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Assay Detail

CHEMBL4322973

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

Binding
Inhibition of recombinant human BACE1 incubated for 3 hrs using APP derived peptide as substrate by HTRF assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of an Extremely Potent Thiazine-Based β-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.
Tadano G, Komano K, Yoshida S, Suzuki S, Nakahara K, Fuchino K, Fujimoto K, Matsuoka E, Yamamoto T, Asada N, Ito H, Sakaguchi G, Kanegawa N, Kido Y, Ando S, Fukushima T, Teisman A, Urmaliya V, Dhuyvetter D, Borghys H, Van Den Bergh A, Austin N, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI.
J Med Chem (2019) 62 : 9331 -9337
PubMed 31549838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.30 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4557670 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4557670 IC50 = 5.0 nM 8.30