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Assay Detail

CHEMBL5034202

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

Binding
Inhibition of recombinant human BACE2 using (MCA)-S-E-V-N-L-D-A-E-F-R-K(dinitrophenol)-R-R-R-R-NH2 as substrate by FRET assay
3
Total Activities
3
Compounds Tested
1
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 2 (CHEMBL2525)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor.
McKinzie DL, Winneroski LL, Green SJ, Hembre EJ, Erickson JA, Willis BA, Monk SA, Aluise CD, Baker TK, Lopez JE, Hendle J, Beck JP, Brier RA, Boggs LN, Borders AR, Cocke PJ, Garcia-Losada P, Lowe SL, Mathes BM, May PC, Porter WJ, Stout SL, Timm DE, Watson BM, Yang Z, Mergott DJ.
J Med Chem (2021) 64 : 8076 -8100
PubMed 34081466 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 9.24 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3667410 1 9.41
CHEMBL3667415 1 9.26
CHEMBL4452566 1 9.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3667410 IC50 = 0.388 nM 9.41
CHEMBL3667415 IC50 = 0.555 nM 9.26
CHEMBL4452566 IC50 = 0.871 nM 9.06