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Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM135117
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:
BDBM135117
Synonyms:
US8846657, 3.7
Type:
Small organic molecule
Emp. Form.:
C29H36ClN7O3
Mol. Mass.:
566.094
SMILES:
COC(C)(C)[C@@H]1CCCN1c1nc2cc(nc(-c3cncc(Cl)c3)c2n1C[C@H]1CC[C@H](C)CC1)-c1noc(=O)[nH]1 |r,wU:27.30,wD:30.34,5.4,(3.32,5.7,;4.09,4.37,;3.32,3.04,;1.99,2.27,;1.99,3.81,;4.09,1.7,;5.56,1.23,;5.56,-.31,;4.09,-.79,;3.19,.46,;1.65,.46,;.74,1.7,;-.72,1.23,;-2.05,2,;-3.39,1.23,;-3.39,-.31,;-2.05,-1.08,;-2.05,-2.62,;-.72,-3.39,;-.72,-4.93,;-2.05,-5.7,;-3.39,-4.93,;-4.72,-5.7,;-3.39,-3.39,;-.72,-.31,;.74,-.79,;1.14,-2.28,;2.63,-2.68,;3.72,-1.59,;5.21,-1.99,;5.6,-3.47,;7.09,-3.87,;4.52,-4.56,;3.03,-4.16,;-4.72,2,;-6.19,1.52,;-7.09,2.77,;-6.19,4.01,;-6.96,5.35,;-4.72,3.54,)|
Structure:
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