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Assay Detail

CHEMBL3398676

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

Binding
Activation of wild-type human presenilin-1 stably overexpressed in CHO cells co-expressing wild-type human amyloid precursor protein assessed as amyloid beta 38 formation after 24 hrs by ELISA
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Presenilin-1 (CHEMBL2473)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR-studies of γ-secretase modulators with PPARγ-agonistic and 5-lipoxygenase-inhibitory activity for Alzheimer's disease.
Flesch D, Ness J, Lamers C, Dehm F, Popella S, Steri R, Ogorek I, Hieke M, Dannhardt G, Werz O, Weggen S, Schubert-Zsilavecz M.
Bioorg Med Chem Lett (2015) 25 : 841 -846
PubMed 25575659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 5.41 6.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3397724 1 6.01
CHEMBL3397717 1 6.00
CHEMBL3397727 1 5.96
CHEMBL1819479 1 5.96
CHEMBL3397721 1 5.93
CHEMBL3397728 1 5.89
CHEMBL3397714 1 5.75
CHEMBL3397719 1 5.68
CHEMBL3397722 1 5.66
CHEMBL3397711 1 5.60
CHEMBL3397716 1 5.50
CHEMBL3397713 1 5.50
CHEMBL3397712 1 5.36
CHEMBL3397723 1 5.35
CHEMBL1171834 1 5.34
CHEMBL3397720 1 4.97
CHEMBL461883 1 4.95
CHEMBL3397726 1 4.95
CHEMBL3397708 1 4.92
CHEMBL3397715 1 4.86
CHEMBL3397710 1 4.85
CHEMBL3397709 1 4.81
CHEMBL3397718 1 4.63
CHEMBL3397725 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3397724 EC50 = 970.0 nM 6.01
CHEMBL3397717 EC50 = 1000.0 nM 6.00
CHEMBL3397727 EC50 = 1100.0 nM 5.96
CHEMBL1819479 EC50 = 1100.0 nM 5.96
CHEMBL3397721 EC50 = 1170.0 nM 5.93
CHEMBL3397728 EC50 = 1300.0 nM 5.89
CHEMBL3397714 EC50 = 1800.0 nM 5.75
CHEMBL3397719 EC50 = 2100.0 nM 5.68
CHEMBL3397722 EC50 = 2200.0 nM 5.66
CHEMBL3397711 EC50 = 2500.0 nM 5.60
CHEMBL3397716 EC50 = 3200.0 nM 5.50
CHEMBL3397713 EC50 = 3200.0 nM 5.50
CHEMBL3397712 EC50 = 4400.0 nM 5.36
CHEMBL3397723 EC50 = 4500.0 nM 5.35
CHEMBL1171834 EC50 = 4600.0 nM 5.34
CHEMBL3397720 EC50 = 10700.0 nM 4.97
CHEMBL461883 EC50 = 11300.0 nM 4.95
CHEMBL3397726 EC50 = 11200.0 nM 4.95
CHEMBL3397708 EC50 = 12000.0 nM 4.92
CHEMBL3397715 EC50 = 13800.0 nM 4.86
CHEMBL3397710 EC50 = 14100.0 nM 4.85
CHEMBL3397709 EC50 = 15600.0 nM 4.81
CHEMBL3397718 EC50 = 23200.0 nM 4.63
CHEMBL3397725 EC50 > 40000.0 nM -