INCB8761 [Ligand Id: 9032] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2029422 |
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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 34:
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]
