effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor (IC50: 18 nM).
    • $29
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  • BI-6901
    T364782040401-92-9
    BI-6901 is a CCR10 antagonist. In a mouse model of DNFB exposure hypersensitivity, BI 6901 displays its anti-inflammatory response in a dose-dependent manner.
    • $199
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  • CCR3 antagonist 1
    T10156879399-82-3In house
    CCR3 antagonist 1 is a potent CCR3 antagonist used in researching inflammatory and immunologic diseases.
    • $93
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  • CCR6 antagonist 1
    T60145588674-64-0
    CCR6 antagonist 1, a chemical compound acting as a CCR6 antagonist, effectively inhibits the CCL20/CCR6 axis. Its utility lies in research focused on autoimmune-mediated inflammatory diseases, including inflammatory bowel diseases (IBDs).
    • $43
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  • Vicriviroc maleate
    T3435599179-03-0
    Vicriviroc maleate (SCH-417690 (maleate))(Sch-417690) is a piperazine-based CCR5 receptor antagonist with activity against human immunodeficiency virus. The IC50 value is 0.91 nM in clinical development for the treatment of HIV-1.
    • $35
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  • CCR2 antagonist 5
    T276821228650-83-6In house
    CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).JNJ-41443532 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.
    • $110
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  • BMS-813160
    T45841286279-29-5
    BMS-813160 is the first dual CCR2/CCR5 antagonist to enter Clinical development for cardiovascular.
    • $34
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  • CCR2-RA-[R]
    T14900512177-83-2
    CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).
    • $39
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  • Artemotil
    T332775887-54-6
    Artemotil (SM-227) is a new, fast-acting antimalarial drug.
    • $50
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  • GSK2239633A
    T114811240516-71-5
    GSK2239633A is an allosteric antagonist of CC-chemokine receptor 4 (CCR4) with a pIC50 of 7.96 for the binding of [125I]-TARC to human CCR4.
    • $32
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  • INCB-9471
    T71665869769-98-2In house
    INCB-9471 is a CCR5 antagonist with anti-HIV activity and inhibits the interaction between HIV-1 gp120.
    • $628
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  • Leronlimab
    T77059674782-26-4
    Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody with both anti-HIV and anti-tumor activity, inhibiting CCR-mediated HIV-1 virus and cancer cell metastasis in mouse tumor models. Leronlimab can be used to study HIV, non-alcoholic steatohepatitis (NASH), and breast cancer.
    • $198
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  • CCR1 antagonist 6
    T107082436773-01-0In house
    CCR1 antagonist 6 is a CCR1 antagonist (IC50: 3 nM).
    • $380
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  • MLN-3897 TFA
    T28072L
    MLN-3897 TFA is a potent CCR1 antagonist that inhibits the binding of 125I-MIP-1α to THP-1 cell membranes.
    • $195
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  • Aplaviroc
    T14307461443-59-4In house
    Aplaviroc (AK 602), an SDP derivative, is a CCR5 antagonist with IC50 values of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW.
    • $545
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  • C-021 dihydrochloride
    T106391784252-84-1In house
    C-021 dihydrochloride is a potent CCR4 antagonist that effectively inhibits functional chemotaxis in humans and mice, with IC50 values of 140 nM and 39 nM, respectively.
    • $68
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  • MLN-3897
    T280721010731-97-1In house
    MLN-3897 (CCR1 antagonist 10) is an orally active antagonist of CCR1 with a Ki of 2.3 nM for 125I-MIP-1α binding to THP-1 cell membranes. MLN-3897 inhibits Akt signaling and MM cell survival and proliferation.
    • $1,330
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  • INCB 3284
    T11648887401-92-5In house
    INCB 3284 is an orally available, selective and high affinity chemokine receptor 2 (CCR2) antagonist that inhibits monocyte chemotactic protein 1 from interacting with hCCR2.INCB 3284 is used in the study of hemorrhagic shock.
    • $33
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  • MK-0812
    TQ0182624733-88-6
    MK-0812 is an effective and specific CCR2 antagonist.
    • $183
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  • AZD-4818
    T302581003566-93-5
    AZD-4818 (CCR1 antagonist) is a chemokine CCR1 antagonist for the treatment of chronic obstructive pulmonary disease.
    • $39
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  • RE-640
    T3188140926-75-6
    NSC-5844 (RE-640) (RE640) is a bisquinoline compound with C-C chemokine receptor type 1 (CCR1)-agonistic activities.
    • $29
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  • ZK 756326
    T3360874911-96-3
    ZK 756326 is a selective, non-peptide CCR8 chemokine receptor agonist (IC50: 1.8 μM, in human; 2.6 μM, in mouse). Displays no activity at CCR4 5 and CXCR3 4 and shows higher 28-fold selectivity over 26 other GPCRs (less selective at α2A and 5-HT receptors). Induces chemotaxis and inhibits Env-mediated (HIV) cell-cell fusion.
    • $34
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