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Assay Detail

CHEMBL4428341

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

Binding
Inhibition of gamma secretase isolated from human HeLa cell derived P2 membrane assessed as reduction in amyloid beta (1 to 40 residues) using recombinant human APP-C100 as substrate by DELFIA-based immunoassay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Gamma-secretase (CHEMBL2094135)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Notch Antagonists: Potential Modulators of Cancer and Inflammatory Diseases.
Kumar R, Juillerat-Jeanneret L, Golshayan D.
J Med Chem (2016) 59 : 7719 -7737
PubMed 27045975 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.21 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1770916 NIROGACESTAT 4.0 1 8.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1770916 NIROGACESTAT IC50 = 6.2 nM 8.21