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Assay Detail

CHEMBL4015147

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

Binding
Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Solute carrier family 22 member 12 (CHEMBL6120)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of sulfonamide derivatives as potent Human Uric Acid Transporter 1 (hURAT1) inhibitors.
Yang X, Pang X, Fan L, Li X, Chen Y.
Bioorg Med Chem Lett (2017) 27 : 1919 -1922
PubMed 28351592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.22 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4087516 1 8.70
CHEMBL4088988 1 8.00
CHEMBL4100597 1 7.08
CHEMBL388590 BENZBROMARONE 4.0 1 6.92
CHEMBL4104410 1 6.90
CHEMBL4103898 1 6.69
CHEMBL4066146 1 6.67
CHEMBL4079640 1 6.62
CHEMBL4078667 1 6.58
CHEMBL4074756 1 6.41
CHEMBL4094280 1 6.22
CHEMBL4067774 1 6.15
CHEMBL4066753 1 5.96
CHEMBL4085591 1 5.85
CHEMBL4086514 1 5.70
CHEMBL4096139 1 5.55
CHEMBL4076833 1 5.44
CHEMBL4095219 1 5.40
CHEMBL4068847 1 5.39
CHEMBL4060192 1 5.01
CHEMBL4088415 1 4.92
CHEMBL4064028 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4087516 IC50 = 2.0 nM 8.70
CHEMBL4088988 IC50 = 10.0 nM 8.00
CHEMBL4100597 IC50 = 83.0 nM 7.08
CHEMBL388590 BENZBROMARONE IC50 = 120.0 nM 6.92
CHEMBL4104410 IC50 = 127.0 nM 6.90
CHEMBL4103898 IC50 = 203.0 nM 6.69
CHEMBL4066146 IC50 = 215.0 nM 6.67
CHEMBL4079640 IC50 = 241.0 nM 6.62
CHEMBL4078667 IC50 = 261.0 nM 6.58
CHEMBL4074756 IC50 = 390.0 nM 6.41
CHEMBL4094280 IC50 = 597.0 nM 6.22
CHEMBL4067774 IC50 = 713.0 nM 6.15
CHEMBL4066753 IC50 = 1100.0 nM 5.96
CHEMBL4085591 IC50 = 1400.0 nM 5.85
CHEMBL4086514 IC50 = 2000.0 nM 5.70
CHEMBL4096139 IC50 = 2827.0 nM 5.55
CHEMBL4076833 IC50 = 3600.0 nM 5.44
CHEMBL4095219 IC50 = 4000.0 nM 5.40
CHEMBL4068847 IC50 = 4059.0 nM 5.39
CHEMBL4060192 IC50 = 9836.0 nM 5.01
CHEMBL4088415 IC50 = 11999.0 nM 4.92
CHEMBL4064028 IC50 = 20900.0 nM 4.68