Reaction Details |
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Target | E3 ubiquitin-protein ligase Mdm2 |
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Ligand | BDBM427147 |
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Substrate/Competitor | n/a |
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Meas. Tech. | MDM2-p53 Interaction Using a 96-Well Plate Binding Assay (ELISA) |
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IC50 | 0.790±n/a nM |
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Citation | Chessari, G; Howard, S; Buck, IM; Cons, BD; Johnson, CN; Holvey, RS; Rees, DC; St. Denis, JD; Tamanini, E; Golding, BT; Hardcastle, IR; Cano, CF; Miller, DC; Noble, ME; Griffin, RJ; Osborne, JD; Peach, J; Lewis, A; Hirst, KL; Whittaker, BP; Watson, DW; Mitchell, DR Isoindolinone inhibitors of the MDM2-p53 interaction having anticancer activity US Patent US10544132 Publication Date 1/28/2020 |
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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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BDBM427147 |
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n/a |
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Name | BDBM427147 |
Synonyms: | (3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[1-hydroxy-1-(oxan-4-yl)ethyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]propanoic Acid | US10544132, Example 88 | US10981898, Example 88 |
Type | Small organic molecule |
Emp. Form. | C31H30Cl2FNO6 |
Mol. Mass. | 602.477 |
SMILES | CO[C@]1(N([C@@H](CC(O)=O)c2ccc(Cl)cc2)C(=O)c2cc(cc(F)c12)[C@@](C)(O)C1CCOCC1)c1ccc(Cl)cc1 |r| |
Structure |
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