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Assay Detail

CHEMBL2078135

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Functional
TP_TRANSPORTER: inhibition of TEA uptake in OCT2-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

Solute carrier family 22 member 2 (CHEMBL1770032)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules.
Urakami Y, Okuda M, Masuda S, Akazawa M, Saito H, Inui K.
Pharm Res (2001) 18 : 1528 -1534
PubMed 11758759 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 4.76 5.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL945 AMILORIDE 4.0 1 5.33
CHEMBL517 DISOPYRAMIDE 4.0 1 4.52
CHEMBL640 PROCAINAMIDE 4.0 1 4.44
CHEMBL679 EPINEPHRINE 4.0 1 -
CHEMBL90 HISTAMINE 4.0 1 -
CHEMBL39 SEROTONIN 3.0 1 -
CHEMBL59 DOPAMINE 4.0 1 -
CHEMBL1547 THIAMINE ION 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL945 AMILORIDE Ki = 4700.0 nM 5.33
CHEMBL517 DISOPYRAMIDE Ki = 30000.0 nM 4.52
CHEMBL640 PROCAINAMIDE Ki = 36000.0 nM 4.44
CHEMBL679 EPINEPHRINE Ki = 1191000.0 nM -
CHEMBL90 HISTAMINE Ki = 171000.0 nM -
CHEMBL39 SEROTONIN Ki = 242000.0 nM -
CHEMBL59 DOPAMINE Ki = 347000.0 nM -
CHEMBL1547 THIAMINE ION Ki = 646000.0 nM -