Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM135918
Substrate
n/a
Meas. Tech.
Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay
IC50
386±n/a nM
Citation
 Furet, PGuagnano, VHolzer, PKallen, JMasuya, KStutz, S Cyclohexyl isoquinolinone compounds US Patent  US8859586 Publication Date 10/14/2014 
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:
Human
Description:
Q00987
Residue:
491
Sequence:
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCNRCWALRENWLPEDKGKDKGEISEKAKLENSTQAEEGFDVPDCKKTIVNDSRESCVEENDDKITQASQSQESEDYSQPSTSSSIIYSSQEDVKEFEREETQDKEESVESSLPLNAIEPCVICQGRPKNGCIVHGKTGHLMACFTCAKKLKKRNKPCPVCRQPIQMIVLTYFP
  
Inhibitor
Name:
BDBM135918
Synonyms:
US8859586, 2
Type:
Small organic molecule
Emp. Form.:
C28H35ClN2O4
Mol. Mass.:
499.041
SMILES:
COc1cc2CC(=O)N(C3CCC(CC3)N(C)C(C)=O)C(c3ccc(Cl)cc3)c2cc1OC(C)C |(-4,-.77,;-2.67,,;-1.33,-.77,;;1.33,-.77,;2.67,,;4,-.77,;5.33,,;4,-2.31,;5.33,-3.08,;5.33,-4.62,;6.67,-5.39,;8,-4.62,;8,-3.08,;6.67,-2.31,;9.34,-5.39,;9.34,-6.93,;10.67,-4.62,;12,-5.39,;10.67,-3.08,;2.67,-3.08,;2.67,-4.62,;4,-5.39,;4,-6.93,;2.67,-7.7,;2.67,-9.24,;1.33,-6.93,;1.33,-5.39,;1.33,-2.31,;,-3.08,;-1.33,-2.31,;-2.67,-3.08,;-2.67,-4.62,;-1.33,-5.39,;-4,-5.39,)|
Structure:
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