AMG-232 [Ligand Id: 11133] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3125702 (Amg 232, Amg-232, AMG 232, AMG-232, Krt-232, KRT-232, Mdm2 inhibitor amg-232, Navtemadlin)
  • 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 Binding affinity to human MDM2 by by Surface Plasmon Resonace (SPR) spectroscopy binding assay B 10.35 pKd 0.04 nM Kd J Med Chem (2014) 57: 1454-1472 [PMID:24456472]
ChEMBL Binding affinity to human MDM2 by by surface plasmon resonace spectroscopy B 10.35 pKd 0.04 nM Kd J Med Chem (2014) 57: 10499-10511 [PMID:25384157]
GtoPdb Binding affinity determined in a SPR assay, measuring inhibition of interaction between human p53 and recombinant MDM2. - 10.35 pKd 0.05 nM Kd J Med Chem (2014) 57: 1454-72 [PMID:24456472]
ChEMBL Binding affinity to human MDM2 by by isothermal titration calorimetry B 10.42 pKd 0.04 nM Kd J Med Chem (2014) 57: 10499-10511 [PMID:25384157]
ChEMBL Binding affinity to MDM2 in human SJSA1 cells assessed as induction of p21 gene level after 7 hrs by qRT-PCR assay in presence of 10% human serum B 7.33 pIC50 47 nM IC50 J Med Chem (2014) 57: 10499-10511 [PMID:25384157]
ChEMBL Binding affinity to human GST-thrombin-tagged MDM2 ( 1 to 188 aa) assessed as inhibition of interaction with human p53 preincubated with compound for 20 mins by HTRF assay B 9.2 pIC50 0.63 nM IC50 J Med Chem (2014) 57: 10499-10511 [PMID:25384157]
ChEMBL Binding affinity to human GST-thrombin-tagged MDM2 assessed as inhibition of interaction with human p53 after 1 hr by HTRF assay B 9.22 pIC50 0.6 nM IC50 J Med Chem (2014) 57: 1454-1472 [PMID:24456472]
ChEMBL Inhibition of MDM2 (unknown origin) B 9.22 pIC50 0.6 nM IC50 Eur J Med Chem (2019) 176: 476-491 [PMID:31128449]

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]