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Assay Detail

CHEMBL989874

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

Functional
Enhancement of calcein-AM uptake in MDCK2 cells over expressing MDR1 after 20 mins
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Cell Type MDCK-II
Confidence 1 — Organism
Curated By Autocuration

Target

MDCK-II (CHEMBL4296466)
Type CELL-LINE
Organism Canis lupus familiaris

Publication

Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells.
Sawada GA, Raub TJ, William Higgins J, Brennan NK, Moore TM, Tombline G, Detty MR.
Bioorg Med Chem (2008) 16 : 9745 -9756
PubMed 18849167 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 4.93 5.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6966 VERAPAMIL 4.0 1 5.29
CHEMBL457023 1 5.27
CHEMBL436099 1 5.17
CHEMBL229938 1 5.15
CHEMBL229404 1 5.01
CHEMBL461674 1 4.85
CHEMBL229402 1 4.80
CHEMBL460394 1 4.70
CHEMBL460395 1 4.60
CHEMBL462522 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6966 VERAPAMIL EC50 = 5100.0 nM 5.29
CHEMBL457023 EC50 = 5400.0 nM 5.27
CHEMBL436099 EC50 = 6700.0 nM 5.17
CHEMBL229938 EC50 = 7100.0 nM 5.15
CHEMBL229404 EC50 = 9800.0 nM 5.01
CHEMBL461674 EC50 = 14000.0 nM 4.85
CHEMBL229402 EC50 = 16000.0 nM 4.80
CHEMBL460394 EC50 = 20000.0 nM 4.70
CHEMBL460395 EC50 = 25000.0 nM 4.60
CHEMBL462522 EC50 = 35000.0 nM 4.46