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Assay Detail

CHEMBL5164639

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

Binding
Inhibition of MDM2 (unknown origin)
5
Total Activities
5
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

Structure-Based Discovery of MDM2/4 Dual Inhibitors that Exert Antitumor Activities against MDM4-Overexpressing Cancer Cells.
Zhang S, Yan Z, Li Y, Gong Y, Lyu X, Lou J, Zhang D, Meng X, Zhao Y.
J Med Chem (2022) 65 : 6207 -6230
PubMed 35420431 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.10 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4091801 ALRIZOMADLIN 2.0 1 8.42
CHEMBL5196857 1 8.22
CHEMBL5206050 1 8.05
CHEMBL2402573 1 8.05
CHEMBL2386346 RO-5045337 1.0 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4091801 ALRIZOMADLIN IC50 = 3.8 nM 8.42
CHEMBL5196857 IC50 = 6.0 nM 8.22
CHEMBL5206050 IC50 = 9.0 nM 8.05
CHEMBL2402573 IC50 = 9.0 nM 8.05
CHEMBL2386346 RO-5045337 IC50 = 18.0 nM 7.75