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Target
Cellular tumor antigen p53 [16-27]/E3 ubiquitin-protein ligase Mdm2 [23-117]
Ligand
BDBM374753
Substrate
n/a
Meas. Tech.
Mdm2-p53 Inhibition AlphaScreen
IC50
16.0±n/a nM
Citation
 Ramharter, J; Broeker, J; Gille, A; Gollner, A; Henry, M; Kerres, N; Weinstabl, H Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-p53 inhibitors US Patent  US10246467 Publication Date 4/2/2019 
Target
Name:
Cellular tumor antigen p53 [16-27]/E3 ubiquitin-protein ligase Mdm2 [23-117]
Synonyms:
MDM2/P53
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
E3 ubiquitin-protein ligase Mdm2 [23-117]
Synonyms:
E3 ubiquitin-protein ligase Mdm2 (23-117) | MDM2 | MDM2 (aa 23-117) | MDM2_HUMAN
Type:
Oncoprotein
Mol. Mass.:
11177.88
Organism:
Homo sapiens (Human)
Description:
Q00987[23-117]
Residue:
95
Sequence:
EQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSD
  
Component 2
Name:
Cellular tumor antigen p53 [16-27]
Synonyms:
P53 | P53 (aa 16-27) | P53_HUMAN | TP53
Type:
fusion protein
Mol. Mass.:
1475.66
Organism:
Homo sapiens (Human)
Description:
The full-length His6-wt-p53 expressed in E. coli was used in assays.
Residue:
12
Sequence:
QETFSDLWKLLP
  
Inhibitor
Name:
BDBM374753
Synonyms:
US10246467, Example I-36 | US10246467, Example I-37 | US10919913, # I-37
Type:
Small organic molecule
Emp. Form.:
C30H25Cl2FN4O4
Mol. Mass.:
595.448
SMILES:
CC(C)CN1[C@H]2COc3n(nc4cc(ccc34)C(O)=O)[C@H]2[C@H](c2cccc(Cl)c2F)[C@]11C(=O)Nc2cc(Cl)ccc12 |r|
Structure:
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