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TargetE3 ubiquitin-protein ligase Mdm2
LigandBDBM112767
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1661768 (CHEMBL4011380)
Ki 3.4±n/a nM
Citation Aguilar, ALu, JLiu, LDu, DBernard, DMcEachern, DPrzybranowski, SLi, XLuo, RWen, BSun, DWang, HWen, JWang, GZhai, YGuo, MYang, DWang, S Discovery of 4-((3'R,4'S,5'R)-6¿-Chloro-4'-(3-chloro-2-fluorophenyl)-1'-ethyl-2¿-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3¿-indoline]-5'-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Deve J Med Chem60:2819-2839 (2017) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
E3 ubiquitin-protein ligase Mdm2
Name:E3 ubiquitin-protein ligase Mdm2
Synonyms:Double minute 2 protein | Double minute 2 protein (HDM2) | E3 ubiquitin-protein ligase Mdm2 (p53-binding protein Mdm2) | Hdm2 | Human Double Minute 2 (HDM2) | MDM2 | MDM2-MDMX | MDM2_HUMAN | p53-Binding Protein MDM2 | p53-binding protein
Type:Oncoprotein
Mol. Mass.:55196.54
Organism:Homo sapiens (Human)
Description:Q00987
Residue:491
Sequence:
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQY
IMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGT
SVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQ
RKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDS
VSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLA
DYWKCTSCNEMNPPLPSHCNRCWALRENWLPEDKGKDKGEISEKAKLENSTQAEEGFDVP
DCKKTIVNDSRESCVEENDDKITQASQSQESEDYSQPSTSSSIIYSSQEDVKEFEREETQ
DKEESVESSLPLNAIEPCVICQGRPKNGCIVHGKTGHLMACFTCAKKLKKRNKPCPVCRQ
PIQMIVLTYFP
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  Blast E-value cutoff:
BDBM112767
n/a
NameBDBM112767
Synonyms:US8629141, 37
TypeSmall organic molecule
Emp. Form.C30H33Cl2FN4O4
Mol. Mass.603.512
SMILESOC(=O)CN1CCC(CC1)NC(=O)[C@@H]1NC2(CCCCC2)[C@]2([C@H]1c1cccc(Cl)c1F)C(=O)Nc1cc(Cl)ccc21 |r|
Structure
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