Reaction Details |
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Target | Cellular tumor antigen p53 [1-83]/E3 ubiquitin-protein ligase Mdm2 [1-188] |
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Ligand | BDBM427184 |
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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 | 1.90±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 US10981898 Publication Date 4/20/2021 |
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More Info.: | Get all data from this article, Assay Method |
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Cellular tumor antigen p53 [1-83]/E3 ubiquitin-protein ligase Mdm2 [1-188] |
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Name: | Cellular tumor antigen p53 [1-83]/E3 ubiquitin-protein ligase Mdm2 [1-188] |
Synonyms: | MDM2 and p53 | mdm2 |
Type: | Enzyme |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | E3 ubiquitin-protein ligase Mdm2 [1-188] |
Synonyms: | E3 ubiquitin-protein ligase Mdm2 (aa 1-188) | MDM2 | MDM2_HUMAN |
Type: | n/a |
Mol. Mass.: | 21319.18 |
Organism: | Homo sapiens (Human) |
Description: | Q00987[1-188] |
Residue: | 188 |
Sequence: | MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQY
IMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGT
SVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQ
RKRHKSDS
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Component 2 |
Name: | Cellular tumor antigen p53 [1-83] |
Synonyms: | P53 | P53_HUMAN | TP53 | Tumor suppressor p53 |
Type: | Enzyme |
Mol. Mass.: | 8975.74 |
Organism: | Homo sapiens (Human) |
Description: | Residues 1-83 |
Residue: | 83 |
Sequence: | MEEPQSDPSVEPPLSQETFSDLWKLLPENNVLSPLPSQAMDDLMLSPDDIEQWFTEDPGP
DEAPRMPEAAPPVAPAPAAPTPA
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BDBM427184 |
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n/a |
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Name | BDBM427184 |
Synonyms: | US10544132, Example 125 | US10981898, Example 126 |
Type | Small organic molecule |
Emp. Form. | C31H29Cl2F2NO6 |
Mol. Mass. | 620.468 |
SMILES | CC[C@](C)(O)c1cc2C(=O)N([C@@H](CC(O)=O)c3ccc(Cl)cc3)[C@](OCC3(F)COC3)(c2c(F)c1)c1ccc(Cl)cc1 |r| |
Structure |
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