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Assay Detail

CHEMBL4049296

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

Binding
Inhibition of recombinant human BACE1 (1 to 460 residues) using CEVNLDAEFK as substrate preincubated for 10 mins followed by substrate addition measured after 6.5 hrs by TR-FRET assay
2
Total Activities
2
Compounds Tested
2
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

Toward β-Secretase-1 Inhibitors with Improved Isoform Selectivity.
Johansson P, Kaspersson K, Gurrell IK, Bäck E, Eketjäll S, Scott CW, Cebers G, Thorne P, McKenzie MJ, Beaton H, Davey P, Kolmodin K, Holenz J, Duggan ME, Budd Haeberlein S, Bürli RW.
J Med Chem (2018) 61 : 3491 -3502
PubMed 29617572 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.58 7.58
IC50 1 9.22 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2177913 AZD-3839 1.0 1 9.22
CHEMBL3989948 LANABECESTAT 3.0 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2177913 AZD-3839 IC50 = 0.6 nM 9.22
CHEMBL3989948 LANABECESTAT Ki = 26.0 nM 7.58