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Assay Detail

CHEMBL1219907

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

Binding
Induction of MRP1 expressed in MDCK cells assessed as calcein AM accumulation by fluorescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type MDCK
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Multidrug resistance-associated protein 1 (CHEMBL3004)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phenylsulfonylfuroxans as modulators of multidrug-resistance-associated protein-1 and P-glycoprotein.
Fruttero R, Crosetti M, Chegaev K, Guglielmo S, Gasco A, Berardi F, Niso M, Perrone R, Panaro MA, Colabufo NA.
J Med Chem (2010) 53 : 5467 -5475
PubMed 20684594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 4.52 5.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1097451 1 5.12
CHEMBL1215644 1 4.92
CHEMBL1215713 1 4.87
CHEMBL299112 1 4.82
CHEMBL1215576 1 4.53
CHEMBL1215507 1 4.35
CHEMBL1097450 1 4.34
CHEMBL363325 1 4.31
CHEMBL1215647 1 4.20
CHEMBL1215577 1 4.14
CHEMBL1215574 1 4.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1097451 EC50 = 7610.0 nM 5.12
CHEMBL1215644 EC50 = 12000.0 nM 4.92
CHEMBL1215713 EC50 = 13600.0 nM 4.87
CHEMBL299112 EC50 = 15100.0 nM 4.82
CHEMBL1215576 EC50 = 29500.0 nM 4.53
CHEMBL1215507 EC50 = 45000.0 nM 4.35
CHEMBL1097450 EC50 = 46000.0 nM 4.34
CHEMBL363325 EC50 = 49100.0 nM 4.31
CHEMBL1215647 EC50 = 63000.0 nM 4.20
CHEMBL1215577 EC50 = 72000.0 nM 4.14
CHEMBL1215574 EC50 = 85800.0 nM 4.07