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Assay Detail

CHEMBL4619101

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

Binding
Modulation of human gamma secretase expressed in HEK293 cells assessed as reduction in total amyloid beta (1 to 42 residues) production
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of RO7185876, a Highly Potent γ-Secretase Modulator (GSM) as a Potential Treatment for Alzheimer's Disease.
Ratni H, Alker A, Bartels B, Bissantz C, Chen W, Gerlach I, Limberg A, Lu M, Neidhart W, Pichereau S, Reutlinger M, Rodriguez-Sarmiento RM, Jakob-Roetne R, Schmitt G, Zhang E, Baumann K.
ACS Med Chem Lett (2020) 11 : 1257 -1268
PubMed 32551009 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.61 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4644426 1 8.70
CHEMBL4645821 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4644426 IC50 = 2.0 nM 8.70
CHEMBL4645821 IC50 = 3.0 nM 8.52