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Assay Detail

CHEMBL1936474

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

Binding
Inhibition of BACE1 using methoxycoumarin-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys-dinitrophenyl as substrate preincubated 1 hr before substrate addition measured after 15 mins by FRET assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation.
Chiriano G, De Simone A, Mancini F, Perez DI, Cavalli A, Bolognesi ML, Legname G, Martinez A, Andrisano V, Carloni P, Roberti M.
Eur J Med Chem (2012) 48 : 206 -213
PubMed 22209418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.75 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378225 1 8.00
CHEMBL1933457 1 5.25
CHEMBL1933459 1 5.22
CHEMBL1933456 1 5.13
CHEMBL1933455 1 5.13
CHEMBL1933453 1 -
CHEMBL1933452 1 -
CHEMBL1933451 1 -
CHEMBL1933450 1 -
CHEMBL1933454 1 -
CHEMBL1933458 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378225 IC50 = 10.0 nM 8.00
CHEMBL1933457 IC50 = 5590.0 nM 5.25
CHEMBL1933459 IC50 = 5950.0 nM 5.22
CHEMBL1933456 IC50 = 7320.0 nM 5.13
CHEMBL1933455 IC50 = 7400.0 nM 5.13
CHEMBL1933453 IC50 - -
CHEMBL1933452 IC50 - -
CHEMBL1933451 IC50 - -
CHEMBL1933450 IC50 - -
CHEMBL1933454 IC50 - -
CHEMBL1933458 IC50 - -