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Assay Detail

CHEMBL856870

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

Binding
Inhibition of human BACE1 by MBPC125Swe assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC-12
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase.
Maillard MC, Hom RK, Benson TE, Moon JB, Mamo S, Bienkowski M, Tomasselli AG, Woods DD, Prince DB, Paddock DJ, Emmons TL, Tucker JA, Dappen MS, Brogley L, Thorsett ED, Jewett N, Sinha S, John V.
J Med Chem (2007) 50 : 776 -781
PubMed 17300163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.13 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373533 1 8.30
CHEMBL221597 1 7.70
CHEMBL265861 1 7.16
CHEMBL375540 1 6.89
CHEMBL221086 1 6.89
CHEMBL265862 1 6.70
CHEMBL220813 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373533 IC50 = 5.0 nM 8.30
CHEMBL221597 IC50 = 20.0 nM 7.70
CHEMBL265861 IC50 = 70.0 nM 7.16
CHEMBL375540 IC50 = 130.0 nM 6.89
CHEMBL221086 IC50 = 130.0 nM 6.89
CHEMBL265862 IC50 = 200.0 nM 6.70
CHEMBL220813 IC50 = 500.0 nM 6.30