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Assay Detail

CHEMBL833073

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Functional
inhibitory activity against human CYP3A4 production
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Cell line
Confidence 1 — Organism
Curated By Intermediate

Target

Cell line (CHEMBL614840)
Type CELL-LINE
Organism Homo sapiens

Publication

Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.
Lewis TA, Young MA, Arrington MP, Bayless L, Cai X, Collart P, Eckman JB, Ellis JL, Ene DG, Libertine L, Nicolas JM, Scannell RT, Wels BF, Wenberg K, Wypij DM.
Bioorg Med Chem Lett (2004) 14 : 5591 -5594
PubMed 15482930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.10 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185905 1 8.22
CHEMBL186125 1 8.22
CHEMBL444083 1 8.22
CHEMBL187264 1 8.10
CHEMBL425358 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185905 IC50 = 6.0 nM 8.22
CHEMBL186125 IC50 = 6.0 nM 8.22
CHEMBL444083 IC50 = 6.0 nM 8.22
CHEMBL187264 IC50 = 8.0 nM 8.10
CHEMBL425358 IC50 = 18.0 nM 7.75