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ChEMBL ligand: CHEMBL2105720 (Lesinurad, RDEA 594, RDEA-594, RDEA594, Zurampic) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]