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GPCR/G Protein

Cholecystokinin Receptor

Melanin-concentrating Hormone Receptor (MCHR)

(34)

Melanocortin Receptor

Neuropeptide FF Receptor

(9)

Neuropeptide W

(3)

Neuropeptide Y Receptor

Prostaglandin Receptor

(435)

Protease-activated Receptor

Succinate Receptor 1 (SUCNR1)

Immunology/Inflammation

Aryl Hydrocarbon Receptor

Immunology/Inflammation related

NOD-like Receptor (NLR)

Prostaglandin Receptor

Reactive Oxygen Species

Thrombopoietin Receptor

Microbiology/Virology

Penicillin-binding protein (PBP)

(4)

RSV

(86)

Reverse Transcriptase

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.

Filter HomeSignaling PathwaysImmunology/Inflammation-Microbiology/Virology-GPCR/G ProteinCCR

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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Cosalane

T23910154212-56-3In house

Cosalane (NSC 658586) is an HIV replication inhibitor, an inhibitor of chemokine receptor 7 (CCR7) signalling in humans and mice, with antiviral activity that blocks the binding of CCR7 to its natural ligands, CCL19 and CCL21.

$372

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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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BX471

T2375217645-70-0

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

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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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BMS-813160

T45841286279-29-5

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

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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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Tivumecirnon

T698342174938-78-2

Tivumecirnon (FLX475) is a selective and orally active CCR4 antagonist that inhibits the infiltration and migration of regulatory T cells (Tregs) into the tumour microenvironment, exhibiting antitumour activity.

$169

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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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RS102895

TQ0283300815-41-2

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

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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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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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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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Mogamulizumab

T767821159266-37-1

Mogamulizumab (KW-0761) is a monoclonal antibody targeting T cell CC chemokine receptor 4. It exhibits anticancer activity by eliminating tumor cells through antibody-dependent cytotoxicity (ADCC) and can be used in the study of cancer, adult T-cell leukemia/lymphoma (ATLL), and cutaneous T-cell lymphoma (CTCL).

$476

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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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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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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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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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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).

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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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RE-640

T3188140926-75-6

NSC-5844 (RE-640) (RE640) is a bisquinoline compound with C-C chemokine receptor type 1 (CCR1)-agonistic activities.

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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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AZD2098

T4300566203-88-1

AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor used for asthma research.

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