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Assay Detail

CHEMBL5157441

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

Toxicity
Inhibition of OAT1 (unknown origin) expressed in HEK293 cells assessed as inhibition of 6-CFL uptake preincubated for 30 mins followed by incubation with 6-CFL and measured after 15 mins by fluorescence based analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Solute carrier family 22 member 6 (CHEMBL1641347)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel verinurad analogs as dual inhibitors of URAT1 and GLUT9 with improved Druggability for the treatment of hyperuricemia.
Zhao Z, Liu J, Kuang P, Luo J, Surineni G, Cen X, Wu T, Cao Y, Zhou P, Pang J, Zhang Q, Chen J.
Eur J Med Chem (2022) 229 : 114092 -114092
PubMed 34998055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.59 4.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5170470 1 4.89
CHEMBL5190525 1 4.59
CHEMBL5202967 1 4.49
CHEMBL5178161 1 4.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5170470 IC50 = 12740.0 nM 4.89
CHEMBL5190525 IC50 = 25540.0 nM 4.59
CHEMBL5202967 IC50 = 32140.0 nM 4.49
CHEMBL5178161 IC50 = 41250.0 nM 4.38