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Assay Detail

CHEMBL940879

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Binding
Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in Amyloid beta38 formation by LPECL assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type H4
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Conversion of the LXR-agonist TO-901317--from inverse to normal modulation of gamma-secretase by addition of a carboxylic acid and a lipophilic anchor.
Narlawar R, Baumann K, Czech C, Schmidt B.
Bioorg Med Chem Lett (2007) 17 : 5428 -5431
PubMed 17723298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 5.00 5.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL218756 1 5.24
CHEMBL392028 1 5.11
CHEMBL385554 1 5.03
CHEMBL249202 1 4.62
CHEMBL247693 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL218756 EC50 = 5800.0 nM 5.24
CHEMBL392028 EC50 = 7800.0 nM 5.11
CHEMBL385554 EC50 = 9300.0 nM 5.03
CHEMBL249202 EC50 = 23700.0 nM 4.62
CHEMBL247693 EC50 - -