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.

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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.

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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.

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bindarit

T6413130641-38-2

Bindarit is a selective inhibitor of monocyte chemoattractant proteins MCP-1 CCL2, MCP-3 CCL7 and MCP-2 CCL8 with anti-inflammatory effects. Bindarit specifically inhibits p65- and p65 p50-induced MCP-1 promoter activation and has no effect on other tested activated promoters.

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BX471

T2375217645-70-0

BX471 (BX 471) is a potent, selective non-peptide CCR1 antagonist.

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bms-813160

T45841286279-29-5

BMS-813160 is the first dual CCR2 CCR5 antagonist to enter Clinical development for cardiovascular.

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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.

$263

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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.

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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).

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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.

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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).

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R243

T24700688352-84-3

R243 is CCR8 signaling and chemotaxis inhibitor.

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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.

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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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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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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.

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BMS CCR2 22

T14688445479-97-0

BMS CCR2 22 is a potent and selective antagonist of CCR2 with calcium flux IC50 of 18 nM, chemotaxis IC50 of 1 nM, and binding IC50 of 5.1 nM.

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PF-4136309

T34301341224-83-6

PF-4136309 (INCB8761) is a specific, effective, and orally bioavailable CCR2 antagonist.

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RS102895

TQ0283300815-41-2

RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.

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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.

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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.

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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).

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CCX140

T149091100318-47-5

CCX140 (CCX140-B) (CCX140-B) is an antagonist of CCR2.

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RS102895 hydrochloride

T127731173022-16-6

RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).

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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.

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