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Assay Detail

CHEMBL666254

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

ADMET
Inhibition of human cytochrome P450 3A4 as total cyclosporin oxidation (1 uM)
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.
Bromidge SM, Brown AM, Clarke SE, Dodgson K, Gager T, Grassam HL, Jeffrey PM, Joiner GF, King FD, Middlemiss DN, Moss SF, Newman H, Riley G, Routledge C, Wyman P.
J Med Chem (1999) 42 : 202 -205
PubMed 9925723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.81 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292759 1 5.22
CHEMBL542139 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292759 IC50 = 6000.0 nM 5.22
CHEMBL542139 IC50 = 40000.0 nM 4.40