lesinurad [Ligand Id: 7673] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 mediated 14C-uric acid uptake expressed in HEK293 cells using 14C-uric acid as substrate incubated for 30 mins by liquid scintillation counting analysis | B | 5.03 | pIC50 | 9380 | nM | IC50 | Eur J Med Chem (2022) 244: 114816-114816 [PMID:36219903] |
| 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 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 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 mediated 14C-uric acid uptake expressed in HEK293 cells using 14C-uric acid as substrate incubated for 30 mins by liquid scintillation counter | B | 5.26 | pIC50 | 5540 | nM | IC50 | J Med Chem (2022) 65: 4218-4237 [PMID:35084182] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
