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ChEMBL ligand: CHEMBL4449512 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]