RS-504393 [Ligand Id: 781] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL134074
  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
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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 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]