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Assay Detail

CHEMBL5031856

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

Binding
Inhibition of BACE1 in human SKNBE2 cells expressing wildtype APP assessed as reduction in amyloid beta 42 level incubated for 18 hrs by sandwich AlphaLISA assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SKNBE2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-secretase 1 (CHEMBL4822)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions.
Ueno T, Matsuoka E, Asada N, Yamamoto S, Kanegawa N, Ito M, Ito H, Moechars D, Rombouts FJR, Gijsen HJM, Kusakabe KI.
J Med Chem (2021) 64 : 14165 -14174
PubMed 34553947 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.21 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4557670 1 9.00
CHEMBL5093159 1 8.96
CHEMBL5075689 1 8.64
CHEMBL5079271 1 7.54
CHEMBL5072129 1 6.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4557670 IC50 = 1.0 nM 9.00
CHEMBL5093159 IC50 = 1.1 nM 8.96
CHEMBL5075689 IC50 = 2.3 nM 8.64
CHEMBL5079271 IC50 = 29.0 nM 7.54
CHEMBL5072129 IC50 = 123.0 nM 6.91