lesinurad [Ligand Id: 7673] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2105720 (Lesinurad, RDEA594, RDEA 594, RDEA-594, Zurampic)
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  • Organic anion transporter 4/Solute carrier family 22 member 11 in Human [ChEMBL: CHEMBL2073677] [GtoPdb: 1030] [UniProtKB: Q9NSA0]
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  • Urate anion exchanger 1/Solute carrier family 22 member 12 in Human [ChEMBL: CHEMBL6120] [GtoPdb: 1031] [UniProtKB: Q96S37]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 4.52 pIC50 >30000 nM IC50 ACS Med Chem Lett (2017) 8: 299-303 [PMID:28337320]
ChEMBL Inhibition of human ERG B 4.52 pIC50 >30000 nM IC50 ACS Med Chem Lett (2017) 8: 299-303 [PMID:28337320]
ChEMBL Inhibition of human ERG B 4.52 pIC50 >30000 nM IC50 ACS Med Chem Lett (2017) 8: 299-303 [PMID:28337320]
Organic anion transporter 4/Solute carrier family 22 member 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073677] [GtoPdb: 1030] [UniProtKB: Q9NSA0]
ChEMBL Inhibition of OAT4 (unknown origin) B 5.14 pIC50 7300 nM IC50 Eur J Med Chem (2019) 166: 186-196 [PMID:30769179]
ChEMBL Inhibition of human OAT4 expressed in HEK293 cells by assessed as [14C]urate uptake preincubated for 5 mins followed by [14C]urate addition and measured after 10 mins by liquid scintillation counting method B 5.69 pIC50 2030 nM IC50 J Med Chem (2020) 63: 3834-3867 [PMID:31774679]
Urate anion exchanger 1/Solute carrier family 22 member 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6120] [GtoPdb: 1031] [UniProtKB: Q96S37]
ChEMBL Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method B 4.82 pIC50 15100 nM IC50 ACS Med Chem Lett (2017) 8: 299-303 [PMID:28337320]
ChEMBL Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition by liquid scintillation counting method B 4.88 pIC50 13210 nM IC50 J Med Chem (2020) 63: 10829-10854 [PMID:32897699]
ChEMBL Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method B 5.14 pIC50 7300 nM IC50 ACS Med Chem Lett (2017) 8: 299-303 [PMID:28337320]
ChEMBL Inhibition of human URAT1 B 5.14 pIC50 7300 nM IC50 Bioorg Med Chem Lett (2019) 29: 383-388 [PMID:30579795]
ChEMBL Inhibition of human URAT1 expressed in HEK293 cells assessed as reduction in [8-14C]uric acid uptake B 5.14 pIC50 7200 nM IC50 Bioorg Med Chem Lett (2019) 29: 383-388 [PMID:30579795]
ChEMBL Inhibition of URAT1 (unknown origin) B 5.17 pIC50 6700 nM IC50 MedChemComm (2016) 7: 1587-1595
ChEMBL Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method B 5.36 pIC50 4400 nM IC50 ACS Med Chem Lett (2017) 8: 299-303 [PMID:28337320]
ChEMBL Inhibition of URAT1 (unknown origin) B 5.43 pIC50 3700 nM IC50 Eur J Med Chem (2019) 166: 186-196 [PMID:30769179]
ChEMBL Inhibition of human URAT1 expressed in HEK293T cells by assessed as [14C]urate uptake preincubated for 5 mins followed by [14C]urate addition and measured after 10 mins by liquid scintillation counting method B 5.45 pIC50 3530 nM IC50 J Med Chem (2020) 63: 3834-3867 [PMID:31774679]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]