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Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM31197
Substrate
PMDM6-F Peptide
Meas. Tech.
Fluorescence Polarization-Based (FP-Based) Binding Assay
pH
7.5±n/a
Temperature
296.15±n/a K
Ki
36±9 nM
Citation
 Lu, Y; Nikolovska-Coleska, Z; Fang, X; Gao, W; Shangary, S; Qiu, S; Qin, D; Wang, S Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy. J Med Chem 49:3759-62 (2006) [PubMed]  Article 
Target
Name:
E3 ubiquitin-protein ligase Mdm2
Synonyms:
Double minute 2 protein | Double minute 2 protein (HDM2) | E3 ubiquitin-protein ligase Mdm2 (p53-binding protein Mdm2) | Hdm2 | Human Double Minute 2 (HDM2) | MDM2 | MDM2-MDMX | MDM2_HUMAN | p53-Binding Protein MDM2 | p53-binding protein
Type:
Oncoprotein
Mol. Mass.:
55196.54
Organism:
Homo sapiens (Human)
Description:
Q00987
Residue:
491
Sequence:
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCNRCWALRENWLPEDKGKDKGEISEKAKLENSTQAEEGFDVPDCKKTIVNDSRESCVEENDDKITQASQSQESEDYSQPSTSSSIIYSSQEDVKEFEREETQDKEESVESSLPLNAIEPCVICQGRPKNGCIVHGKTGHLMACFTCAKKLKKRNKPCPVCRQPIQMIVLTYFP
  
Inhibitor
Name:
BDBM31197
Synonyms:
CHEMBL211045 | Nutlin-3 | med.21724, Compound 186
Type:
Small organic molecule
Emp. Form.:
C30H30Cl2N4O4
Mol. Mass.:
581.49
SMILES:
COc1ccc(C2=NC(C(N2C(=O)N2CCNC(=O)C2)c2ccc(Cl)cc2)c2ccc(Cl)cc2)c(OC(C)C)c1 |t:6|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PMDM6-F Peptide
Synonyms:
n/a
Type:
Fluorescence probe
Mol. Mass.:
4802.47
Organism:
n/a
Description:
n/a
Residue:
45
Sequence:
FAMETAALAETAALAPHEMETAIPTYRCLLTRPGLACCLEASNNH