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Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM135239
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:
BDBM135239
Synonyms:
US8846657, 3.132
Type:
Small organic molecule
Emp. Form.:
C29H36ClN7O3
Mol. Mass.:
566.094
SMILES:
CC(C)[C@@H]1C[C@](C)(O)CN1c1nc2cc(nc(-c3cncc(Cl)c3)c2n1C[C@H]1CC[C@H](C)CC1)-c1noc(=O)[nH]1 |r,wU:27.30,5.5,wD:30.34,5.6,3.2,(4.09,4.55,;3.32,3.21,;1.78,3.21,;4.09,1.88,;5.56,1.41,;5.56,-.13,;7.1,-.13,;6.33,-1.47,;4.09,-.61,;3.19,.64,;1.65,.64,;.74,1.88,;-.72,1.41,;-2.06,2.18,;-3.39,1.41,;-3.39,-.13,;-2.06,-.9,;-2.06,-2.44,;-.72,-3.21,;-.72,-4.75,;-2.06,-5.52,;-3.39,-4.75,;-4.73,-5.52,;-3.39,-3.21,;-.72,-.13,;.74,-.61,;.74,-2.15,;2.07,-2.92,;3.41,-2.15,;4.74,-2.92,;4.74,-4.46,;6.07,-5.23,;3.41,-5.23,;2.07,-4.46,;-4.73,2.18,;-6.19,1.7,;-7.1,2.95,;-6.19,4.19,;-6.96,5.52,;-4.73,3.72,)|
Structure:
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