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Assay Detail

CHEMBL2187563

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

Binding
Inhibition of BACE1-mediated amyloid beta 40 release in C57/BL6 mouse primary cortical neurons after overnight incubation by ELISA
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type Cerebral cortex neuron
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-secretase 1 (CHEMBL4593)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design and synthesis of β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of β-amyloid peptides.
Swahn BM, Kolmodin K, Karlström S, von Berg S, Söderman P, Holenz J, Berg S, Lindström J, Sundström M, Turek D, Kihlström J, Slivo C, Andersson L, Pyring D, Rotticci D, Ohberg L, Kers A, Bogar K, von Kieseritzky F, Bergh M, Olsson LL, Janson J, Eketjäll S, Georgievska B, Jeppsson F, Fälting J.
J Med Chem (2012) 55 : 9346 -9361
PubMed 22924815 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.42 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152903 1 8.59
CHEMBL2177304 1 8.47
CHEMBL2177919 1 7.52
CHEMBL2177917 1 7.40
CHEMBL2177913 AZD-3839 1.0 1 7.29
CHEMBL2177914 1 7.28
CHEMBL2177904 1 7.17
CHEMBL2177909 1 6.69
CHEMBL2177906 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152903 IC50 = 2.6 nM 8.59
CHEMBL2177304 IC50 = 3.4 nM 8.47
CHEMBL2177919 IC50 = 30.0 nM 7.52
CHEMBL2177917 IC50 = 40.0 nM 7.40
CHEMBL2177913 AZD-3839 IC50 = 51.0 nM 7.29
CHEMBL2177914 IC50 = 53.0 nM 7.28
CHEMBL2177904 IC50 = 68.0 nM 7.17
CHEMBL2177909 IC50 = 204.0 nM 6.69
CHEMBL2177906 IC50 = 436.0 nM 6.36