Reaction Details
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E3 ubiquitin-protein ligase Mdm2 [1-188]
Ligand
BDBM299600
Substrate
n/a
Meas. Tech.
Homogenous Time-Resolved Fluorescence Assay (HTRF2 Assay)
IC50
0.200±n/a nM
Citation
Bartberger, MD; Gonzalez Buenrostro, A; Beck, HP; Chen, X; Connors, RV; Deignan, J; Duquette, JA; Eksterowicz, J; Fisher, B; Fox, BM; Fu, J; Fu, Z; Gonzalez Lopez De Turiso, F; Gribble, Jr., MW; Gustin, DJ; Heath, JA; Huang, X; Jiao, X; Johnson, MG; Kayser, F; Kopecky, DJ; Lai, S; Li, Y; Li, Z; Liu, J; Low, JD; Lucas, BS; Ma, Z; McGee, LR; McIntosh, J; McMinn, DL; Medina, JC; Mihalic, JT; Olson, SH; Rew, Y; Roveto, PM; Sun, D; Wang, X; Wang, Y; Yan, X; Yu, M; Zhu, J Piperidinone derivatives as MDM2 inhibitors for the treatment of cancer US Patent US9593129 Publication Date 3/14/2017 More Info.:
Target
Name:
E3 ubiquitin-protein ligase Mdm2 [1-188]
Synonyms:
E3 ubiquitin-protein ligase Mdm2 (aa 1-188) | MDM2 | MDM2_HUMAN
Type:
n/a
Mol. Mass.:
21319.18
Organism:
Homo sapiens (Human)
Description:
Q00987[1-188]
Residue:
188
Sequence:
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDS
Inhibitor
Name:
BDBM299600
Synonyms:
2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-2-(N-(2-cyanophenyl)methylsulfonamido)-1-cyclopropylethyl)-3-methyl-2-oxopiperidin-3-yl)acetic acid | US9593129, Example 278
Type:
Small organic molecule
Emp. Form.:
C33H33Cl2N3O5S
Mol. Mass.:
654.603
SMILES:
C[C@]1(CC(O)=O)C[C@@H](C(N([C@H](CN(c2ccccc2[N+]#[C-])S(C)(=O)=O)C2CC2)C1=O)c1ccc(Cl)cc1)c1cccc(Cl)c1 |r|
Structure:
