Reaction Details Report a problem with these data
Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM31287
Substrate
Fl 9mer
Meas. Tech.
Fluorescent Peptide Displacement Assay
pH
7.5±n/a
Temperature
296.15±n/a K
IC50
810±n/a nM
Citation
Leonard, K; Marugan, JJ; Raboisson, P; Calvo, R; Gushue, JM; Koblish, HK; Lattanze, J; Zhao, S; Cummings, MD; Player, MR; Maroney, AC; Lu, T Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity. Bioorg Med Chem Lett 16:3463-8 (2006) [PubMed] Article
More Info.:
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:
BDBM31287
Synonyms:
1,4-benzodiazepine-2,5-dione scaffold, 52
Type:
Small organic molecule
Emp. Form.:
C27H24Cl2IN3O4
Mol. Mass.:
652.308
SMILES:
Nc1cc(Cl)ccc1CN1[C@@H](c2ccc(Cl)cc2)C(=O)N(CCCCC(O)=O)c2ccc(I)cc2C1=O |r|
Substrate
Name:
Fl 9mer
Synonyms:
n/a
Type:
fluorescent peptide
Mol. Mass.:
2263.48
Organism:
n/a
Description:
n/a
Residue:
18
Sequence:
FLRESCEINFMDYWEGLN