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TargetE3 ubiquitin-protein ligase Mdm2
LigandBDBM50229787
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1509562 (CHEMBL3602309)
Ki 20±n/a nM
Citation Holzer, PMasuya, KFuret, PKallen, JValat-Stachyra, TFerretti, SBerghausen, JBouisset-Leonard, MBuschmann, NPissot-Soldermann, CRynn, CRuetz, SStutz, SChène, PJeay, SGessier, 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
More Info.:Get all data from this article,  Assay Method
 
E3 ubiquitin-protein ligase Mdm2
Name:E3 ubiquitin-protein ligase Mdm2
Synonyms:6.3.2.- | Double minute 2 protein | E3 ubiquitin-protein ligase Mdm2 | MDM2_MOUSE | Mdm2 | Oncoprotein Mdm2 | p53-binding protein Mdm2
Type:PROTEIN
Mol. Mass.:54524.71
Organism:Mus musculus
Description:ChEMBL_109855
Residue:489
Sequence:
MCNTNMSVSTEGAASTSQIPASEQETLVRPKPLLLKLLKSVGAQNDTYTMKEIIFYIGQY
IMTKRLYDEKQQHIVYCSNDLLGDVFGVPSFSVKEHRKIYAMIYRNLVAVSQQDSGTSLS
ESRRQPEGGSDLKDPLQAPPEEKPSSSDLISRLSTSSRRRSISETEENTDELPGERHRKR
RRSLSFDPSLGLCELREMCSGGSSSSSSSSSESTETPSHQDLDDGVSEHSGDCLDQDSVS
DQFSVEFEVESLDSEDYSLSDEGHELSDEDDEVYRVTVYQTGESDTDSFEGDPEISLADY
WKCTSCNEMNPPLPSHCKRCWTLRENWLPDDKGKDKVEISEKAKLENSAQAEEGLDVPDG
KKLTENDAKEPCAEEDSEEKAEQTPLSQESDDYSQPSTSSSIVYSSQESVKELKEETQDK
DESVESSFSLNAIEPCVICQGRPKNGCIVHGKTGHLMSCFTCAKKLKKRNKPCPVCRQPI
QMIVLTYFN
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  Blast E-value cutoff:
BDBM50229787
n/a
NameBDBM50229787
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
TypeSmall organic molecule
Emp. Form.C30H30Cl2N4O4
Mol. Mass.581.49
SMILESCOc1ccc(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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