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Assay Detail

CHEMBL2078155

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

Functional
TP_TRANSPORTER: inhibition of PAH uptake in Xenopus laevis oocytes
8
Total Activities
8
Compounds Tested
2
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 6 (CHEMBL1777665)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Interaction and transport of thiazide diuretics, loop diuretics, and acetazolamide via rat renal organic anion transporter rOAT1.
Uwai Y, Saito H, Hashimoto Y, Inui KI.
J Pharmacol Exp Ther (2000) 295 : 261 -265
PubMed 10991988

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 4 - -
Ki 4 5.14 5.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1072 BUMETANIDE 4.0 1 5.26
CHEMBL35 FUROSEMIDE 4.0 1 5.02
CHEMBL19 METHAZOLAMIDE 4.0 1 -
CHEMBL18 ETHOXZOLAMIDE 4.0 1 -
CHEMBL61593 CYCLOTHIAZIDE 4.0 1 -
CHEMBL842 CHLOROTHIAZIDE 4.0 1 -
CHEMBL20 ACETAZOLAMIDE 4.0 1 -
CHEMBL435 HYDROCHLOROTHIAZIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1072 BUMETANIDE Ki = 5500.0 nM 5.26
CHEMBL35 FUROSEMIDE Ki = 9500.0 nM 5.02
CHEMBL19 METHAZOLAMIDE Activity - -
CHEMBL18 ETHOXZOLAMIDE Activity - -
CHEMBL61593 CYCLOTHIAZIDE Activity - -
CHEMBL842 CHLOROTHIAZIDE Activity - -
CHEMBL20 ACETAZOLAMIDE Ki = 1100000.0 nM -
CHEMBL435 HYDROCHLOROTHIAZIDE Ki = 150000.0 nM -