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Assay Detail

CHEMBL853214

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

ADMET
Brain concentration for reduction of DEA-extractable brain beta amyloid in orally dosed APP-YAC mouse after 4 hrs relative to control
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Mus musculus
Confidence 1 — Organism
Curated By Intermediate

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

3,4-Fused cyclohexyl sulfones as gamma-secretase inhibitors.
Shaw D, Best J, Dinnell K, Nadin A, Shearman M, Pattison C, Peachey J, Reilly M, Williams B, Wrigley J, Harrison T.
Bioorg Med Chem Lett (2006) 16 : 3073 -3077
PubMed 16617016 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.08 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL209888 1 7.70
CHEMBL377691 1 7.06
CHEMBL377264 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL209888 EC50 = 20.0 nM 7.70
CHEMBL377691 EC50 = 88.0 nM 7.06
CHEMBL377264 EC50 = 327.0 nM 6.49