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Assay Detail

CHEMBL1921609

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

Binding
Inhibition of gamma secretase in human H4 cells overexpressing human APP assessed as reduction in amyloid beta-42 secretion after 22 hrs
32
Total Activities
32
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

Aminothiazoles as γ-secretase modulators.
Lübbers T, Flohr A, Jolidon S, David-Pierson P, Jacobsen H, Ozmen L, Baumann K.
Bioorg Med Chem Lett (2011) 21 : 6554 -6558
PubMed 21924610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 6.40 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1915569 1 7.36
CHEMBL1915568 1 7.28
CHEMBL1915575 1 7.07
CHEMBL1915571 1 6.91
CHEMBL1915583 1 6.90
CHEMBL1915582 1 6.88
CHEMBL1915567 1 6.88
CHEMBL1915562 1 6.87
CHEMBL1915570 1 6.68
CHEMBL1915559 1 6.67
CHEMBL1915580 1 6.67
CHEMBL1915578 1 6.61
CHEMBL1915579 1 6.60
CHEMBL1915754 1 6.50
CHEMBL1915561 1 6.47
CHEMBL1915755 1 6.42
CHEMBL1915756 1 6.32
CHEMBL1915752 1 6.19
CHEMBL1915573 1 6.17
CHEMBL1915572 1 6.13
CHEMBL1915564 1 6.10
CHEMBL1915558 1 6.09
CHEMBL1915565 1 6.06
CHEMBL1915566 1 6.05
CHEMBL1915577 1 6.00
CHEMBL1915757 1 5.54
CHEMBL1915581 1 5.47
CHEMBL1915576 1 5.46
CHEMBL1915753 1 5.26
CHEMBL1915574 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1915569 IC50 = 44.0 nM 7.36
CHEMBL1915568 IC50 = 52.0 nM 7.28
CHEMBL1915575 IC50 = 86.0 nM 7.07
CHEMBL1915571 IC50 = 123.0 nM 6.91
CHEMBL1915583 IC50 = 127.0 nM 6.90
CHEMBL1915582 IC50 = 133.0 nM 6.88
CHEMBL1915567 IC50 = 133.0 nM 6.88
CHEMBL1915562 IC50 = 136.0 nM 6.87
CHEMBL1915570 IC50 = 209.0 nM 6.68
CHEMBL1915559 IC50 = 214.0 nM 6.67
CHEMBL1915580 IC50 = 212.0 nM 6.67
CHEMBL1915578 IC50 = 244.0 nM 6.61
CHEMBL1915579 IC50 = 252.0 nM 6.60
CHEMBL1915754 IC50 = 319.0 nM 6.50
CHEMBL1915561 IC50 = 339.0 nM 6.47
CHEMBL1915755 IC50 = 376.0 nM 6.42
CHEMBL1915756 IC50 = 483.0 nM 6.32
CHEMBL1915752 IC50 = 651.0 nM 6.19
CHEMBL1915573 IC50 = 675.0 nM 6.17
CHEMBL1915572 IC50 = 733.0 nM 6.13
CHEMBL1915564 IC50 = 789.0 nM 6.10
CHEMBL1915558 IC50 = 815.0 nM 6.09
CHEMBL1915565 IC50 = 880.0 nM 6.06
CHEMBL1915566 IC50 = 898.0 nM 6.05
CHEMBL1915577 IC50 = 999.0 nM 6.00
CHEMBL1915757 IC50 = 2868.0 nM 5.54
CHEMBL1915581 IC50 = 3358.0 nM 5.47
CHEMBL1915576 IC50 = 3431.0 nM 5.46
CHEMBL1915753 IC50 = 5548.0 nM 5.26
CHEMBL1915574 IC50 > 1250.0 nM -
CHEMBL1915563 IC50 > 5000.0 nM -
CHEMBL1915560 IC50 > 40000.0 nM -