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Assay Detail

CHEMBL5035554

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

Binding
Inhibition of P-glycoprotein in human LCC6MDR cells assessed as reversal fold by measuring reduction in paclitaxel by measuring paclitaxel IC50 at 1 uM after 5 days by Cell Titer-Glo luminescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type LCC6MDR
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
Wong ILK, Wang XK, Liu Z, Sun W, Li FX, Wang BC, Li P, Wan SB, Chow LMC.
Eur J Med Chem (2021) 226 : 113795 -113795
PubMed 34597896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.27 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5089855 1 8.74
CHEMBL5088809 1 8.66
CHEMBL6966 VERAPAMIL 4.0 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5089855 IC50 = 1.8 nM 8.74
CHEMBL5088809 IC50 = 2.2 nM 8.66
CHEMBL6966 VERAPAMIL IC50 = 38.0 nM 7.42