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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 |
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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]