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Assay Detail

CHEMBL2383516

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Binding
Antagonist activity at human GST-tagged MDM2 assessed as inhibition of binding to full length p53
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

E3 ubiquitin-protein ligase Mdm2 (CHEMBL5023)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of the p53/hdm2 protein-protein interaction-path to the clinic.
Carry JC, Garcia-Echeverria C.
Bioorg Med Chem Lett (2013) 23 : 2480 -2485
PubMed 23541651 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.33 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405395 1 8.30
CHEMBL191334 NUTLIN-3 1 7.00
CHEMBL2381406 1 7.00
CHEMBL1818538 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405395 IC50 = 5.0 nM 8.30
CHEMBL191334 NUTLIN-3 IC50 = 100.0 nM 7.00
CHEMBL2381406 IC50 = 100.0 nM 7.00
CHEMBL1818538 IC50 = 100.0 nM 7.00