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Assay Detail

CHEMBL856871

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

Functional
Inhibition of beta amyloid production in human HEK293 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Beta-secretase (BACE) (CHEMBL2111390)
Type PROTEIN FAMILY
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
EC50 7 7.19 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373533 1 8.52
CHEMBL221597 1 7.82
CHEMBL221086 1 7.40
CHEMBL265861 1 7.10
CHEMBL375540 1 6.64
CHEMBL265862 1 6.64
CHEMBL220813 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373533 EC50 = 3.0 nM 8.52
CHEMBL221597 EC50 = 15.0 nM 7.82
CHEMBL221086 EC50 = 40.0 nM 7.40
CHEMBL265861 EC50 = 80.0 nM 7.10
CHEMBL375540 EC50 = 230.0 nM 6.64
CHEMBL265862 EC50 = 230.0 nM 6.64
CHEMBL220813 EC50 = 600.0 nM 6.22