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

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ChEMBL ligand: CHEMBL3125702 (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]
Protein Mdm4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255126] [UniProtKB: O15151]
ChEMBL Inhibition of MDM4 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 6207-6230 [PMID:35420431]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]