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Target
Cellular tumor antigen p53 [1-83]/E3 ubiquitin-protein ligase Mdm2 [1-188]
Ligand
BDBM427147
Substrate
n/a
Meas. Tech.
MDM2-p53 Interaction Using a 96-Well Plate Binding Assay (ELISA)
IC50
0.790±n/a nM
Citation
 Chessari, G; Howard, S; Buck, IM; Cons, BD; Johnson, CN; Holvey, RS; Rees, DC; St. Denis, JD; Tamanini, E; Golding, BT; Hardcastle, IR; Cano, CF; Miller, DC; Noble, ME; Griffin, RJ; Osborne, JD; Peach, J; Lewis, A; Hirst, KL; Whittaker, BP; Watson, DW; Mitchell, DR Isoindolinone inhibitors of the MDM2-p53 interaction having anticancer activity US Patent  US10981898 Publication Date 4/20/2021
Target
Name:
Cellular tumor antigen p53 [1-83]/E3 ubiquitin-protein ligase Mdm2 [1-188]
Synonyms:
MDM2 and p53 | mdm2
Type:
Enzyme
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
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
  
Component 2
Name:
Cellular tumor antigen p53 [1-83]
Synonyms:
P53 | P53_HUMAN | TP53 | Tumor suppressor p53
Type:
Enzyme
Mol. Mass.:
8975.74
Organism:
Homo sapiens (Human)
Description:
Residues 1-83
Residue:
83
Sequence:
MEEPQSDPSVEPPLSQETFSDLWKLLPENNVLSPLPSQAMDDLMLSPDDIEQWFTEDPGPDEAPRMPEAAPPVAPAPAAPTPA
  
Inhibitor
Name:
BDBM427147
Synonyms:
(3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[1-hydroxy-1-(oxan-4-yl)ethyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]propanoic Acid | US10544132, Example 88 | US10981898, Example 88
Type:
Small organic molecule
Emp. Form.:
C31H30Cl2FNO6
Mol. Mass.:
602.477
SMILES:
CO[C@]1(N([C@@H](CC(O)=O)c2ccc(Cl)cc2)C(=O)c2cc(cc(F)c12)[C@@](C)(O)C1CCOCC1)c1ccc(Cl)cc1 |r|
Structure:
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