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Assay Detail

CHEMBL989869

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

Binding
Inhibition of verapamil-induced ATPase activity in lipid activated mouse P-glycoprotein mdr3 cys-less mutant assessed as ATP hydrolysis per ug of protein
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
IC50 15 5.23 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL462522 1 6.16
CHEMBL229938 1 6.06
CHEMBL229403 1 6.00
CHEMBL457023 1 5.92
CHEMBL457869 1 5.51
CHEMBL461674 1 5.28
CHEMBL461672 1 5.24
CHEMBL461671 1 5.10
CHEMBL148507 1 4.96
CHEMBL229402 1 4.82
CHEMBL514092 1 4.52
CHEMBL515523 1 4.26
CHEMBL457022 1 4.15
CHEMBL460395 1 -
CHEMBL229404 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL462522 IC50 = 700.0 nM 6.16
CHEMBL229938 IC50 = 880.0 nM 6.06
CHEMBL229403 IC50 = 1000.0 nM 6.00
CHEMBL457023 IC50 = 1200.0 nM 5.92
CHEMBL457869 IC50 = 3100.0 nM 5.51
CHEMBL461674 IC50 = 5300.0 nM 5.28
CHEMBL461672 IC50 = 5700.0 nM 5.24
CHEMBL461671 IC50 = 7900.0 nM 5.10
CHEMBL148507 IC50 = 11000.0 nM 4.96
CHEMBL229402 IC50 = 15000.0 nM 4.82
CHEMBL514092 IC50 = 30000.0 nM 4.52
CHEMBL515523 IC50 = 55000.0 nM 4.26
CHEMBL457022 IC50 = 71000.0 nM 4.15
CHEMBL460395 IC50 > 100000.0 nM -
CHEMBL229404 IC50 > 100000.0 nM -