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Target
Cellular tumor antigen p53 [16-27]/E3 ubiquitin-protein ligase Mdm2 [23-117]
Ligand
BDBM374777
Substrate
n/a
Meas. Tech.
Mdm2-p53 Inhibition AlphaScreen
IC50
7.00±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:
BDBM374777
Synonyms:
US10246467, Example I-78 | US10919913, # I-80
Type:
Small organic molecule
Emp. Form.:
C29H22Cl2FN5O4
Mol. Mass.:
594.42
SMILES:
OC(=O)c1ccc2c3OC[C@H]4[C@H]([C@H](c5ccnc(Cl)c5F)[C@@]5(N4CC4CC4)C(=O)Nc4cc(Cl)ccc54)n3nc2c1 |r|
Structure:
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