MG-277 [Ligand Id: 11724] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4449512
  • MDM2 proto-oncogene/p53-binding protein Mdm-2 in Human [ChEMBL: CHEMBL5023] [GtoPdb: 3136] [UniProtKB: Q00987]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
MDM2 proto-oncogene/p53-binding protein Mdm-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5023] [GtoPdb: 3136] [UniProtKB: Q00987]
ChEMBL Displacement of PMDM6-F fluorescent probe from human recombinant His-tagged MDM2 (1 to 118 residues) after 15 mins by fluorescence polarization assay B 7.17 pIC50 67.5 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
cereblon/Protein cereblon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3763008] [GtoPdb: 3086] [UniProtKB: Q96SW2]
ChEMBL Binding affinity to cereblon in human MDA-MB-231 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 100 uM of lenalidomide B 5.67 pIC50 2138 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human MDA-MB-468 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 100 uM lenalidomide B 5.68 pIC50 2072 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human MDA-MB-231 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 30 uM of lenalidomide B 5.86 pIC50 1372 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human RV4:11/IRMI-2 cells harboring p53 hotspot mutation Y236H/R249G assessed as reduction in cell growth inhibition measured after 4 days in presence of 100 uM lenalidomide B 6.01 pIC50 981.8 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human MDA-MB-468 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 30 uM lenalidomide B 6.02 pIC50 963.9 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human MDA-MB-231 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 10 uM of lenalidomide B 6.21 pIC50 623.1 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human RV4:11 cells expressing wild type p53 assessed as reduction in cell growth inhibition measured after 4 days in presence of 100 uM lenalidomide B 6.3 pIC50 495.5 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human MDA-MB-468 cells assessed as reduction in cell growth inhibition measured after 4 days in presence of 10 uM lenalidomide B 6.38 pIC50 418.9 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human RV4:11/IRMI-2 cells harboring p53 hotspot mutation Y236H/R249G assessed as reduction in cell growth inhibition measured after 4 days in presence of 30 uM lenalidomide B 6.4 pIC50 400.2 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human RV4:11 cells expressing wild type p53 assessed as reduction in cell growth inhibition measured after 4 days in presence of 30 uM lenalidomide B 6.68 pIC50 210.5 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human RV4:11/IRMI-2 cells harboring p53 hotspot mutation Y236H/R249G assessed as reduction in cell growth inhibition measured after 4 days in presence of 10 uM lenalidomide B 6.77 pIC50 168.1 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human RV4:11 cells expressing wild type p53 assessed as reduction in cell growth inhibition measured after 4 days in presence of 10 uM lenalidomide B 7.02 pIC50 95.7 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human MDA-MB-231 cells assessed as cell growth inhibition measured after 4 days B 7.49 pIC50 32.2 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 days B 7.54 pIC50 28.7 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human RV4:11/IRMI-2 cells harboring p53 hotspot mutation Y236H/R249G assessed as cell growth inhibition measured after 4 days B 8.51 pIC50 3.1 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
GtoPdb Binding affinity to cereblon in human RV4:11/IRMI-2 cells that express p53 mutation Y236H/R249G assessed as cell growth inhibition measured after 4 days. - 8.51 pIC50 3.1 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]
ChEMBL Binding affinity to cereblon in human RV4:11 cells expressing wild type p53 assessed as cell growth inhibition measured after 4 days B 8.7 pIC50 2 nM IC50 J Med Chem (2019) 62: 9471-9487 [PMID:31560543]

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]