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Assay Detail

CHEMBL5034201

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

Functional
In vivo inhibition of BACE1 in dog assessed as reduction in amyloid-beta level at 3 mg/kg, po measured upto 48 hrs by sandwich ELISA assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 5 8.85 10.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4452566 1 10.01
CHEMBL3667410 1 9.92
CHEMBL3667415 1 9.89
CHEMBL2396989 LY-2886721 1.0 1 7.85
CHEMBL3701713 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4452566 IC50 = 0.097 nM 10.01
CHEMBL3667410 IC50 = 0.12 nM 9.92
CHEMBL3667415 IC50 = 0.13 nM 9.89
CHEMBL2396989 LY-2886721 IC50 = 14.0 nM 7.85
CHEMBL3701713 IC50 = 276.0 nM 6.56