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Assay Detail

CHEMBL2078148

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

Functional
TP_TRANSPORTER: inhibition of calcein-AM efflux in MDR1-expressing MDCK cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type MDCK
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1.
Chen C, Mireles RJ, Campbell SD, Lin J, Mills JB, Xu JJ, Smolarek TA.
Drug Metab Dispos (2005) 33 : 537 -546
PubMed 15616150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.85 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL503 LOVASTATIN 4.0 1 5.00
CHEMBL1064 SIMVASTATIN 4.0 1 5.00
CHEMBL333687 ATORVASTATIN LACTONE 1 4.85
CHEMBL159 VINBLASTINE 4.0 1 4.54
CHEMBL1201391 TENIVASTATIN 2.0 1 -
CHEMBL1201373 LOVASTATIN ACID -1.0 1 -
CHEMBL1790017 ATORVASTATIN ACID 1 -
CHEMBL1144 PRAVASTATIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL503 LOVASTATIN IC50 = 10000.0 nM 5.00
CHEMBL1064 SIMVASTATIN IC50 = 10000.0 nM 5.00
CHEMBL333687 ATORVASTATIN LACTONE IC50 = 14000.0 nM 4.85
CHEMBL159 VINBLASTINE IC50 = 29000.0 nM 4.54
CHEMBL1201391 TENIVASTATIN IC50 - -
CHEMBL1201373 LOVASTATIN ACID IC50 - -
CHEMBL1790017 ATORVASTATIN ACID IC50 - -
CHEMBL1144 PRAVASTATIN IC50 - -