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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.

  • 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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  • Artemotil
    T332775887-54-6
    Artemotil (SM-227) is a new, fast-acting antimalarial drug.
    • $50
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    TargetMol | Citations Cited
  • 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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  • CCR1 antagonist 6
    T107082436773-01-0In house
    CCR1 antagonist 6 is a CCR1 antagonist (IC50: 3 nM).
    • $380
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  • Aplaviroc
    T14307461443-59-4In house
    Aplaviroc (AK 602) is a novel and highly potent CCR5 antagonist with antiviral activity that inhibits HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW and can be used in the study of human immunodeficiency virus infection.
    • $545
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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-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.
    • $195
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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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  • 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).
    • $47
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  • K777
    T15641233277-99-1In house
    K777 is a potent, orally active and irreversible inhibitor of cysteine protease. K777 is a potent CYP3A4 inhibitor (IC50= 60 nM). K777 is also a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, which is the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 targets cathepsin-mediated cell entry and wxibits a broad-spectrum antiviral activity. K777 inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.
    • $78
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  • CCR3 antagonist 1
    T10156879399-82-3In house
    CCR3 antagonist 1 is a potent CCR3 antagonist, used for the research of inflammatory and immunologic diseases.
    • $93
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  • C-021 dihydrochloride
    T106391784252-84-1In house
    C-021 dihydrochloride is a potent CCR4 antagonist. It potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM.
    • $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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  • MK-0812
    TQ0182624733-88-6
    MK-0812 is an effective and specific CCR2 antagonist.
    • $183
    35 days
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  • BX471
    T2375217645-70-0
    BX471 (BX 471) is a potent, selective non-peptide CCR1 antagonist.
    • $35
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    TargetMol | Citations Cited
  • Pirfenidone
    T238653179-13-8
    Pirfenidone (AMR69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production. Pirfenidone inhibits fibroblast, epidermal, platelet-derived, and transforming beta-1 growth factors, thereby slowing tumor cell proliferation. This agent also inhibits DNA synthesis and the production of mRNA for collagen types I and III, resulting in a reduction in radiation-induced fibrosis.
    • $30
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    TargetMol | Citations Cited
  • 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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    TargetMol | Citations Cited
  • WAY-639418
    T9942643042-43-7
    WAY-639418 has potential anti-inflammatory and anti-HIV activity and can be used to study CCR5-mediated inflammatory and immunomodulatory diseases.
    • $41
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  • CMPD167
    T82702313994-79-5
    CMPD167 (MRK-1) is a potent, orally active inhibitor of CCR5 with significant in vitro antiviral efficacy [1].
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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.
    • $47
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  • Plozalizumab
    T771181610761-46-0
    Plozalizumab (MLN-1202) is a humanized selective and potent anti-CCR2 antibody.Plozalizumab has antitumor activity.Plozalizumab is used in the study of malignant melanoma.
    • $372
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  • INCB 3284
    T11648887401-92-5
    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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  • Cenicriviroc Mesylate
    T10756497223-28-6
    Cenicriviroc Mesylate is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.
    • $432
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  • CCR1 antagonist 9
    T107101220026-26-5
    CCR1 antagonist 9 is an effective and selective CCR1 antagonist (IC50: 6.8 nM in calcium flux assay).
    • $259
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  • CCR5 antagonist 1
    T10714716354-86-8
    CCR5 antagonist 1 is a CCR5 antagonist extracted from WO 2004054974 A2. It can inhibit HIV replication.
    • $2,870
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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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  • 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.
    • $59
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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-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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  • INCB-9471
    T71665869769-98-2
    INCB-9471 is a CCR5 antagonist with anti-HIV activity and inhibits the interaction between HIV-1 gp120.
    • $628
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  • SB-649701
    T79095935262-95-6
    SB-649701 is a potent antagonist of the human CCR8 receptor, exhibiting a pIC50 value of 7.7, and is utilized in asthma research [1].
    • $1,520
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  • 3-(hydroxymethyl)cyclopentanone
    TN2951113681-11-1
    3-Hydroxymethylcyclopentanone is a precursor to synthesize methyl epijasmonate. 3-Hydroxymethylcyclopentanone compounds, which are useful as intermediates in the preparation of HIV chemokine CCR-5 receptor antagonists.
    • $360
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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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  • CCR2 antagonist 1
    T107111683534-96-4
    CCR2 antagonist 1 is a high-affinity and long-residence-time antagonist of CCR2 (Ki: 2.4 nM).
    • $2,220
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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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  • CCR1 antagonist 8
    T148991295298-26-8
    CCR1 antagonist 8, a third azaindazole series compound, is a CCR1 antagonist (IC50: 1.8 nM in Ca2+ flux assay).
    • $1,080
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  • AZ084
    T10425929300-19-6
    AZ084 is a potent, selective, allosteric, and oral active CCR8 antagonist (Ki: 0.9 nM). It has the potential to treat asthma.
    • $135
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  • BMS-813160
    T45841286279-29-5
    BMS-813160 is the first dual CCR2/CCR5 antagonist to enter Clinical development for cardiovascular.
    • $57
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  • Eburicoic acid
    TN1599560-66-7
    Eburicoic acid (ZINC4655149) exhibits anti-inflammatory and antioxidant activity thereby protecting the liver from CCl4-induced hepatic damage and can be used in studies about anti-liver cancer.
    • $76
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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.
    • $68
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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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  • 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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  • 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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  • 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-04634817
    T12419L1228111-63-4
    PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2/CCR5 antagonist. It also has comparable human and rodent CCR2 potency (rat IC50=20.8 nM). PF-0463481
    • $1,820
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  • IPG7236
    T790962756350-91-9
    IPG7236, a selective CCR8 antagonist, demonstrates notable tumor suppression in a mouse xenograft model of human breast cancer and is applicable in cancer research [1].
    • $1,670
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  • AZD2423
    T143731229603-37-5
    AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator and it has an IC50 of 1.2 nM for CCR2 Ca2+ flux [1][2][3].
    • $1,970
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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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  • 5-Hydroxy-7,8-dimethoxyflavanone
    TN3119113981-49-0
    5-Hydroxy-7,8-dimethoxyflavanone is isolated from Andrographis paniculata Nees. leaves and roots with anti-inflammatory activity.
    • $2,590
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