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]
Created with Highcharts 10.3.3ValuesChart context menuC-C chemokine receptor type 2pKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd MousepKi MousepIC50 MousepEC50 MousepKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuHERGpKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
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 35:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]