Reaction Details 
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E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM50448963
Substrate
n/a
Meas. Tech.
ChEMBL_1296787 (CHEMBL3132470)
IC50
0.100000±n/a nM
Citation
Sun, D; Li, Z; Rew, Y; Gribble, M; Bartberger, MD; Beck, HP; Canon, J; Chen, A; Chen, X; Chow, D; Deignan, J; Duquette, J; Eksterowicz, J; Fisher, B; Fox, BM; Fu, J; Gonzalez, AZ; Gonzalez-Lopez De Turiso, F; Houze, JB; Huang, X; Jiang, M; Jin, L; Kayser, F; Liu, JJ; Lo, MC; Long, AM; Lucas, B; McGee, LR; McIntosh, J; Mihalic, J; Oliner, JD; Osgood, T; Peterson, ML; Roveto, P; Saiki, AY; Shaffer, P; Toteva, M; Wang, Y; Wang, YC; Wortman, S; Yakowec, P; Yan, X; Ye, Q; Yu, D; Yu, M; Zhao, X; Zhou, J; Zhu, J; Olson, SH; Medina, JC Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development. J Med Chem 57:1454-72 (2014) [PubMed] ArticleMore 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:
BDBM50448963
Synonyms:
CHEMBL3125537 | US9296736, 351 | US9593129, Example 351
Type:
Small organic molecule
Emp. Form.:
C29H35Cl2NO5S
Mol. Mass.:
580.563
SMILES:
CC(C)(C)S(=O)(=O)C[C@H](C1CC1)N1[C@@H]([C@H](C[C@](C)(CC(O)=O)C1=O)c1cccc(Cl)c1)c1ccc(Cl)cc1 |r|
Structure:
