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Assay Detail

CHEMBL896440

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

Binding
Inhibition of gamma secretase in APP-transfected CHO cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent gamma-secretase inhibitors.
Yang MG, Shi JL, Modi DP, Wells J, Cochran BM, Wolf MA, Thompson LA, Ramanjulu MM, Roach AH, Zaczek R, Robertson DW, Wexler RR, Olson RE.
Bioorg Med Chem Lett (2007) 17 : 3910 -3915
PubMed 17502143 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.64 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL232938 1 8.38
CHEMBL232182 1 8.24
CHEMBL232936 1 8.21
CHEMBL399204 1 8.17
CHEMBL392265 1 7.96
CHEMBL429438 1 7.90
CHEMBL232346 1 7.89
CHEMBL231941 1 7.85
CHEMBL232138 1 7.82
CHEMBL232739 1 7.82
CHEMBL393520 1 7.72
CHEMBL232183 1 7.71
CHEMBL231984 1 7.70
CHEMBL450279 1 7.68
CHEMBL449960 1 7.68
CHEMBL401045 1 7.58
CHEMBL401044 1 7.55
CHEMBL399819 1 7.09
CHEMBL233172 1 7.02
CHEMBL231725 1 6.94
CHEMBL273493 1 6.55
CHEMBL232367 1 6.55
CHEMBL398379 1 -
CHEMBL401434 1 -
CHEMBL232968 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL232938 IC50 = 4.2 nM 8.38
CHEMBL232182 IC50 = 5.8 nM 8.24
CHEMBL232936 IC50 = 6.1 nM 8.21
CHEMBL399204 IC50 = 6.7 nM 8.17
CHEMBL392265 IC50 = 11.0 nM 7.96
CHEMBL429438 IC50 = 12.5 nM 7.90
CHEMBL232346 IC50 = 13.0 nM 7.89
CHEMBL231941 IC50 = 14.0 nM 7.85
CHEMBL232138 IC50 = 15.0 nM 7.82
CHEMBL232739 IC50 = 15.0 nM 7.82
CHEMBL393520 IC50 = 19.0 nM 7.72
CHEMBL232183 IC50 = 19.5 nM 7.71
CHEMBL231984 IC50 = 20.0 nM 7.70
CHEMBL450279 IC50 = 21.0 nM 7.68
CHEMBL449960 IC50 = 21.0 nM 7.68
CHEMBL401045 IC50 = 26.1 nM 7.58
CHEMBL401044 IC50 = 28.0 nM 7.55
CHEMBL399819 IC50 = 82.0 nM 7.09
CHEMBL233172 IC50 = 96.0 nM 7.02
CHEMBL231725 IC50 = 115.0 nM 6.94
CHEMBL273493 IC50 = 280.0 nM 6.55
CHEMBL232367 IC50 = 280.0 nM 6.55
CHEMBL398379 IC50 - -
CHEMBL401434 IC50 - -
CHEMBL232968 IC50 - -