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Assay Detail

CHEMBL902178

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

Binding
Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-40 formation LPECL assay
16
Total Activities
16
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

N-Substituted carbazolyloxyacetic acids modulate Alzheimer associated gamma-secretase.
Narlawar R, Pérez Revuelta BI, Baumann K, Schubenel R, Haass C, Steiner H, Schmidt B.
Bioorg Med Chem Lett (2007) 17 : 176 -182
PubMed 17035010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.56 4.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392028 1 4.72
CHEMBL248090 1 4.40
CHEMBL248089 1 -
CHEMBL385554 1 -
CHEMBL218756 1 -
CHEMBL247894 1 -
CHEMBL247693 1 -
CHEMBL247692 1 -
CHEMBL247691 1 -
CHEMBL392639 1 -
CHEMBL247492 1 -
CHEMBL396693 1 -
CHEMBL247491 1 -
CHEMBL247490 1 -
CHEMBL396692 1 -
CHEMBL438846 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392028 IC50 = 19000.0 nM 4.72
CHEMBL248090 IC50 = 40000.0 nM 4.40
CHEMBL248089 IC50 > 40000.0 nM -
CHEMBL385554 IC50 > 20000.0 nM -
CHEMBL218756 IC50 > 40000.0 nM -
CHEMBL247894 IC50 > 40000.0 nM -
CHEMBL247693 IC50 > 40000.0 nM -
CHEMBL247692 IC50 > 40000.0 nM -
CHEMBL247691 IC50 > 40000.0 nM -
CHEMBL392639 IC50 > 40000.0 nM -
CHEMBL247492 IC50 > 40000.0 nM -
CHEMBL396693 IC50 > 40000.0 nM -
CHEMBL247491 IC50 > 40000.0 nM -
CHEMBL247490 IC50 > 40000.0 nM -
CHEMBL396692 IC50 > 40000.0 nM -
CHEMBL438846 IC50 > 40000.0 nM -