Reaction Details |
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Target | Cellular tumor antigen p53 [16-27]/E3 ubiquitin-protein ligase Mdm2 [23-117] |
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Ligand | BDBM374781 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Mdm2-p53 Inhibition AlphaScreen |
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IC50 | 35.0±n/a nM |
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Citation | Ramharter, J; Broeker, J; Gille, A; Gollner, A; Henry, M; Kerres, N; Weinstabl, H Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-p53 inhibitors US Patent US10246467 Publication Date 4/2/2019 |
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More Info.: | Get all data from this article, Assay Method |
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Cellular tumor antigen p53 [16-27]/E3 ubiquitin-protein ligase Mdm2 [23-117] |
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Name: | Cellular tumor antigen p53 [16-27]/E3 ubiquitin-protein ligase Mdm2 [23-117] |
Synonyms: | MDM2/P53 |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | E3 ubiquitin-protein ligase Mdm2 [23-117] |
Synonyms: | E3 ubiquitin-protein ligase Mdm2 (23-117) | MDM2 | MDM2 (aa 23-117) | MDM2_HUMAN |
Type: | Oncoprotein |
Mol. Mass.: | 11177.88 |
Organism: | Homo sapiens (Human) |
Description: | Q00987[23-117] |
Residue: | 95 |
Sequence: | EQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLL
GDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSD
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Component 2 |
Name: | Cellular tumor antigen p53 [16-27] |
Synonyms: | P53 | P53 (aa 16-27) | P53_HUMAN | TP53 |
Type: | fusion protein |
Mol. Mass.: | 1475.66 |
Organism: | Homo sapiens (Human) |
Description: | The full-length His6-wt-p53 expressed in E. coli was used in assays. |
Residue: | 12 |
Sequence: | |
BDBM374781 |
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n/a |
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Name | BDBM374781 |
Synonyms: | US10246467, Example I-86 | US10919913, # I-86 |
Type | Small organic molecule |
Emp. Form. | C31H25Cl2FN4O4 |
Mol. Mass. | 607.459 |
SMILES | OC(=O)c1ccc2c3OCC[C@H]4[C@H]([C@H](c5cccc(Cl)c5F)[C@@]5(N4CC4CC4)C(=O)Nc4cc(Cl)ccc54)n3nc2c1 |r| |
Structure |
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