ChEMBL ligand: CHEMBL3125702 (Amg 232, AMG 232, AMG-232, Krt-232, KRT-232, Mdm2 inhibitor amg-232, Navtemadlin)
MDM2 proto-oncogene/E3 ubiquitin-protein ligase Mdm2 in Human [ChEMBL: CHEMBL5023] [GtoPdb: 3136] [UniProtKB: Q00987] There should be some charts here, you may need to enable JavaScript!
Protein Mdm4 in Human [ChEMBL: CHEMBL1255126] [UniProtKB: O15151] 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/E3 ubiquitin-protein ligase Mdm2 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	Homogenous Time-Resolved Fluorescence Assay (HTRF2 Assay): The standard assay conditions for the in vitro HTRF assay consisted of a 50 ul total reaction volume in black 384-well Costar polypropylene plates in 1×PBS buffer pH 7.4, 1 mM DTT, 0.1% BSA, 2.5 nM GST-hMDM2 (aa 1-188), 5 nM biotinylated-p53 (aa 1-83), 1.8 nM SA-XLent (Cisbio; Bedford, Mass.), 0.6 nM anti-GST cryptate monoclonal antibody (Cisbio; Bedford, Mass.) and 200 mM KF. Amino acid residues 1-188 of human MDM2 were expressed as an amino-terminal glutathione-S-transferase (GST) fusion protein (GST-hMDM2) in Escherichia coli. Residues 1-83 of human p53 were expressed as an amino-terminal AviTag™-TrxA-6×His fusion protein (biotinylated p53) in E. coli. Each protein was purified from cell paste by affinity chromatography.Specifically, 10 uL of GST-hMDM2 was incubated with 10 ul of diluted compound (various concentrations, serially diluted) in 10% DMSO for 20 minutes at room temperature. 20 uL of biotinylated-p53 was added to the GST-hMDM2+compound mixture, and then incubated at room temperature for 60 min. 10 uL of detection buffer consisting of SA-XLent, anti-GST cryptate antibody and KF was added to GST-hMDM2, biotinylated-p53 and compound reaction and left at room temperature to reach equilibrium for >4 hrs. The final concentration of DMSO in the reaction was 2%. Time-resolved fluorescence readings were measured on a microplate multilabel reader. Percentage of inhibition was calculated relative to nutlin-3. All assay conditions remained the same as described above, with the exception of the following changes in reagent concentrations: 0.2 nM GST-hMDM2 (1-188), 0.5 nM biotinylated-p53 (1-83), 0.18 nM SA-XLent, and 100 mM KF.	B	9	pIC50	1	nM	IC50	US-9593129-B2. Piperidinone derivatives as MDM2 inhibitors for the treatment of cancer (2017)
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 36:

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]