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Assay Detail

CHEMBL5041730

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

Binding
Inhibition of human amyloid beta (1 to 42) in human SKNBE2 cells expressing wild-type amyloid precursor protein hAPP695 incubated for 18 hrs by sandwich ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SKNBE2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Amyloid-beta precursor protein (CHEMBL2487)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo.
Peschiulli A, Oehlrich D, Van Gool M, Austin N, Van Brandt S, Surkyn M, De Cleyn M, Vos A, Tresadern G, Rombouts FJR, Macdonald GJ, Moechars D, Trabanco AA, Gijsen HJM.
ACS Med Chem Lett (2022) 13 : 76 -83
PubMed 35059126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.53 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5084378 1 9.00
CHEMBL5093303 1 9.00
CHEMBL5082406 1 8.92
CHEMBL5074068 1 8.89
CHEMBL5077699 1 8.60
CHEMBL5085412 1 8.59
CHEMBL2152899 1 8.48
CHEMBL5075933 1 8.44
CHEMBL5093195 1 8.32
CHEMBL5073381 1 8.20
CHEMBL5085521 1 8.07
CHEMBL5088449 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5084378 IC50 = 1.0 nM 9.00
CHEMBL5093303 IC50 = 1.0 nM 9.00
CHEMBL5082406 IC50 = 1.2 nM 8.92
CHEMBL5074068 IC50 = 1.3 nM 8.89
CHEMBL5077699 IC50 = 2.5 nM 8.60
CHEMBL5085412 IC50 = 2.6 nM 8.59
CHEMBL2152899 IC50 = 3.3 nM 8.48
CHEMBL5075933 IC50 = 3.6 nM 8.44
CHEMBL5093195 IC50 = 4.8 nM 8.32
CHEMBL5073381 IC50 = 6.3 nM 8.20
CHEMBL5085521 IC50 = 8.5 nM 8.07
CHEMBL5088449 IC50 = 12.6 nM 7.90