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Assay Detail

CHEMBL3887616

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

Binding
Cell-Based Assay: The ability of compounds to modulate production of amyloid beta protein Abeta(1-42) was determined using human WT-APP overexpressing CHO cells. Cells were plated at 22,000 cells/100 uL well in 96 well tissue culture treated, clear plates (Falcon) in DMEM/F12 based medium and incubated for 24 hours at 37° C. Compounds for testing were diluted in 100% DMSO to achieve an eleven points, half log, dose response for IC50 determinations. Compounds were added in fresh medium to achieve 1% final DMSO. Appropriate vehicle or inhibitor controls were added into control wells individually to obtain minimum or maximum inhibition values, respectively, for the assay signal window before the plates were incubated for 24 hours at 37° C. This procedure produces conditioned media in each well which is tested for Abeta(1-42) levels in the ELISA detection step described next. The remaining cell cultures in each well are also tested for cell toxicity as described below.
73
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 73 7.15 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3942982 1 8.48
CHEMBL3893460 1 8.26
CHEMBL3890783 1 8.24
CHEMBL3951810 1 8.11
CHEMBL3959250 1 8.08
CHEMBL3980608 1 8.04
CHEMBL3929506 1 8.00
CHEMBL3948397 1 7.96
CHEMBL3978667 1 7.96
CHEMBL3962470 1 7.94
CHEMBL3906008 1 7.88
CHEMBL3955146 1 7.84
CHEMBL3917064 1 7.84
CHEMBL3976595 1 7.82
CHEMBL3979115 1 7.80
CHEMBL3925476 1 7.80
CHEMBL3968096 1 7.70
CHEMBL3985730 1 7.67
CHEMBL3924102 1 7.62
CHEMBL3918666 1 7.61
CHEMBL3906428 1 7.60
CHEMBL4115891 1 7.58
CHEMBL3910627 1 7.57
CHEMBL3911070 1 7.56
CHEMBL3908938 1 7.54
CHEMBL3902117 1 7.52
CHEMBL3918851 1 7.47
CHEMBL3890183 1 7.42
CHEMBL3972571 1 7.39
CHEMBL3938538 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3942982 IC50 = 3.34 nM 8.48
CHEMBL3893460 IC50 = 5.48 nM 8.26
CHEMBL3890783 IC50 = 5.78 nM 8.24
CHEMBL3951810 IC50 = 7.84 nM 8.11
CHEMBL3959250 IC50 = 8.35 nM 8.08
CHEMBL3980608 IC50 = 9.1 nM 8.04
CHEMBL3929506 IC50 = 10.0 nM 8.00
CHEMBL3948397 IC50 = 11.0 nM 7.96
CHEMBL3978667 IC50 = 11.1 nM 7.96
CHEMBL3962470 IC50 = 11.4 nM 7.94
CHEMBL3906008 IC50 = 13.3 nM 7.88
CHEMBL3955146 IC50 = 14.3 nM 7.84
CHEMBL3917064 IC50 = 14.5 nM 7.84
CHEMBL3976595 IC50 = 15.0 nM 7.82
CHEMBL3925476 IC50 = 15.7 nM 7.80
CHEMBL3979115 IC50 = 16.0 nM 7.80
CHEMBL3968096 IC50 = 19.8 nM 7.70
CHEMBL3985730 IC50 = 21.6 nM 7.67
CHEMBL3924102 IC50 = 24.2 nM 7.62
CHEMBL3918666 IC50 = 24.6 nM 7.61
CHEMBL3906428 IC50 = 25.0 nM 7.60
CHEMBL4115891 IC50 = 26.6 nM 7.58
CHEMBL3910627 IC50 = 26.8 nM 7.57
CHEMBL3911070 IC50 = 27.6 nM 7.56
CHEMBL3908938 IC50 = 29.1 nM 7.54
CHEMBL3902117 IC50 = 29.9 nM 7.52
CHEMBL3918851 IC50 = 33.5 nM 7.47
CHEMBL3890183 IC50 = 38.4 nM 7.42
CHEMBL3972571 IC50 = 40.5 nM 7.39
CHEMBL3938538 IC50 = 46.4 nM 7.33
CHEMBL3960512 IC50 = 52.4 nM 7.28
CHEMBL3926551 IC50 = 52.1 nM 7.28
CHEMBL3896372 IC50 = 60.6 nM 7.22
CHEMBL3928795 IC50 = 60.3 nM 7.22
CHEMBL3953711 IC50 = 63.8 nM 7.20
CHEMBL3980167 IC50 = 73.5 nM 7.13
CHEMBL3913030 IC50 = 73.3 nM 7.13
CHEMBL3949792 IC50 = 73.5 nM 7.13
CHEMBL3935522 IC50 = 73.3 nM 7.13
CHEMBL3900856 IC50 = 80.0 nM 7.10
CHEMBL3946187 IC50 = 81.2 nM 7.09
CHEMBL3965573 IC50 = 96.6 nM 7.01
CHEMBL3935854 IC50 = 98.0 nM 7.01
CHEMBL3889603 IC50 = 112.0 nM 6.95
CHEMBL3935477 IC50 = 117.0 nM 6.93
CHEMBL3935655 IC50 = 120.0 nM 6.92
CHEMBL3890892 IC50 = 140.0 nM 6.85
CHEMBL3956978 IC50 = 146.0 nM 6.84
CHEMBL3912132 IC50 = 153.0 nM 6.82
CHEMBL3966656 IC50 = 158.0 nM 6.80