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Assay Detail

CHEMBL5041739

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

ADMET
Inhibition of human CYP3A4 by fluorescence plate reader analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 3A4 (CHEMBL340)
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 4 5.52 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5075933 1 6.05
CHEMBL5073381 1 5.51
CHEMBL5088449 1 5.36
CHEMBL2152899 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5075933 IC50 = 900.0 nM 6.05
CHEMBL5073381 IC50 = 3100.0 nM 5.51
CHEMBL5088449 IC50 = 4400.0 nM 5.36
CHEMBL2152899 IC50 = 6700.0 nM 5.17