Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM143590
Substrate
n/a
Meas. Tech.
Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay
IC50
0.241±n/a nM
Citation
 Furet, PGuagnano, VHolzer, PMah, RMasuya, KSchlapbach, AStutz, SVaupel, A Pyrazolopyrrolidine compounds US Patent  US8969341 Publication Date 3/3/2015 
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:
BDBM143590
Synonyms:
US8969341, 153
Type:
Small organic molecule
Emp. Form.:
C27H26Cl2N6O4
Mol. Mass.:
569.439
SMILES:
COc1ncc(c(OC)n1)-n1nc2C(=O)N([C@H](c2c1C(C)C)c1ccc(Cl)cc1C)c1cc(Cl)c(=O)n(C)c1 |r|
Structure:
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