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Assay Detail

CHEMBL869349

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Functional
Antiproliferative activity against wild type p53 MCF7 cell line
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.
Marugan JJ, Leonard K, Raboisson P, Gushue JM, Calvo R, Koblish HK, Lattanze J, Zhao S, Cummings MD, Player MR, Schubert C, Maroney AC, Lu T.
Bioorg Med Chem Lett (2006) 16 : 3115 -3120
PubMed 16630722 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.93 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL208562 1 6.10
CHEMBL210545 1 5.96
CHEMBL377203 1 5.89
CHEMBL207364 1 5.77
CHEMBL377614 1 -
CHEMBL425780 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL208562 IC50 = 800.0 nM 6.10
CHEMBL210545 IC50 = 1100.0 nM 5.96
CHEMBL377203 IC50 = 1300.0 nM 5.89
CHEMBL207364 IC50 = 1700.0 nM 5.77
CHEMBL377614 IC50 16000.0 nM -
CHEMBL425780 IC50 - -