Reaction Details |
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Target | E3 ubiquitin-protein ligase Mdm2 |
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Ligand | BDBM50448959 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1296787 (CHEMBL3132470) |
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IC50 | 0.200000±n/a nM |
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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 Chem57:1454-72 (2014) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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E3 ubiquitin-protein ligase Mdm2 |
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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: | MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQY
IMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGT
SVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQ
RKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDS
VSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLA
DYWKCTSCNEMNPPLPSHCNRCWALRENWLPEDKGKDKGEISEKAKLENSTQAEEGFDVP
DCKKTIVNDSRESCVEENDDKITQASQSQESEDYSQPSTSSSIIYSSQEDVKEFEREETQ
DKEESVESSLPLNAIEPCVICQGRPKNGCIVHGKTGHLMACFTCAKKLKKRNKPCPVCRQ
PIQMIVLTYFP
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BDBM50448959 |
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n/a |
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Name | BDBM50448959 |
Synonyms: | CHEMBL3125697 | US9296736, 350 | US9593129, Example 350 |
Type | Small organic molecule |
Emp. Form. | C28H33Cl2NO5S |
Mol. Mass. | 566.536 |
SMILES | CC(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 |
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