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Assay Detail

CHEMBL974426

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

Binding
Inhibition of verapamil-stimulated ATPase activity of mouse cysteine-less MDR3
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

ATP-dependent translocase ABCB1 (CHEMBL2573)
Type SINGLE PROTEIN
Organism Mus musculus

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 5.09 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490121 1 6.55
CHEMBL524129 1 5.34
CHEMBL523281 1 4.82
CHEMBL490549 1 4.68
CHEMBL493641 1 4.64
CHEMBL495469 1 4.50
CHEMBL491928 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490121 IC50 = 280.0 nM 6.55
CHEMBL524129 IC50 = 4600.0 nM 5.34
CHEMBL523281 IC50 = 15000.0 nM 4.82
CHEMBL490549 IC50 = 21000.0 nM 4.68
CHEMBL493641 IC50 = 23000.0 nM 4.64
CHEMBL495469 IC50 = 32000.0 nM 4.50
CHEMBL491928 IC50 > 120000.0 nM -