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Assay Detail

CHEMBL4820208

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

Binding
Reversal of P-glycoprotein mediated multidrug resistance in human KBV cells assessed as reversal of resistance to vincristine-induced cytotoxicity by measuring vincristine IC50 at 5 uM measured after 72 hrs by MTT assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.
Wang B, Liu S, Huang W, Ma M, Chen X, Zeng W, Liang K, Wang H, Bi Y, Li X.
Eur J Med Chem (2021) 211 : 113107 -113107
PubMed 33360797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.25 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL348475 TARIQUIDAR 3.0 1 8.48
CHEMBL4863423 1 8.40
CHEMBL6966 VERAPAMIL 4.0 1 8.34
CHEMBL4161103 1 7.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL348475 TARIQUIDAR IC50 = 3.34 nM 8.48
CHEMBL4863423 IC50 = 4.02 nM 8.40
CHEMBL6966 VERAPAMIL IC50 = 4.59 nM 8.34
CHEMBL4161103 IC50 = 16.58 nM 7.78