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Assay Detail

CHEMBL5164642

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Binding
Inhibition of human MDM2 by TR-FRET assay
3
Total Activities
3
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 3 9.23 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3653256 SIREMADLIN 2.0 1 9.68
CHEMBL3601398 CGM-097 1.0 1 8.77
CHEMBL5180980 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3653256 SIREMADLIN IC50 = 0.21 nM 9.68
CHEMBL3601398 CGM-097 IC50 = 1.7 nM 8.77
CHEMBL5180980 IC50 < 0.1 nM -