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Assay Detail

CHEMBL4614136

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Binding
Inhibition of human BACE2
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 2 (CHEMBL2525)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.
Winneroski LL, Erickson JA, Green SJ, Lopez JE, Stout SL, Porter WJ, Timm DE, Audia JE, Barberis M, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hembre EJ, Hendle J, Garcia-Losada P, Minguez JM, Mathes BM, May PC, Monk SA, Rankovic Z, Shi Y, Watson BM, Yang Z, Mergott DJ.
Bioorg Med Chem (2020) 28 : 115194 -115194
PubMed 31786008 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.39 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4637426 1 8.28
CHEMBL2396989 LY-2886721 1.0 1 7.99
CHEMBL4643727 1 7.66
CHEMBL4636286 1 7.36
CHEMBL2333941 LY-2811376 1.0 1 6.54
CHEMBL4644249 1 5.80
CHEMBL4642463 1 5.13
CHEMBL4636311 1 4.61
CHEMBL4640948 1 4.13
CHEMBL4637568 1 -
CHEMBL4637913 1 -
CHEMBL4648644 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4637426 IC50 = 5.3 nM 8.28
CHEMBL2396989 LY-2886721 IC50 = 10.2 nM 7.99
CHEMBL4643727 IC50 = 22.0 nM 7.66
CHEMBL4636286 IC50 = 44.0 nM 7.36
CHEMBL2333941 LY-2811376 IC50 = 288.0 nM 6.54
CHEMBL4644249 IC50 = 1580.0 nM 5.80
CHEMBL4642463 IC50 = 7330.0 nM 5.13
CHEMBL4636311 IC50 = 24600.0 nM 4.61
CHEMBL4640948 IC50 = 73600.0 nM 4.13
CHEMBL4637568 IC50 > 100000.0 nM -
CHEMBL4637913 IC50 = 104000.0 nM -
CHEMBL4648644 IC50 > 100000.0 nM -