INCB8761 [Ligand Id: 9032] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2029422
  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
  • CCR2/C-C chemokine receptor type 2 in Mouse [ChEMBL: CHEMBL5412] [GtoPdb: 59] [UniProtKB: P51683]
  • CCR2/C-C chemokine receptor type 2 in Rat [ChEMBL: CHEMBL1293204] [GtoPdb: 59] [UniProtKB: O55193]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
ChEMBL Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry F 7.72 pIC50 19 nM IC50 ACS Med Chem Lett (2011) 2: 913-918 [PMID:24900280]
GtoPdb - - 8.28 pIC50 5.2 nM IC50 ACS Med Chem Lett (2011) 2: 913-8 [PMID:24900280]
ChEMBL Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting B 8.28 pIC50 5.2 nM IC50 ACS Med Chem Lett (2011) 2: 913-918 [PMID:24900280]
ChEMBL Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy F 8.41 pIC50 3.9 nM IC50 ACS Med Chem Lett (2011) 2: 913-918 [PMID:24900280]
ChEMBL Inhibition of CCR2-mediated calcium mobilization F 8.48 pIC50 3.3 nM IC50 ACS Med Chem Lett (2011) 2: 913-918 [PMID:24900280]
ChEMBL Inhibition of CCR2-mediated Erk phosphorylation B 9.3 pIC50 0.5 nM IC50 ACS Med Chem Lett (2011) 2: 913-918 [PMID:24900280]
CCR2/C-C chemokine receptor type 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5412] [GtoPdb: 59] [UniProtKB: P51683]
ChEMBL Binding affinity to mouse CCR2 B 7.77 pIC50 17 nM IC50 ACS Med Chem Lett (2011) 2: 913-918 [PMID:24900280]
ChEMBL Antagonist activity at mouse CCR2 F 7.8 pIC50 16 nM IC50 ACS Med Chem Lett (2011) 2: 913-918 [PMID:24900280]
CCR2/C-C chemokine receptor type 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293204] [GtoPdb: 59] [UniProtKB: O55193]
ChEMBL Binding affinity to rat CCR2 B 7.89 pIC50 13 nM IC50 ACS Med Chem Lett (2011) 2: 913-918 [PMID:24900280]
ChEMBL Antagonist activity at rat CCR2 F 8.55 pIC50 2.8 nM IC50 ACS Med Chem Lett (2011) 2: 913-918 [PMID:24900280]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]dofetilide from human ERG B 4.52 pIC50 >30000 nM IC50 ACS Med Chem Lett (2011) 2: 913-918 [PMID:24900280]
ChEMBL Inhibition of human ERG by patch clamp assay B 4.7 pIC50 20000 nM IC50 ACS Med Chem Lett (2011) 2: 913-918 [PMID:24900280]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]