Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2076282

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

Functional
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type Caco-2
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

ATP-dependent translocase ABCB1 (CHEMBL4302)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein.
Wandel C, Kim R, Wood M, Wood A.
Anesthesiology (2002) 96 : 913 -920
PubMed 11964599 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.38 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL841 LOPERAMIDE 4.0 1 5.60
CHEMBL658 SUFENTANIL 4.0 1 5.35
CHEMBL596 FENTANYL 4.0 1 5.19
CHEMBL634 ALFENTANIL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL841 LOPERAMIDE IC50 = 2500.0 nM 5.60
CHEMBL658 SUFENTANIL IC50 = 4500.0 nM 5.35
CHEMBL596 FENTANYL IC50 = 6500.0 nM 5.19
CHEMBL634 ALFENTANIL IC50 = 112000.0 nM -