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Assay Detail

CHEMBL3088771

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

Binding
Modulation of gamma-secretase in HEK293 cells expressing guinea pig Swedish mutant SFV-APP695sw coexpressing DLL4 assessed as inhibition of notch processing in human TE671 cells after 3 days by dual-cell luciferase reporter gene assay
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 2-methylpyridine-based biaryl amides as γ-secretase modulators for the treatment of Alzheimer's disease.
Chen JJ, Qian W, Biswas K, Yuan C, Amegadzie A, Liu Q, Nixey T, Zhu J, Ncube M, Rzasa RM, Chavez F, Chen N, DeMorin F, Rumfelt S, Tegley CM, Allen JR, Hitchcock S, Hungate R, Bartberger MD, Zalameda L, Liu Y, McCarter JD, Zhang J, Zhu L, Babu-Khan S, Luo Y, Bradley J, Wen PH, Reid DL, Koegler F, Dean C, Hickman D, Correll TL, Williamson T, Wood S.
Bioorg Med Chem Lett (2013) 23 : 6447 -6454
PubMed 24139583 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.43 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392068 1 5.92
CHEMBL3087342 1 4.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392068 IC50 = 1200.0 nM 5.92
CHEMBL3087342 IC50 = 11800.0 nM 4.93