Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2156544

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

Binding
Inhibition of MDM2 binding to p53
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of novel dihydroimidazothiazole derivatives as p53-MDM2 protein-protein interaction inhibitors: synthesis, biological evaluation and structure-activity relationships.
Miyazaki M, Kawato H, Naito H, Ikeda M, Miyazaki M, Kitagawa M, Seki T, Fukutake S, Aonuma M, Soga T.
Bioorg Med Chem Lett (2012) 22 : 6338 -6342
PubMed 22995624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.26 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191334 NUTLIN-3 1 7.05
CHEMBL407632 NUTLIN-2 1 6.85
CHEMBL2152332 1 4.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191334 NUTLIN-3 IC50 = 90.0 nM 7.05
CHEMBL407632 NUTLIN-2 IC50 = 140.0 nM 6.85
CHEMBL2152332 IC50 = 13600.0 nM 4.87