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Assay Detail

CHEMBL961375

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

Binding
Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Caco-2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.
Colabufo NA, Berardi F, Contino M, Inglese C, Niso M, Perrone R.
Bioorg Med Chem Lett (2008) 18 : 3741 -3744
PubMed 18524592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 4.46 4.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6966 VERAPAMIL 4.0 1 4.70
CHEMBL387052 1 4.56
CHEMBL160 CYCLOSPORINE 4.0 1 4.34
CHEMBL83 TAMOXIFEN 4.0 1 4.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6966 VERAPAMIL EC50 = 20000.0 nM 4.70
CHEMBL387052 EC50 = 27600.0 nM 4.56
CHEMBL160 CYCLOSPORINE EC50 = 45500.0 nM 4.34
CHEMBL83 TAMOXIFEN EC50 = 56500.0 nM 4.25