MK-0812 [Ligand Id: 9048] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3305901
  • CCR2 in Monkey [GtoPdb: 59]
  • 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 in Monkey [GtoPdb: 59]
GtoPdb Measuring inhibition of [125]I-MCP-1 binding by MK-0812 on isolated monocytes. - 8.35 pIC50 4.5 nM IC50 J. Immunol. Methods (2010) 352: 101-10 [PMID:19913021]
CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
ChEMBL Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry B 9.32 pKd 0.48 nM Kd Eur. J. Med. Chem. (2015) 93: 121-134 [PMID:25666912]
ChEMBL Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry B 9.26 pKi 0.55 nM Ki Eur. J. Med. Chem. (2015) 93: 121-134 [PMID:25666912]

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]