Target
Cellular tumor antigen p53 [1-83]/E3 ubiquitin-protein ligase Mdm2 [1-188]
Ligand
BDBM427124
Substrate
n/a
Meas. Tech.
MDM2-p53 Interaction Using a 96-Well Plate Binding Assay (ELISA)
IC50
2.00±n/a nM
Citation
 Chessari, GHoward, SBuck, IMCons, BDJohnson, CNHolvey, RSRees, DCSt. Denis, JDTamanini, EGolding, BTHardcastle, IRCano, CFMiller, DCNoble, MEGriffin, RJOsborne, JDPeach, JLewis, AHirst, KLWhittaker, BPWatson, DWMitchell, 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:
BDBM427124
Synonyms:
US10544132, Example 71 | US10981898, Example 71 | US11236047, Example 71 | US20230338337, Example 71
Type:
Small organic molecule
Emp. Form.:
C30H28Cl2FNO6
Mol. Mass.:
588.451
SMILES:
CC(C)(O)c1cc2C(=O)N([C@@H](CC(O)=O)c3ccc(Cl)cc3)[C@](O[C@H]3CCOC3)(c2c(F)c1)c1ccc(Cl)cc1 |r|
Structure:
Search PDB for entries with ligand similarity: