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

CHEMBL3584052

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

Binding
Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing paclitaxel resistance measured as cell survival after 5 days by MTS assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
Wong IL, Wang BC, Yuan J, Duan LX, Liu Z, Liu T, Li XM, Hu X, Zhang XY, Jiang T, Wan SB, Chow LM.
J Med Chem (2015) 58 : 4529 -4549
PubMed 25985195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.78 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160 CYCLOSPORINE 4.0 1 7.50
CHEMBL3582149 1 6.90
CHEMBL3582168 1 6.85
CHEMBL3582148 1 6.80
CHEMBL3582155 1 6.80
CHEMBL3582167 1 6.77
CHEMBL3582156 1 6.67
CHEMBL3582170 1 6.65
CHEMBL3582169 1 6.55
CHEMBL6966 VERAPAMIL 4.0 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160 CYCLOSPORINE EC50 = 32.0 nM 7.50
CHEMBL3582149 EC50 = 127.0 nM 6.90
CHEMBL3582168 EC50 = 140.0 nM 6.85
CHEMBL3582148 EC50 = 157.0 nM 6.80
CHEMBL3582155 EC50 = 159.0 nM 6.80
CHEMBL3582167 EC50 = 171.0 nM 6.77
CHEMBL3582156 EC50 = 214.0 nM 6.67
CHEMBL3582170 EC50 = 225.0 nM 6.65
CHEMBL3582169 EC50 = 280.0 nM 6.55
CHEMBL6966 VERAPAMIL EC50 = 446.0 nM 6.35