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Assay Detail

CHEMBL3603534

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

Binding
Inhibition of MDM2/p53 interaction (unknown origin) assessed as p53 nuclear translocation by GRIP p53 translocation assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Tumour suppressor p53/oncoprotein Mdm2 (CHEMBL1907611)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
Holzer P, Masuya K, Furet P, Kallen J, Valat-Stachyra T, Ferretti S, Berghausen J, Bouisset-Leonard M, Buschmann N, Pissot-Soldermann C, Rynn C, Ruetz S, Stutz S, Chène P, Jeay S, Gessier F.
J Med Chem (2015) 58 : 6348 -6358
PubMed 26181851 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.65 6.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3601398 CGM-097 1.0 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3601398 CGM-097 IC50 = 224.0 nM 6.65