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Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM129796
Substrate
n/a
Meas. Tech.
Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay
IC50
0.07±n/a nM
Citation
 Furet, P; Guagnano, V; Holzer, P; Kallen, J; Liao, L; Mah, R; Mao, L; Masuya, K; Schlapbach, A; Stutz, S; Vaupel, A Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases US Patent  US8815926 Publication Date 8/26/2014 
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:
BDBM129796
Synonyms:
US8815926, 75
Type:
Small organic molecule
Emp. Form.:
C28H27Cl2N5O3
Mol. Mass.:
552.452
SMILES:
COc1ncc(-c2nc3C(=O)N([C@H](c3n2C(C)C)c2ccc(Cl)cc2C)c2cc(Cl)ccc2C)c(OC)n1 |r|
Structure:
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