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Assay Detail

CHEMBL4352996

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of p53 protein binding to MDM2 (unknown origin)
10
Total Activities
10
Compounds Tested
2
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

The past, present and future of potential small-molecule drugs targeting p53-MDM2/MDMX for cancer therapy.
Liu Y, Wang X, Wang G, Yang Y, Yuan Y, Ouyang L.
Eur J Med Chem (2019) 176 : 92 -104
PubMed 31100649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.35 9.10
Ki 3 7.77 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4463050 1 9.22
CHEMBL4514512 1 9.10
CHEMBL4539285 1 8.96
CHEMBL4548050 1 8.92
CHEMBL2177813 1 7.47
CHEMBL2089208 1 7.05
CHEMBL2089203 1 7.04
CHEMBL2396744 1 6.31
CHEMBL208562 1 6.15
CHEMBL191334 NUTLIN-3 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4463050 Ki = 0.6 nM 9.22
CHEMBL4514512 IC50 = 0.8 nM 9.10
CHEMBL4539285 IC50 = 1.1 nM 8.96
CHEMBL4548050 IC50 = 1.2 nM 8.92
CHEMBL2177813 IC50 = 34.0 nM 7.47
CHEMBL2089208 Ki = 89.0 nM 7.05
CHEMBL2089203 Ki = 91.0 nM 7.04
CHEMBL2396744 IC50 = 490.0 nM 6.31
CHEMBL208562 IC50 = 704.0 nM 6.15
CHEMBL191334 NUTLIN-3 IC50 = 30000.0 nM 4.52