Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL3125702 (Amg 232, Amg-232, AMG 232, AMG-232, Krt-232, KRT-232, Mdm2 inhibitor amg-232, Navtemadlin) |
---|
There should be some charts here, you may need to enable JavaScript!
|
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]