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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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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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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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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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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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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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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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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CCR2 antagonist 3

T107121380100-86-6

CCR2 antagonist 3 (AZD-2927) is an antagonist of CCR2.

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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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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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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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RS102895

TQ0283300815-41-2

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

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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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MK-0812 Succinate

T16091851916-42-2

MK-0812 Succinate is an effective and selective CCR2 antagonist. It also has a high affinity at CCR2.

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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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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.

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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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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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Artemotil

T332775887-54-6

Artemotil (SM-227) is a new, fast-acting antimalarial drug.

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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).

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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.

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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 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.

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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.

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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.

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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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DAPTA

T7624106362-34-9

DAPTA (Adaptavir) is an inhibitor of CCR5, shows potent anti-HIV activities.

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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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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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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.

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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).

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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.

$100

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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.

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SB297006

T467458816-69-6

SB297006 is an antagonist of C-C chemokine receptor 3 (CCR3; IC50 = 39 nM), which normally is activated by eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES, and MIP-1δ. It is at least 250-fold selective for CCR3 over a panel of other chemokine receptors. SB 297006 blocks CCR3-mediated calcium mobilization induced by eotaxin, eotaxin-2, and MCP-4 in transfected cells. It suppresses antigen-induced accumulation of Th2 lymphocytes and eosinophils in lungs of mice when delivered subcutaneously (100 mg kg).

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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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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.

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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.

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