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Assay Detail

CHEMBL974429

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

Binding
Inhibition of verapamil-stimulated ATPase activity of human histidine10-tagged MDR1 expressed in BHK cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Rhodamine inhibitors of P-glycoprotein: an amide/thioamide "switch" for ATPase activity.
Gannon MK, Holt JJ, Bennett SM, Wetzel BR, Loo TW, Bartlett MC, Clarke DM, Sawada GA, Higgins JW, Tombline G, Raub TJ, Detty MR.
J Med Chem (2009) 52 : 3328 -3341
PubMed 19402665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.29 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL450642 1 6.17
CHEMBL490121 1 5.64
CHEMBL522826 1 5.28
CHEMBL491577 1 5.17
CHEMBL495469 1 5.10
CHEMBL492602 1 5.05
CHEMBL522966 1 4.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL450642 IC50 = 670.0 nM 6.17
CHEMBL490121 IC50 = 2300.0 nM 5.64
CHEMBL522826 IC50 = 5300.0 nM 5.28
CHEMBL491577 IC50 = 6800.0 nM 5.17
CHEMBL495469 IC50 = 7900.0 nM 5.10
CHEMBL492602 IC50 = 9000.0 nM 5.05
CHEMBL522966 IC50 = 23600.0 nM 4.63