Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM427195
Substrate
n/a
Meas. Tech.
MDM2-p53 Interaction Using a 96-Well Plate Binding Assay (ELISA)
IC50
1.30±n/a nM
Citation
 Chessari, GHoward, SBuck, IMCons, BDJohnson, CNHolvey, RSRees, DCSt. Denis, JDTamanini, EGolding, BTHardcastle, IRCano, CFMiller, DCNoble, MEGriffin, RJOsborne, JDPeach, JLewis, AHirst, KLWhittaker, BPWatson, DWMitchell, DR Isoindolinone inhibitors of the MDM2-p53 interaction having anticancer activity US Patent  US10544132 Publication Date 1/28/2020 
Target
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:
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCNRCWALRENWLPEDKGKDKGEISEKAKLENSTQAEEGFDVPDCKKTIVNDSRESCVEENDDKITQASQSQESEDYSQPSTSSSIIYSSQEDVKEFEREETQDKEESVESSLPLNAIEPCVICQGRPKNGCIVHGKTGHLMACFTCAKKLKKRNKPCPVCRQPIQMIVLTYFP
  
Inhibitor
Name:
BDBM427195
Synonyms:
US10544132, Example 136 | US10981898, Example 137 | US11236047, Example 136
Type:
Small organic molecule
Emp. Form.:
C34H37Cl2FN2O5
Mol. Mass.:
643.572
SMILES:
CC[C@](O)(C1CCN(CCC(=O)OC)CC1)c1cc2C(=O)N(Cc3ccc(Cl)cc3)[C@](OC)(c2c(F)c1)c1ccc(Cl)cc1 |r|
Structure:
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