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Assay Detail

CHEMBL4019946

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

Binding
Inhibition of MDM2 in human U87MG cells assessed as reduction in MDM2 interaction with p53 after 10 mins by quantitative sandwich immune-enzymatic assay
15
Total Activities
15
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

Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
Giustiniano M, Daniele S, Pelliccia S, La Pietra V, Pietrobono D, Brancaccio D, Cosconati S, Messere A, Giuntini S, Cerofolini L, Fragai M, Luchinat C, Taliani S, La Regina G, Da Settimo F, Silvestri R, Martini C, Novellino E, Marinelli L.
J Med Chem (2017) 60 : 8115 -8130
PubMed 28921985 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.46 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4095983 1 8.11
CHEMBL4064911 1 8.04
CHEMBL4102803 1 8.02
CHEMBL4100348 1 7.86
CHEMBL4080951 1 7.72
CHEMBL4084848 1 7.63
CHEMBL4105199 1 7.45
CHEMBL4074577 1 7.37
CHEMBL4073512 1 7.30
CHEMBL4095042 1 7.18
CHEMBL4065471 1 7.03
CHEMBL2152332 1 6.97
CHEMBL4092607 1 6.94
CHEMBL4068667 1 6.85
CHEMBL3347643 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4095983 IC50 = 7.85 nM 8.11
CHEMBL4064911 IC50 = 9.2 nM 8.04
CHEMBL4102803 IC50 = 9.6 nM 8.02
CHEMBL4100348 IC50 = 13.8 nM 7.86
CHEMBL4080951 IC50 = 18.9 nM 7.72
CHEMBL4084848 IC50 = 23.4 nM 7.63
CHEMBL4105199 IC50 = 35.4 nM 7.45
CHEMBL4074577 IC50 = 43.0 nM 7.37
CHEMBL4073512 IC50 = 50.3 nM 7.30
CHEMBL4095042 IC50 = 65.3 nM 7.18
CHEMBL4065471 IC50 = 93.7 nM 7.03
CHEMBL2152332 IC50 = 108.0 nM 6.97
CHEMBL4092607 IC50 = 115.0 nM 6.94
CHEMBL4068667 IC50 = 141.5 nM 6.85
CHEMBL3347643 IC50 > 1000.0 nM -