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Assay Detail

CHEMBL4630545

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

Binding
Modulation of gamma secretase in HEK293 cells transfected with human APP with Swedish and London familial AD mutation assessed as reduction in Abeta42 levels incubated for 5 hrs by sandwich immuno-assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Generation of Leads for γ-Secretase Modulation.
Mandal M, Buevich A, Caldwell JP, Hyde L, Huang X, Liu X, McKittrick B, Mazzola RD, Pissarnitski D, Palani A, Zhang L, Parker E, Xiao L, Rindgen D, Zhu Z.
J Med Chem (2020) 63 : 8216 -8230
PubMed 32786237 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.92 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4632652 1 7.82
CHEMBL1950434 1 7.54
CHEMBL2180376 1 7.48
CHEMBL1950535 1 7.43
CHEMBL2312555 1 7.41
CHEMBL4641625 1 7.32
CHEMBL4643105 1 7.28
CHEMBL4634921 1 7.26
CHEMBL1224151 1 7.19
CHEMBL4648298 1 7.16
CHEMBL4634696 1 6.97
CHEMBL4637679 1 6.95
CHEMBL1643425 1 6.94
CHEMBL4642697 1 6.84
CHEMBL4636430 1 6.40
CHEMBL4639757 1 6.33
CHEMBL4643160 1 6.29
CHEMBL4639056 1 5.81
CHEMBL4644009 1 5.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4632652 IC50 = 15.0 nM 7.82
CHEMBL1950434 IC50 = 29.0 nM 7.54
CHEMBL2180376 IC50 = 33.0 nM 7.48
CHEMBL1950535 IC50 = 37.0 nM 7.43
CHEMBL2312555 IC50 = 39.0 nM 7.41
CHEMBL4641625 IC50 = 48.0 nM 7.32
CHEMBL4643105 IC50 = 52.0 nM 7.28
CHEMBL4634921 IC50 = 55.0 nM 7.26
CHEMBL1224151 IC50 = 64.0 nM 7.19
CHEMBL4648298 IC50 = 69.0 nM 7.16
CHEMBL4634696 IC50 = 107.0 nM 6.97
CHEMBL4637679 IC50 = 113.0 nM 6.95
CHEMBL1643425 IC50 = 116.0 nM 6.94
CHEMBL4642697 IC50 = 143.0 nM 6.84
CHEMBL4636430 IC50 = 400.0 nM 6.40
CHEMBL4639757 IC50 = 462.0 nM 6.33
CHEMBL4643160 IC50 = 512.0 nM 6.29
CHEMBL4639056 IC50 = 1554.0 nM 5.81
CHEMBL4644009 IC50 = 9289.0 nM 5.03