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Assay Detail

CHEMBL5164657

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

Functional
Cytotoxicity against human U2OS cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U2OS
Confidence 1 — Organism
Curated By Autocuration

Target

U2OS (CHEMBL615023)
Type CELL-LINE
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 6 6.09 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5181559 1 6.43
CHEMBL5205792 1 6.30
CHEMBL5196857 1 6.19
CHEMBL5176086 1 6.09
CHEMBL5188708 1 6.07
CHEMBL191334 NUTLIN-3 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5181559 IC50 = 370.0 nM 6.43
CHEMBL5205792 IC50 = 500.0 nM 6.30
CHEMBL5196857 IC50 = 640.0 nM 6.19
CHEMBL5176086 IC50 = 820.0 nM 6.09
CHEMBL5188708 IC50 = 860.0 nM 6.07
CHEMBL191334 NUTLIN-3 IC50 = 3350.0 nM 5.47