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Assay Detail

CHEMBL4044308

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Binding
Inhibition of bovine milk xanthine oxidase pre-incubated for 30 mins followed by xanthine addition and measured every 30 secs for 5 mins by spectrophotometry
17
Total Activities
17
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

Synthesis and evaluation of hydroxychalcones as multifunctional non-purine xanthine oxidase inhibitors for the treatment of hyperuricemia.
Xie Z, Luo X, Zou Z, Zhang X, Huang F, Li R, Liao S, Liu Y.
Bioorg Med Chem Lett (2017) 27 : 3602 -3606
PubMed 28655421 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.21 4.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1467 ALLOPURINOL 4.0 1 4.71
CHEMBL129795 ISOLIQUIRITIGENIN 1 4.33
CHEMBL148472 1 4.25
CHEMBL32147 2'-HYDROXYCHALCONE 1 4.15
CHEMBL126804 1 4.10
CHEMBL150755 1 4.06
CHEMBL4088114 1 4.05
CHEMBL3823220 1 4.04
CHEMBL2282149 1 -
CHEMBL147067 1 -
CHEMBL388322 3-HYDROXY CHALCONE 1 -
CHEMBL7747 4-HYDROXYCHALCONE 1 -
CHEMBL105310 2',4'-DIHYDROXYCHALCONE 1 -
CHEMBL4066829 1 -
CHEMBL1083821 1 -
CHEMBL165 RESVERATROL 3.0 1 -
CHEMBL145927 4,4'-DIHYDROXYCHALCONE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1467 ALLOPURINOL IC50 = 19600.0 nM 4.71
CHEMBL129795 ISOLIQUIRITIGENIN IC50 = 47300.0 nM 4.33
CHEMBL148472 IC50 = 56800.0 nM 4.25
CHEMBL32147 2'-HYDROXYCHALCONE IC50 = 71300.0 nM 4.15
CHEMBL126804 IC50 = 79400.0 nM 4.10
CHEMBL150755 IC50 = 87400.0 nM 4.06
CHEMBL4088114 IC50 = 88300.0 nM 4.05
CHEMBL3823220 IC50 = 91800.0 nM 4.04
CHEMBL2282149 IC50 = 165000.0 nM -
CHEMBL147067 IC50 = 145000.0 nM -
CHEMBL388322 3-HYDROXY CHALCONE IC50 = 228000.0 nM -
CHEMBL7747 4-HYDROXYCHALCONE IC50 = 159000.0 nM -
CHEMBL105310 2',4'-DIHYDROXYCHALCONE IC50 = 107000.0 nM -
CHEMBL4066829 IC50 = 133000.0 nM -
CHEMBL1083821 IC50 = 108000.0 nM -
CHEMBL165 RESVERATROL IC50 - -
CHEMBL145927 4,4'-DIHYDROXYCHALCONE IC50 = 117000.0 nM -