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Assay Detail

CHEMBL3602307

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Binding
Inhibition of human MDM2 by TR-FRET assay
2
Total Activities
2
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

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
Ki 2 8.54 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3601398 CGM-097 1.0 1 8.89
CHEMBL191334 NUTLIN-3 1 8.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3601398 CGM-097 Ki = 1.3 nM 8.89
CHEMBL191334 NUTLIN-3 Ki = 6.4 nM 8.19