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Assay Detail

CHEMBL1816004

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

Binding
Modulation of gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in amyloid beta40 production after 20 to 24 hrs by liquid phase electrochemiluminescence assay
13
Total Activities
13
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

NSAID-derived γ-secretase modulation requires an acidic moiety on the carbazole scaffold.
Zall A, Kieser D, Höttecke N, Naumann EC, Thomaszewski B, Schneider K, Steinbacher DT, Schubenel R, Masur S, Baumann K, Schmidt B.
Bioorg Med Chem (2011) 19 : 4903 -4909
PubMed 21763147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.32 4.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1812408 1 4.50
CHEMBL1812407 1 4.14
CHEMBL375635 1 -
CHEMBL247691 1 -
CHEMBL1812401 1 -
CHEMBL1812402 1 -
CHEMBL1812403 1 -
CHEMBL1812405 1 -
CHEMBL1812406 1 -
CHEMBL1812410 1 -
CHEMBL1812411 1 -
CHEMBL1812412 1 -
CHEMBL218756 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1812408 IC50 = 32000.0 nM 4.50
CHEMBL1812407 IC50 = 72000.0 nM 4.14
CHEMBL375635 IC50 > 40000.0 nM -
CHEMBL247691 IC50 > 40000.0 nM -
CHEMBL1812401 IC50 > 40000.0 nM -
CHEMBL1812402 IC50 = 105000.0 nM -
CHEMBL1812403 IC50 > 80000.0 nM -
CHEMBL1812405 IC50 > 80000.0 nM -
CHEMBL1812406 IC50 > 80000.0 nM -
CHEMBL1812410 IC50 = 102000.0 nM -
CHEMBL1812411 IC50 > 80000.0 nM -
CHEMBL1812412 IC50 > 40000.0 nM -
CHEMBL218756 IC50 > 40000.0 nM -