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Assay Detail

CHEMBL5380230

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

Binding
Inhibition of human recombinant P-gp ATPase activity in isolated membranes incubated in presence of verapamil by firefly luciferase based luminescence analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Consensus screening for a challenging target: the quest for P-glycoprotein inhibitors.
Governa P, Biagi M, Manetti F, Forli S.
RSC Med Chem (2024) 15 : 720 -732
PubMed 38389870 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.37 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5426932 1 5.89
CHEMBL5399482 1 5.62
CHEMBL5409299 1 5.50
CHEMBL5437506 1 5.48
CHEMBL5402786 1 5.32
CHEMBL5394140 1 5.30
CHEMBL5405630 1 5.10
CHEMBL487805 SCUTELLARIN 1 4.71
CHEMBL5403462 1 -
CHEMBL5420251 1 -
CHEMBL5417022 1 -
CHEMBL5400953 1 -
CHEMBL5401400 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5426932 IC50 = 1280.0 nM 5.89
CHEMBL5399482 IC50 = 2400.0 nM 5.62
CHEMBL5409299 IC50 = 3170.0 nM 5.50
CHEMBL5437506 IC50 = 3310.0 nM 5.48
CHEMBL5402786 IC50 = 4800.0 nM 5.32
CHEMBL5394140 IC50 = 4990.0 nM 5.30
CHEMBL5405630 IC50 = 7900.0 nM 5.10
CHEMBL487805 SCUTELLARIN IC50 = 19710.0 nM 4.71
CHEMBL5403462 IC50 > 50000.0 nM -
CHEMBL5420251 IC50 > 50000.0 nM -
CHEMBL5417022 IC50 > 50000.0 nM -
CHEMBL5400953 IC50 > 50000.0 nM -
CHEMBL5401400 IC50 > 50000.0 nM -