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Assay Detail

CHEMBL2077571

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

Functional
TP_TRANSPORTER: inhibition of TEA uptake (in the absence of bicarbonate) (TEA: 20 uM) in OCT1-expressing HEK293 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Solute carrier family 22 member 1 (CHEMBL2073670)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

The cation transporters rOCT1 and rOCT2 interact with bicarbonate but play only a minor role for amantadine uptake into rat renal proximal tubules.
Goralski KB, Lou G, Prowse MT, Gorboulev V, Volk C, Koepsell H, Sitar DS.
J Pharmacol Exp Ther (2002) 303 : 959 -968
PubMed 12438515 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.74 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2074851 Cyanine-863 1 6.35
CHEMBL170 QUININE 4.0 1 5.96
CHEMBL640 PROCAINAMIDE 4.0 1 4.92
CHEMBL660 AMANTADINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2074851 Cyanine-863 IC50 = 450.0 nM 6.35
CHEMBL170 QUININE IC50 = 1100.0 nM 5.96
CHEMBL640 PROCAINAMIDE IC50 = 12000.0 nM 4.92
CHEMBL660 AMANTADINE IC50 = 280000.0 nM -