| Reaction Details |
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 | Report a problem with these data |
| Target | Protein Mdm4 |
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| Ligand | BDBM50229787 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1509591 (CHEMBL3603474) |
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| IC50 | 4300±n/a nM |
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| Citation |  Holzer, P; Masuya, K; Furet, P; Kallen, J; Valat-Stachyra, T; Ferretti, S; Berghausen, J; Bouisset-Leonard, M; Buschmann, N; Pissot-Soldermann, C; Rynn, C; Ruetz, S; Stutz, S; Chène, P; Jeay, S; Gessier, F Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. J Med Chem58:6348-58 (2015) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Protein Mdm4 |
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| Name: | Protein Mdm4 |
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| Synonyms: | Double minute 4 protein | Double minute 4 protein (HDM4) | MDM2-MDMX | MDM4 | MDM4_HUMAN | MDMX | Mdm2-like p53-binding protein | Protein Mdm4 | Protein Mdmx | p53-Binding Protein HDMX | p53-binding protein | p53-binding protein Mdm4 |
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| Type: | Oncoprotein |
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| Mol. Mass.: | 54842.04 |
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| Organism: | Homo sapiens (Human) |
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| Description: | The HDMX(1-188) were expressed in Escherichia coli BL21 (DE3) as a GST fusion and purified on glutathione sepharose. |
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| Residue: | 490 |
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| Sequence: | MTSFSTSAQCSTSDSACRISPGQINQVRPKLPLLKILHAAGAQGEMFTVKEVMHYLGQYI
MVKQLYDQQEQHMVYCGGDLLGELLGRQSFSVKDPSPLYDMLRKNLVTLATATTDAAQTL
ALAQDHSMDIPSQDQLKQSAEESSTSRKRTTEDDIPTLPTSEHKCIHSREDEDLIENLAQ
DETSRLDLGFEEWDVAGLPWWFLGNLRSNYTPRSNGSTDLQTNQDVGTAIVSDTTDDLWF
LNESVSEQLGVGIKVEAADTEQTSEEVGKVSDKKVIEVGKNDDLEDSKSLSDDTDVEVTS
EDEWQCTECKKFNSPSKRYCFRCWALRKDWYSDCSKLTHSLSTSDITAIPEKENEGNDVP
DCRRTISAPVVRPKDAYIKKENSKLFDPCNSVEFLDLAHSSESQETISSMGEQLDNLSEQ
RTDTENMEDCQNLLKPCSLCEKRPRDGNIIHGRTGHLVTCFHCARRLKKAGASCPICKKE
IQLVIKVFIA
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| BDBM50229787 |
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| n/a |
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| Name | BDBM50229787 |
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| 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 |
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| Type | Small organic molecule |
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| Emp. Form. | C30H30Cl2N4O4 |
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| Mol. Mass. | 581.49 |
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| 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| |
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| Structure | 
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