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Assay Detail

CHEMBL652104

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

Functional
MDR-modulating activity as a measure to inhibit P-glycoprotein (PGP) mediated transmembrane transport in human T-lymphoblast cell line CEM vcr 1000 using the daunomycin efflux assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CCRF-CEM/VCR-1000
Confidence 1 — Organism
Curated By Intermediate

Target

CCRF-CEM/VCR-1000 (CHEMBL614540)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and pharmacological activity of the stereoisomers of GP-88, a propafenone-type modulator of multidrug resistance.
Chiba P, Rebitzer S, Richter E, Hitzler M, Ecker G.
Bioorg Med Chem Lett (1998) 8 : 829 -832
PubMed 9871549 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.17 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1788268 1 6.58
CHEMBL1322675 1 6.43
CHEMBL170328 1 6.24
CHEMBL168258 1 6.11
CHEMBL349429 1 5.85
CHEMBL353163 1 5.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1788268 EC50 = 260.0 nM 6.58
CHEMBL1322675 EC50 = 370.0 nM 6.43
CHEMBL170328 EC50 = 580.0 nM 6.24
CHEMBL168258 EC50 = 780.0 nM 6.11
CHEMBL349429 EC50 = 1400.0 nM 5.85
CHEMBL353163 EC50 = 1560.0 nM 5.81