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Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM135147
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:
BDBM135147
Synonyms:
US8846657, 3.39
Type:
Small organic molecule
Emp. Form.:
C25H27ClF3N5O2
Mol. Mass.:
521.962
SMILES:
C[C@H]1CC[C@H](Cn2c(nc3cc(nc(-c4cncc(Cl)c4)c23)C(O)=O)N2CCC[C@H]2C(F)(F)F)CC1 |r,wU:4.4,wD:1.0,29.33,(6.57,-3.2,;5.09,-2.81,;4.69,-1.32,;3.2,-.92,;2.11,-2.01,;.62,-1.61,;.23,-.12,;1.13,1.12,;.23,2.37,;-1.24,1.89,;-2.57,2.66,;-3.91,1.89,;-3.91,.35,;-2.57,-.42,;-2.57,-1.96,;-1.24,-2.73,;-1.24,-4.27,;-2.57,-5.04,;-3.91,-4.27,;-5.24,-5.04,;-3.91,-2.73,;-1.24,.35,;-5.24,2.66,;-6.57,1.89,;-5.24,4.2,;2.67,1.12,;3.58,-.12,;5.04,.35,;5.04,1.89,;3.58,2.37,;2.81,3.7,;3.58,5.04,;1.27,3.7,;2.04,5.04,;2.51,-3.5,;4,-3.89,)|
Structure:
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