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Assay Detail

CHEMBL2078583

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

Functional
TP_TRANSPORTER: drug resistance (paclitaxel) in MES-SA/DX5 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type MES-SA/Dx5
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity.
Lee BH, Lee CO, Kwon MJ, Yi KY, Yoo SE, Choi SU.
Anticancer Drugs (2003) 14 : 175 -181
PubMed 12569305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.21 5.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6966 VERAPAMIL 4.0 1 5.32
CHEMBL36148 (S)-VERAPAMIL 1 5.27
CHEMBL197 DEXVERAPAMIL 2.0 1 5.26
CHEMBL2074950 1 5.18
CHEMBL2074952 1 5.12
CHEMBL2074951 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6966 VERAPAMIL IC50 = 4780.0 nM 5.32
CHEMBL36148 (S)-VERAPAMIL IC50 = 5330.0 nM 5.27
CHEMBL197 DEXVERAPAMIL IC50 = 5520.0 nM 5.26
CHEMBL2074950 IC50 = 6630.0 nM 5.18
CHEMBL2074952 IC50 = 7630.0 nM 5.12
CHEMBL2074951 IC50 = 7650.0 nM 5.12