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Assay Detail

CHEMBL3243052

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

Binding
Binding affinity to MDM2 in human SJSA1 cells assessed as upregulation of p21 mRNA expression after 7 hrs by qRT-PCR analysis in absence of human serum
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SJSA-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.
Gonzalez AZ, Eksterowicz J, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Duquette J, Fox BM, Fu J, Huang X, Houze JB, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, McMinn DL, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D.
J Med Chem (2014) 57 : 2472 -2488
PubMed 24548297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.18 7.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3125527 1 7.74
CHEMBL3233130 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3125527 IC50 = 18.4 nM 7.74
CHEMBL3233130 IC50 = 240.0 nM 6.62