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Assay Detail

CHEMBL4731278

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

Toxicity
Hepatotoxicity in rat liver mitochondria assessed as inhibition of mitochondrial respiration by measuring mitochondrial respiratory control ratio of oxygen consumption in presence of substrate and ADP to rate after complete conversion of ADP to ATP by Clark-type oxygen electrode method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Rattus norvegicus
Tissue Liver
Subcellular Mitochondria
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

ADMET (CHEMBL612558)
Type ADMET

Publication

Discovery of Dotinurad (FYU-981), a New Phenol Derivative with Highly Potent Uric Acid Lowering Activity.
Uda J,Kobashi S,Miyata S,Ashizawa N,Matsumoto K,Iwanaga T
ACS Med Chem Lett (2020) 11 : 2017 -2023
PubMed 33062187 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.64 5.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388590 BENZBROMARONE 4.0 1 5.51
CHEMBL4781629 1 5.44
CHEMBL4753182 1 5.18
CHEMBL4781818 1 4.92
CHEMBL4748804 1 4.75
CHEMBL4796568 1 4.62
CHEMBL4594446 DOTINURAD 3.0 1 4.57
CHEMBL4744854 1 4.51
CHEMBL4790389 1 4.43
CHEMBL4785752 1 4.40
CHEMBL4796932 1 4.28
CHEMBL4744184 1 4.26
CHEMBL4740995 1 4.23
CHEMBL4760971 1 4.23
CHEMBL4778323 1 4.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388590 BENZBROMARONE IC50 = 3100.0 nM 5.51
CHEMBL4781629 IC50 = 3600.0 nM 5.44
CHEMBL4753182 IC50 = 6600.0 nM 5.18
CHEMBL4781818 IC50 = 12000.0 nM 4.92
CHEMBL4748804 IC50 = 18000.0 nM 4.75
CHEMBL4796568 IC50 = 24000.0 nM 4.62
CHEMBL4594446 DOTINURAD IC50 = 27000.0 nM 4.57
CHEMBL4744854 IC50 = 31000.0 nM 4.51
CHEMBL4790389 IC50 = 37000.0 nM 4.43
CHEMBL4785752 IC50 = 40000.0 nM 4.40
CHEMBL4796932 IC50 = 53000.0 nM 4.28
CHEMBL4744184 IC50 = 55000.0 nM 4.26
CHEMBL4740995 IC50 = 59000.0 nM 4.23
CHEMBL4760971 IC50 = 59000.0 nM 4.23
CHEMBL4778323 IC50 = 63000.0 nM 4.20