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Assay Detail

CHEMBL4388902

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

Binding
Inhibition of gamma secretase in mouse Neuro2 cells expressing endogenous levels of amyloid precursor protein assessed as reduction in Abeta42 levels incubated for 18 hrs by sandwich ELISA
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 34 7.07 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4541193 1 8.15
CHEMBL2151205 E-2212 1.0 1 7.96
CHEMBL4521904 1 7.80
CHEMBL4451760 1 7.77
CHEMBL4458813 1 7.72
CHEMBL4520168 1 7.72
CHEMBL4549121 1 7.64
CHEMBL4536918 1 7.55
CHEMBL4544029 1 7.47
CHEMBL4539673 1 7.44
CHEMBL4516657 1 7.39
CHEMBL4542879 1 7.38
CHEMBL4446595 1 7.38
CHEMBL4579909 1 7.34
CHEMBL4466805 1 7.31
CHEMBL4462407 1 7.30
CHEMBL4591352 1 7.23
CHEMBL4560947 1 7.13
CHEMBL4591622 1 7.07
CHEMBL4535866 1 7.07
CHEMBL4524417 1 6.97
CHEMBL4590743 1 6.78
CHEMBL2151216 1 6.74
CHEMBL4436587 1 6.73
CHEMBL4582605 1 6.60
CHEMBL4457660 1 6.56
CHEMBL4449897 1 6.53
CHEMBL4468761 1 6.47
CHEMBL4527794 1 6.17
CHEMBL4542411 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4541193 IC50 = 7.0 nM 8.15
CHEMBL2151205 E-2212 IC50 = 11.0 nM 7.96
CHEMBL4521904 IC50 = 16.0 nM 7.80
CHEMBL4451760 IC50 = 17.0 nM 7.77
CHEMBL4458813 IC50 = 19.0 nM 7.72
CHEMBL4520168 IC50 = 19.0 nM 7.72
CHEMBL4549121 IC50 = 23.0 nM 7.64
CHEMBL4536918 IC50 = 28.0 nM 7.55
CHEMBL4544029 IC50 = 34.0 nM 7.47
CHEMBL4539673 IC50 = 36.0 nM 7.44
CHEMBL4516657 IC50 = 41.0 nM 7.39
CHEMBL4542879 IC50 = 42.0 nM 7.38
CHEMBL4446595 IC50 = 42.0 nM 7.38
CHEMBL4579909 IC50 = 46.0 nM 7.34
CHEMBL4466805 IC50 = 49.0 nM 7.31
CHEMBL4462407 IC50 = 50.0 nM 7.30
CHEMBL4591352 IC50 = 59.0 nM 7.23
CHEMBL4560947 IC50 = 74.0 nM 7.13
CHEMBL4591622 IC50 = 85.0 nM 7.07
CHEMBL4535866 IC50 = 85.0 nM 7.07
CHEMBL4524417 IC50 = 107.0 nM 6.97
CHEMBL4590743 IC50 = 166.0 nM 6.78
CHEMBL2151216 IC50 = 182.0 nM 6.74
CHEMBL4436587 IC50 = 186.0 nM 6.73
CHEMBL4582605 IC50 = 251.0 nM 6.60
CHEMBL4457660 IC50 = 275.0 nM 6.56
CHEMBL4449897 IC50 = 295.0 nM 6.53
CHEMBL4468761 IC50 = 339.0 nM 6.47
CHEMBL4527794 IC50 = 680.0 nM 6.17
CHEMBL4542411 IC50 = 780.0 nM 6.11
CHEMBL4435638 IC50 = 1670.0 nM 5.78
CHEMBL4474036 IC50 = 8500.0 nM 5.07
CHEMBL4474638 IC50 > 10000.0 nM -
CHEMBL4534560 IC50 > 10000.0 nM -