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 | BDBM50448934 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Homogenous Time-Resolved Fluorescence Assay (HTRF2 Assay) |
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pH | 7.4±n/a |
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Temperature | 298.15±n/a K |
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IC50 | 0.2±n/a nM |
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Comments | extracted |
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Citation | Bartberger, MD; Gonzalez Buenrostro, A; Beck, HP; Chen, X; Connors, RV; Deignan, J; Duquette, JA; Eksterowicz, J; Fisher, B; Fox, BM; Fu, J; Fu, Z; Gonzalez Lopez De Turiso, F; Gribble, MW; Gustin, DJ; Heath, JA; Huang, X; Jiao, X; Johnson, MG; Kayser, F; Kopecky, DJ; Lai, S; Li, Y; Li, Z; Liu, J; Low, JD; Lucas, BS; Ma, Z; McGee, LR; McIntosh, J; McMinn, DL; Medina, JC; Mihalic, JT; Olson, SH; Rew, Y; Roveto, PM; Sun, D; Wang, X; Wang, Y; Yan, X; Yu, M; Zhu, J Piperidinone derivatives as MDM2 inhibitors for the treatment of cancer US Patent US9296736 Publication Date 3/29/2016 |
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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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BDBM50448934 |
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n/a |
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Name | BDBM50448934 |
Synonyms: | CHEMBL3125529 | US9296736, 343 | US9593129, Example 343 |
Type | Small organic molecule |
Emp. Form. | C28H33Cl2NO5S |
Mol. Mass. | 566.536 |
SMILES | CC[C@@H](CS(=O)(=O)C1CCC1)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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