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Assay Detail

CHEMBL2154123

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

ADMET
Inhibition of human MATE1 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Multidrug and toxin extrusion protein 1 (CHEMBL1743126)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
Kido Y, Matsson P, Giacomini KM.
J Med Chem (2011) 54 : 4548 -4558
PubMed 21599003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.14 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL46 ONDANSETRON 4.0 1 6.82
CHEMBL95 TACRINE 4.0 1 5.96
CHEMBL30 CIMETIDINE 4.0 1 5.24
CHEMBL11 IMIPRAMINE 4.0 1 5.00
CHEMBL932 DIPYRIDAMOLE 4.0 1 4.58
CHEMBL900 ORPHENADRINE 4.0 1 4.19
CHEMBL517 DISOPYRAMIDE 4.0 1 4.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL46 ONDANSETRON IC50 = 150.0 nM 6.82
CHEMBL95 TACRINE IC50 = 1100.0 nM 5.96
CHEMBL30 CIMETIDINE IC50 = 5700.0 nM 5.24
CHEMBL11 IMIPRAMINE IC50 = 10000.0 nM 5.00
CHEMBL932 DIPYRIDAMOLE IC50 = 26000.0 nM 4.58
CHEMBL900 ORPHENADRINE IC50 = 65000.0 nM 4.19
CHEMBL517 DISOPYRAMIDE IC50 = 66000.0 nM 4.18