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Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM148144
Substrate
n/a
Meas. Tech.
FRET Assay
IC50
7±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  US8962611 Publication Date 2/24/2015 
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:
BDBM148144
Synonyms:
US8962611, 3.97
Type:
Small organic molecule
Emp. Form.:
C29H35ClN8O3
Mol. Mass.:
579.093
SMILES:
CCN(C)C(=O)[C@@H]1CCCN1c1nc2cc(nc(-c3cncc(Cl)c3)c2n1C[C@H]1CC[C@H](C)CC1)-c1noc(=O)[nH]1 |r,wU:31.35,wD:6.5,28.31,(7.23,4.94,;6.14,3.85,;4.65,4.25,;4.25,5.73,;3.56,3.16,;2.07,3.56,;3.96,1.67,;5.42,1.2,;5.42,-.34,;3.96,-.82,;3.05,.43,;1.51,.43,;.61,1.67,;-.86,1.2,;-2.19,1.97,;-3.52,1.2,;-3.52,-.34,;-2.19,-1.11,;-2.19,-2.65,;-.86,-3.42,;-.86,-4.96,;-2.19,-5.73,;-3.52,-4.96,;-4.86,-5.73,;-3.52,-3.42,;-.86,-.34,;.61,-.82,;1.01,-2.31,;2.5,-2.71,;2.89,-4.19,;4.38,-4.59,;5.47,-3.5,;6.96,-3.9,;5.07,-2.02,;3.58,-1.62,;-4.86,1.97,;-6.32,1.49,;-7.23,2.74,;-6.32,3.98,;-7.09,5.31,;-4.86,3.51,)|
Structure:
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