Reaction Details |
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Target | Cellular tumor antigen p53 |
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Ligand | BDBM50229787 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_874346 (CHEMBL2182644) |
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IC50 | 7100±n/a nM |
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Citation | Rew, Y; Sun, D; Gonzalez-Lopez De Turiso, F; Bartberger, MD; Beck, HP; Canon, J; Chen, A; Chow, D; Deignan, J; Fox, BM; Gustin, D; Huang, X; Jiang, M; Jiao, X; Jin, L; Kayser, F; Kopecky, DJ; Li, Y; Lo, MC; Long, AM; Michelsen, K; Oliner, JD; Osgood, T; Ragains, M; Saiki, AY; Schneider, S; Toteva, M; Yakowec, P; Yan, X; Ye, Q; Yu, D; Zhao, X; Zhou, J; Medina, JC; Olson, SH Structure-based design of novel inhibitors of the MDM2-p53 interaction. J Med Chem55:4936-54 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Cellular tumor antigen p53 |
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Name: | Cellular tumor antigen p53 |
Synonyms: | Antigen NY-CO-13 | CREB-binding protein/p53 | GST-p53 | His6-p53 | P53 | P53_HUMAN | Phosphoprotein p53 | TP53 | Tumor Suppressor p53 |
Type: | fusion protein |
Mol. Mass.: | 43654.73 |
Organism: | Homo sapiens (Human) |
Description: | The full-length His6-wt-p53 expressed in E. coli was used in assays. |
Residue: | 393 |
Sequence: | MEEPQSDPSVEPPLSQETFSDLWKLLPENNVLSPLPSQAMDDLMLSPDDIEQWFTEDPGP
DEAPRMPEAAPPVAPAPAAPTPAAPAPAPSWPLSSSVPSQKTYQGSYGFRLGFLHSGTAK
SVTCTYSPALNKMFCQLAKTCPVQLWVDSTPPPGTRVRAMAIYKQSQHMTEVVRRCPHHE
RCSDSDGLAPPQHLIRVEGNLRVEYLDDRNTFRHSVVVPYEPPEVGSDCTTIHYNYMCNS
SCMGGMNRRPILTIITLEDSSGNLLGRNSFEVRVCACPGRDRRTEEENLRKKGEPHHELP
PGSTKRALPNNTSSSPQPKKKPLDGEYFTLQIRGRERFEMFRELNEALELKDAQAGKEPG
GSRAHSSHLKSKKGQSTSRHKKLMFKTEGPDSD
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BDBM50229787 |
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n/a |
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Name | BDBM50229787 |
Synonyms: | (4S,5R)-Nutlin-3 | (rac)-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazol-1-yl)(piperazin-1-yl)methanone | 4-((4S,5R)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one | 4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one | 4-[(4S,5R)-4,5-Bis-(4-chloro-phenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one | CHEMBL191334 | NUTLIN-3 | Nutlin-3a | rac-4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one |
Type | Small organic molecule |
Emp. Form. | C30H30Cl2N4O4 |
Mol. Mass. | 581.49 |
SMILES | COc1ccc(C2=N[C@H]([C@H](N2C(=O)N2CCNC(=O)C2)c2ccc(Cl)cc2)c2ccc(Cl)cc2)c(OC(C)C)c1 |t:6| |
Structure |
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