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Assay Detail

CHEMBL4388922

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

Binding
Inhibition of gamma secretase in human SKNBE2 cells expressing human APP695 assessed as increase in Abeta38 levels incubated for 18 hrs by sandwich ELISA
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Gamma-secretase (CHEMBL2094135)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators.
Bischoff FP, Velter AI, Minne G, Pieters S, Berthelot D, De Cleyn M, Gijsen HJM, Macdonald G, Surkyn M, Van Brandt S, Van Roosbroeck Y, Zavattaro C, Mercken M, Austin N, Dhuyvetter D, Borghys H, Ahmad I, Samanta SK.
Bioorg Med Chem Lett (2019) 29 : 1737 -1745
PubMed 31122869 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.17 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4451760 1 7.85
CHEMBL4471286 1 7.82
CHEMBL4563162 1 7.77
CHEMBL4458813 1 7.75
CHEMBL4466805 1 7.72
CHEMBL4587055 1 7.66
CHEMBL4521904 1 7.64
CHEMBL4536918 1 7.60
CHEMBL4549121 1 7.58
CHEMBL4520168 1 7.51
CHEMBL4544029 1 7.50
CHEMBL4539673 1 7.44
CHEMBL4542879 1 7.44
CHEMBL4535885 1 7.41
CHEMBL4560947 1 7.39
CHEMBL4446595 1 7.35
CHEMBL4591352 1 7.23
CHEMBL4558822 1 7.18
CHEMBL4516657 1 7.14
CHEMBL4524417 1 7.01
CHEMBL4590743 1 6.97
CHEMBL4535866 1 6.96
CHEMBL4462407 1 6.95
CHEMBL4436587 1 6.93
CHEMBL4468761 1 6.66
CHEMBL4582605 1 6.46
CHEMBL4449897 1 6.22
CHEMBL4474036 1 5.40
CHEMBL4534560 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4451760 IC50 = 14.0 nM 7.85
CHEMBL4471286 IC50 = 15.0 nM 7.82
CHEMBL4563162 IC50 = 17.0 nM 7.77
CHEMBL4458813 IC50 = 18.0 nM 7.75
CHEMBL4466805 IC50 = 19.0 nM 7.72
CHEMBL4587055 IC50 = 22.0 nM 7.66
CHEMBL4521904 IC50 = 23.0 nM 7.64
CHEMBL4536918 IC50 = 25.0 nM 7.60
CHEMBL4549121 IC50 = 26.0 nM 7.58
CHEMBL4520168 IC50 = 31.0 nM 7.51
CHEMBL4544029 IC50 = 32.0 nM 7.50
CHEMBL4539673 IC50 = 36.0 nM 7.44
CHEMBL4542879 IC50 = 36.0 nM 7.44
CHEMBL4535885 IC50 = 39.0 nM 7.41
CHEMBL4560947 IC50 = 41.0 nM 7.39
CHEMBL4446595 IC50 = 45.0 nM 7.35
CHEMBL4591352 IC50 = 59.0 nM 7.23
CHEMBL4558822 IC50 = 66.0 nM 7.18
CHEMBL4516657 IC50 = 72.0 nM 7.14
CHEMBL4524417 IC50 = 98.0 nM 7.01
CHEMBL4590743 IC50 = 107.0 nM 6.97
CHEMBL4535866 IC50 = 110.0 nM 6.96
CHEMBL4462407 IC50 = 112.0 nM 6.95
CHEMBL4436587 IC50 = 117.0 nM 6.93
CHEMBL4468761 IC50 = 219.0 nM 6.66
CHEMBL4582605 IC50 = 347.0 nM 6.46
CHEMBL4449897 IC50 = 603.0 nM 6.22
CHEMBL4474036 IC50 = 3981.0 nM 5.40
CHEMBL4534560 IC50 = 4000.0 nM 5.40