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ChEMBL ligand: CHEMBL134074 |
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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 | Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 5.2 | pKi | 6309.57 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
ChEMBL | Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 5.6 | pKi | 2511.89 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
ChEMBL | Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 6.07 | pKi | 851.14 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
ChEMBL | Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 6.28 | pKi | 524.81 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
ChEMBL | Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 6.35 | pKi | 446.68 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
ChEMBL | Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells | B | 6.66 | pKi | 218.78 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
ChEMBL | Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2) | B | 6.68 | pKi | 208.93 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
GtoPdb | - | - | 6.7 | pKi | - | - | - | J Med Chem (2003) 46: 4070-86 [PMID:12954060] |
ChEMBL | Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 6.76 | pKi | 173.78 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
ChEMBL | Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 7.23 | pKi | 58.88 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
ChEMBL | Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity) | F | 7.05 | pIC50 | 89 | nM | IC50 | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
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]