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Assay Detail

CHEMBL2076246

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

Functional
TP_TRANSPORTER: inhibition of TEA uptake (TEA: 10 uM) in Xenopus laevis oocytes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Xenopus laevis
Cell Type Oocyte
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1.
Arndt P, Volk C, Gorboulev V, Budiman T, Popp C, Ulzheimer-Teuber I, Akhoundova A, Koppatz S, Bamberg E, Nagel G, Koepsell H.
Am J Physiol Renal Physiol (2001) 281 : F454 -F468
PubMed 11502595 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.12 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2074851 Cyanine-863 1 6.29
CHEMBL170 QUININE 4.0 1 5.39
CHEMBL2074659 MEPIPERPHENIDOL BROMIDE -1.0 1 5.15
CHEMBL2074857 TETRAPROPYLAMMONIUM 1 4.95
CHEMBL1294 QUINIDINE 4.0 1 4.90
CHEMBL72 DESIPRAMINE 4.0 1 4.76
CHEMBL2074647 METIPRENALINE 2.0 1 4.43
CHEMBL463 AMINOHIPPURIC ACID 4.0 1 -
CHEMBL110739 CORTICOSTERONE 3.0 1 -
CHEMBL897 PROBENECID 4.0 1 -
CHEMBL821 GUANIDINE 4.0 1 -
CHEMBL1686 ALPHA-KETOGLUTARIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2074851 Cyanine-863 IC50 = 510.0 nM 6.29
CHEMBL170 QUININE IC50 = 4100.0 nM 5.39
CHEMBL2074659 MEPIPERPHENIDOL BROMIDE IC50 = 7100.0 nM 5.15
CHEMBL2074857 TETRAPROPYLAMMONIUM IC50 = 11300.0 nM 4.95
CHEMBL1294 QUINIDINE IC50 = 12700.0 nM 4.90
CHEMBL72 DESIPRAMINE IC50 = 17500.0 nM 4.76
CHEMBL2074647 METIPRENALINE IC50 = 37000.0 nM 4.43
CHEMBL463 AMINOHIPPURIC ACID IC50 = 1300000.0 nM -
CHEMBL110739 CORTICOSTERONE IC50 = 151000.0 nM -
CHEMBL897 PROBENECID IC50 = 1640000.0 nM -
CHEMBL821 GUANIDINE IC50 = 4470000.0 nM -
CHEMBL1686 ALPHA-KETOGLUTARIC ACID IC50 = 740000.0 nM -