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Assay Detail

CHEMBL3868309

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Binding
Inhibition of BACE1 (unknown origin)
12
Total Activities
12
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 1 (CHEMBL4822)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors.
Wu YJ, Guernon J, Rajamani R, Toyn JH, Ahlijanian MK, Albright CF, Muckelbauer J, Chang C, Camac D, Macor JE, Thompson LA.
Bioorg Med Chem Lett (2016) 26 : 5729 -5731
PubMed 27816517 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.88 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2396989 LY-2886721 1.0 1 7.92
CHEMBL3891534 1 7.70
CHEMBL3919597 1 7.48
CHEMBL3909581 1 7.48
CHEMBL3980733 1 7.43
CHEMBL3959813 1 6.80
CHEMBL3910646 1 6.80
CHEMBL3986498 1 6.64
CHEMBL3890737 1 6.29
CHEMBL3900541 1 6.22
CHEMBL3897492 1 6.07
CHEMBL3928503 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2396989 LY-2886721 IC50 = 12.0 nM 7.92
CHEMBL3891534 IC50 = 20.0 nM 7.70
CHEMBL3919597 IC50 = 33.0 nM 7.48
CHEMBL3909581 IC50 = 33.0 nM 7.48
CHEMBL3980733 IC50 = 37.0 nM 7.43
CHEMBL3959813 IC50 = 160.0 nM 6.80
CHEMBL3910646 IC50 = 160.0 nM 6.80
CHEMBL3986498 IC50 = 230.0 nM 6.64
CHEMBL3890737 IC50 = 510.0 nM 6.29
CHEMBL3900541 IC50 = 600.0 nM 6.22
CHEMBL3897492 IC50 = 860.0 nM 6.07
CHEMBL3928503 IC50 = 2000.0 nM 5.70