Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL917719

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

Binding
Inhibition of BACE1
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).
Stachel SJ, Coburn CA, Steele TG, Jones KG, Loutzenhiser EF, Gregro AR, Rajapakse HA, Lai MT, Crouthamel MC, Xu M, Tugusheva K, Lineberger JE, Pietrak BL, Espeseth AS, Shi XP, Chen-Dodson E, Holloway MK, Munshi S, Simon AJ, Kuo L, Vacca JP.
J Med Chem (2004) 47 : 6447 -6450
PubMed 15588077 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.49 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377625 1 8.00
CHEMBL376277 1 7.85
CHEMBL221454 1 7.82
CHEMBL266891 1 7.82
CHEMBL376072 1 7.82
CHEMBL225442 1 7.64
CHEMBL162970 1 7.39
CHEMBL222209 1 7.20
CHEMBL426717 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377625 IC50 = 10.0 nM 8.00
CHEMBL376277 IC50 = 14.0 nM 7.85
CHEMBL221454 IC50 = 15.0 nM 7.82
CHEMBL266891 IC50 = 15.0 nM 7.82
CHEMBL376072 IC50 = 15.0 nM 7.82
CHEMBL225442 IC50 = 23.0 nM 7.64
CHEMBL162970 IC50 = 41.0 nM 7.39
CHEMBL222209 IC50 = 63.0 nM 7.20
CHEMBL426717 IC50 = 1400.0 nM 5.85