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Assay Detail

CHEMBL4409380

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Binding
Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 10 mins followed by substrate addition measured at first 2 mins by spectrophotometric analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Xanthine dehydrogenase/oxidase (CHEMBL3649)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Design, synthesis and biological evaluation of N-(3-(1H-tetrazol-1-yl)phenyl)isonicotinamide derivatives as novel xanthine oxidase inhibitors.
Zhang TJ, Zhang Y, Tu S, Wu YH, Zhang ZH, Meng FH.
Eur J Med Chem (2019) 183 : 111717 -111717
PubMed 31557611 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.74 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1078685 TOPIROXOSTAT 2.0 1 7.68
CHEMBL4453043 1 7.51
CHEMBL4455392 1 7.36
CHEMBL4540231 1 7.30
CHEMBL4444577 1 7.28
CHEMBL4435696 1 7.17
CHEMBL4438449 1 7.04
CHEMBL4472263 1 7.03
CHEMBL4444217 1 7.00
CHEMBL4457729 1 6.96
CHEMBL4530455 1 6.93
CHEMBL4483545 1 6.89
CHEMBL4522159 1 6.88
CHEMBL4568537 1 6.85
CHEMBL4583393 1 6.84
CHEMBL4584553 1 6.82
CHEMBL4548828 1 6.78
CHEMBL4448296 1 6.77
CHEMBL4466230 1 6.76
CHEMBL4483371 1 6.76
CHEMBL4565144 1 6.58
CHEMBL4160962 1 6.51
CHEMBL4456880 1 6.22
CHEMBL4455804 1 5.68
CHEMBL4438198 1 5.54
CHEMBL4524769 1 5.41
CHEMBL4549903 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1078685 TOPIROXOSTAT IC50 = 21.0 nM 7.68
CHEMBL4453043 IC50 = 31.0 nM 7.51
CHEMBL4455392 IC50 = 44.0 nM 7.36
CHEMBL4540231 IC50 = 50.0 nM 7.30
CHEMBL4444577 IC50 = 53.0 nM 7.28
CHEMBL4435696 IC50 = 67.0 nM 7.17
CHEMBL4438449 IC50 = 92.0 nM 7.04
CHEMBL4472263 IC50 = 94.0 nM 7.03
CHEMBL4444217 IC50 = 100.0 nM 7.00
CHEMBL4457729 IC50 = 110.0 nM 6.96
CHEMBL4530455 IC50 = 117.0 nM 6.93
CHEMBL4483545 IC50 = 128.0 nM 6.89
CHEMBL4522159 IC50 = 132.0 nM 6.88
CHEMBL4568537 IC50 = 141.0 nM 6.85
CHEMBL4583393 IC50 = 145.0 nM 6.84
CHEMBL4584553 IC50 = 153.0 nM 6.82
CHEMBL4548828 IC50 = 165.0 nM 6.78
CHEMBL4448296 IC50 = 171.0 nM 6.77
CHEMBL4466230 IC50 = 174.0 nM 6.76
CHEMBL4483371 IC50 = 173.0 nM 6.76
CHEMBL4565144 IC50 = 264.0 nM 6.58
CHEMBL4160962 IC50 = 312.0 nM 6.51
CHEMBL4456880 IC50 = 603.0 nM 6.22
CHEMBL4455804 IC50 = 2100.0 nM 5.68
CHEMBL4438198 IC50 = 2890.0 nM 5.54
CHEMBL4524769 IC50 = 3860.0 nM 5.41
CHEMBL4549903 IC50 = 4590.0 nM 5.34