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Assay Detail

CHEMBL4667905

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

Binding
Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cells cotransfected with Notch1-VP16-GAL4 fusion and Gal4 luciferase reporter plasmid incubated for 24 hrs by luciferase reporter gene assay luminescence assay
13
Total Activities
13
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 Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Velcicky J,Mathison CJN,Nikulin V,Pflieger D,Epple R,Azimioara M,Cow C,Michellys PY,Rigollier P,Beisner DR,Bodendorf U,Guerini D,Liu B,Wen B,Zaharevitz S,Brandl T
ACS Med Chem Lett (2019) 10 : 887 -892
PubMed 31223443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.47 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4759048 1 5.89
CHEMBL4753654 1 5.75
CHEMBL4792187 1 5.68
CHEMBL4789381 1 5.47
CHEMBL4762492 1 5.43
CHEMBL4759943 1 5.43
CHEMBL4762370 1 5.32
CHEMBL4740837 1 5.29
CHEMBL4747630 1 5.23
CHEMBL4753079 1 5.19
CHEMBL4798232 1 -
CHEMBL4741014 1 -
CHEMBL4785324 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4759048 IC50 = 1300.0 nM 5.89
CHEMBL4753654 IC50 = 1800.0 nM 5.75
CHEMBL4792187 IC50 = 2100.0 nM 5.68
CHEMBL4789381 IC50 = 3400.0 nM 5.47
CHEMBL4762492 IC50 = 3700.0 nM 5.43
CHEMBL4759943 IC50 = 3700.0 nM 5.43
CHEMBL4762370 IC50 = 4800.0 nM 5.32
CHEMBL4740837 IC50 = 5100.0 nM 5.29
CHEMBL4747630 IC50 = 5900.0 nM 5.23
CHEMBL4753079 IC50 = 6400.0 nM 5.19
CHEMBL4798232 IC50 > 10000.0 nM -
CHEMBL4741014 IC50 > 10000.0 nM -
CHEMBL4785324 IC50 > 10000.0 nM -