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Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM135208
Substrate
n/a
Meas. Tech.
FRET Assay
IC50
1±n/a nM
Citation
 Christopher, MP; Fradera Llinas, FX; Machacek, M; Martinez, M; Reutershan, MH; Shizuka, M; Sun, B; Thompson, CF; Trotter, BW; Voss, ME; Altman, MD; Bogen, SL; Doll, RJ Substituted imidazopyridines as HDM2 inhibitors US Patent  US8846657 Publication Date 9/30/2014 
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:
Homo sapiens (Human)
Description:
Q00987
Residue:
491
Sequence:
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCNRCWALRENWLPEDKGKDKGEISEKAKLENSTQAEEGFDVPDCKKTIVNDSRESCVEENDDKITQASQSQESEDYSQPSTSSSIIYSSQEDVKEFEREETQDKEESVESSLPLNAIEPCVICQGRPKNGCIVHGKTGHLMACFTCAKKLKKRNKPCPVCRQPIQMIVLTYFP
  
Inhibitor
Name:
BDBM135208
Synonyms:
US8846657, 3.101
Type:
Small organic molecule
Emp. Form.:
C28H30ClN9O3
Mol. Mass.:
576.049
SMILES:
C[C@H]1CC[C@H](Cn2c(nc3cc(nc(-c4cncc(Cl)c4)c23)-c2noc(=O)[nH]2)N2CCCC2c2noc(C)n2)CC1 |r,wU:1.0,wD:4.4,(7.09,-4.45,;5.6,-4.05,;4.52,-5.14,;3.03,-4.74,;2.63,-3.25,;1.14,-2.86,;.74,-1.37,;1.65,-.12,;.74,1.12,;-.72,.65,;-2.05,1.42,;-3.39,.65,;-3.39,-.89,;-2.05,-1.66,;-2.05,-3.2,;-.72,-3.97,;-.72,-5.51,;-2.05,-6.28,;-3.39,-5.51,;-4.72,-6.28,;-3.39,-3.97,;-.72,-.89,;-4.72,1.42,;-6.19,.94,;-7.09,2.19,;-6.19,3.43,;-6.96,4.77,;-4.72,2.96,;3.19,-.12,;4.09,-1.37,;5.56,-.89,;5.56,.65,;4.09,1.12,;3.32,2.46,;1.86,2.93,;1.86,4.47,;3.32,4.95,;4.09,6.28,;4.23,3.7,;3.72,-2.17,;5.21,-2.56,)|
Structure:
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