ChEMBL ligand: CHEMBL2105720 (Lesinurad, Lesinurad component of duzallo, RDEA 594, RDEA-594, RDEA594, Zurampic)
Organic anion transporter 4/Solute carrier family 22 member 11 in Human [ChEMBL: CHEMBL2073677] [GtoPdb: 1030] [UniProtKB: Q9NSA0] There should be some charts here, you may need to enable JavaScript!
Urate anion exchanger 1/Solute carrier family 22 member 12 in Human [ChEMBL: CHEMBL6120] [GtoPdb: 1031] [UniProtKB: Q96S37] There should be some charts here, you may need to enable JavaScript!
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
xanthine dehydrogenase/Xanthine dehydrogenase/oxidase in Human [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
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 OAT4 (unknown origin)	B	5.43	pIC50	3700	nM	IC50	Eur J Med Chem (2023) 245: 114890-114890 [PMID:36335742]
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	In Vitro Urat1 Assay: A plasmid (EX-T4563-M03, GeneCopoeia) containing the full-length human URAT1 gene (SLC22A12) was transfected into Flp-InT-REx-293 cells to construct URAT1 high-expression cell 293/hURAT1. The transfected cells were assayed for ability to uptake uric acid labelled with radioisotope. The test compounds were then evaluated for their activity by determining of their ability to block uric acid uptake by the transfected cells.293/h URAT1 cells were plated at a density of 40000 cells/well in poly D-lysine-coated 96-well plates (BD, 356461) and incubated overnight. The medium was removed and a pre-warmed reaction buffer was added (125 mM sodium gluconate, 4.8 mM potassium gluconate, 1.3 mM calcium gluconate, 1.2 mM potassium dihydrogen phosphate, 1.2 mM magnesium sulfate, 5.6 mM glucose, 25 mM HEPES, pH 7.4) before incubating at 37° C. for 10 minutes. The buffer was removed and another reaction buffer containing 50 μM 14C-uric acid (American Radiolabeled Chemicals, ARC0513) and the test compounds or solvent control was added before incubating at 37° C. for 5 minutes. The buffer was removed, and the plates were washed 3 times with the buffer. Cells were lysed by adding 100 mM NaOH for 20 minutes. Cell lysates were transferred to Isoplate-96 well plates (PerkinElmer, 6005040), mixed with liquid scintillators and were counted in a MicroBeta2 (PerkinElmer) counter.The test compounds were all dissolved in DMSO, and DMSO of the same concentration without the test compounds was used as a solvent control. The amount of uric acid uptake by the cells in the DMSO solvent control was taken as 100%, and the inhibition of uric acid uptake by cells in the test wells for each compound was calculated as a percentage. The IC50 of each compound was calculated using the percentage of inhibition at different concentrations.	B	4.19	pIC50	65000	nM	IC50	US-10336710-B2. Benzimidazole derivatives, preparation method therefor, and applications thereof (2019)
ChEMBL	xanthine oxidase activity: Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan M P: Int J Biochem. 10:317-9, 1979) with minor variations. The procedure was internally standardized using allopurinol and DPI as controls for all experiments after determination of their optimal inhibitory concentrations. Experiments on test compounds were performed in triplicate in multi-well plates using 10 concentrations of each compound that ranged over a 3-fold dilution.	B	4.28	pIC50	52500	nM	IC50	US-10093658-B2. Bifunctional compounds and use for reducing uric acid levels (2018)
ChEMBL	URAT1 activity assay: URAT1 (SLC22A12) activity was evaluated in a cellular uptake assay using a 96-well plate with stably transfected URAT-1/CHO cells. 3H-orotate was used as the test transport agent, which was measured in a liquid scintillation counter, using benzbromarone as a positive control, and DMSO and non-transfected CHO cells as negative controls (Solvo Biotechnology, Boston, Mass.). Generally determined over 7 concentrations (range, 0.01 to 150 μM), a semi-log plot (percent relative transport of oratate vs. time) was generated to determine the concentration at which 50% inhibition was observed (i.e., the IC50).	B	4.73	pIC50	18610	nM	IC50	US-11020397-B2. Compounds and their use for reducing uric acid levels (2021)
ChEMBL	URAT1 activity: URAT1 (SLC22A12) activity was evaluated in a cellular uptake assay using a 96-well plate with stably transfected URAT-1/CHO cells. 3H-orotate was used as the test transport agent, which was measured in a liquid scintillation counter, using benzbromarone as a positive control, and DMSO and non-transfected CHO cells as negative controls (Solvo Biotechnology, Boston, Mass.). Generally determined over 7 concentrations (range, 0.01 to 150 μM), a semi-log plot (percent relative transport of oratate vs. time) was generated to determine the concentration at which 50% inhibition was observed (i.e., the IC50).	B	4.73	pIC50	18610	nM	IC50	US-10752613-B2. Compounds and their use for reducing uric acid levels (2020)
ChEMBL	URAT1 activity assay: URAT1 (SLC22A12) activity was evaluated in a cellular uptake assay using a 96-well plate with stably transfected URAT-1/CHO cells. 3H-orotate was used as the test transport agent, which was measured in a liquid scintillation counter, using benzbromarone as a positive control, and DMSO and non-transfected CHO cells as negative controls (Solvo Biotechnology, Boston, Mass.). Generally determined over 7 concentrations (range, 0.01 to 150 μM), a semi-log plot (percent relative transport of oratate vs. time) was generated to determine the concentration at which 50% inhibition was observed (i.e., the IC50).	B	4.73	pIC50	18610	nM	IC50	US-11020397-B2. Compounds and their use for reducing uric acid levels (2021)
ChEMBL	URAT1 activity: URAT1 (SLC22A12) activity was evaluated in a cellular uptake assay using a 96-well plate with stably transfected URAT-1/CHO cells. 3H-orotate was used as the test transport agent, which was measured in a liquid scintillation counter, using benzbromarone as a positive control, and DMSO and non-transfected CHO cells as negative controls (Solvo Biotechnology, Boston, Mass.). Generally determined over 7 concentrations (range, 0.01 to 150 μM), a semi-log plot (percent relative transport of oratate vs. time) was generated to determine the concentration at which 50% inhibition was observed (i.e., the IC50).	B	4.73	pIC50	18610	nM	IC50	US-10093658-B2. Bifunctional compounds and use for reducing uric acid levels (2018)
ChEMBL	URAT1 (SLC22A12) activity: URAT1 (SLC22A12) activity was evaluated in a cellular uptake assay using a 96-well plate with stably transfected URAT-1/CHO cells. 3H-orotate was used as the test transport agent, which was measured in a liquid scintillation counter, using benzbromarone as a positive control, and DMSO and non-transfected CHO cells as negative controls (Solvo Biotechnology, Boston, Mass.). Over 7 concentrations (range, 0.01 to 150 μM), a semi-log plot (percent relative transport of oratate vs. time) was generated to determine the concentration at which 50% inhibition was observed (i.e., the IC50).	B	4.73	pIC50	18600	nM	IC50	US-10093631-B2. Bifunctional compounds and use for reducing uric acid levels (2018)
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 stably overexpressing in human HEK293 cells assessed as inhibition of 14C-uric acid uptake preincubated for 30 mins followed by substrate addition and measured after 15 mins using 14C-uric acid as substrate by liquid scintillation counting analysis	B	5.12	pIC50	7560	nM	IC50	Eur J Med Chem (2022) 242: 114682-114682 [PMID:36001935]
ChEMBL	Inhibition of URAT1 (unknown origin)	B	5.14	pIC50	7300	nM	IC50	Eur J Med Chem (2023) 245: 114890-114890 [PMID:36335742]
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 human URAT1 transfected in HEK293 cells by measuring 14C-uric acid uptake preincubated for 30 mins followed by 14--uric acid addition and measured after 15 mins by liquid scintillation counter analysis	B	5.14	pIC50	7180	nM	IC50	Eur J Med Chem (2024) 277: 116753-116753 [PMID:39142150]
ChEMBL	Inhibition of URAT1 (unknown origin)	B	5.14	pIC50	7180	nM	IC50	Eur J Med Chem (2024) 277: 116753-116753 [PMID:39142150]
ChEMBL	IC50 for Inhibition of the Test Compounds on URAT1: After trypsin digestion, the expression cells (HEK293) stably expressing URAT1 gene and mock cells were all inoculated into lysine-coated 24-well culture plates, with the cell inoculation density being 1×105 cells/well, and cultured in incubator at 37° C., 5% CO2 and saturated humidity for 2 days. The culture fluid in the culture plate was removed, and the cultured cells were washed twice with DPBS and subjected to warm bath in DPBS buffer solution at 37° C. for 10 min, and then a solution (500 μL) containing radioactive labeled probe substrate ([8-14C] uric acid) and 10 μM test compound (or blank) was used to substitute for DPBS, with the concentration of [8-14C] uric acid being 30 μM and the radiation intensity per well being 0.867 μCi. After 2 min, the reaction was terminated with ice-bathed DPBS buffer solution and washing was carried out for three times. Then 0.1 mol/L NaOH (500 μL) was added into each well to lyse the cells, the lysate was extracted into a scintillation vial and a scintillation fluid (Aquasol-2, 3 mL) was added, and the intensity of radioactivity in the sample was measured using a Tri-Carb 2910TR liquid scintillation analyzer (PerkinElmer, Waltham, USA). The concentration of a certain specific test compound was changed and a series of concentration points (nine concentration points were set between 0.001-10 μM) were set, to obtain the “inhibition rates” of the specific test compound at the above 9 concentration points. IC50 values for inhibition of the test compounds on URAT1 were calculated using the PRISM software based on the “inhibition rate” values of the test compound at different concentrations.	B	5.14	pIC50	7180	nM	IC50	US-10584104-B2. Carboxylic acid URAT1 inhibitor containing diarylmethane structure, preparation method and use thereof (2020)
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 HEK293T cells using 14C- uric acid assessed as uric acid absorption by measuring intracellular liquid radiation value by liquid scintillation counting analysis	B	5.26	pIC50	5540	nM	IC50	J Med Chem (2024) 67: 5032-5052 [PMID:38482820]
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]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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]
xanthine dehydrogenase/Xanthine dehydrogenase/oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989]
ChEMBL	xanthine oxidase activity assay: Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan M P: Int J Biochem. 10:317-9, 1979) with minor variations. The procedure was internally standardized using allopurinol and DPI as controls for all experiments after determination of their optimal inhibitory concentrations. Experiments on test compounds were performed in triplicate in multi-well plates using 10 concentrations of each compound that ranged over a 3-fold dilution.	B	6.52	pIC50	>300	nM	IC50	US-11020397-B2. Compounds and their use for reducing uric acid levels (2021)
ChEMBL	xanthine oxidase activity assay: Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan M P: Int J Biochem. 10:317-9, 1979) with minor variations. The procedure was internally standardized using allopurinol and DPI as controls for all experiments after determination of their optimal inhibitory concentrations. Experiments on test compounds were performed in triplicate in multi-well plates using 10 concentrations of each compound that ranged over a 3-fold dilution.	B	6.52	pIC50	>300	nM	IC50	US-11020397-B2. Compounds and their use for reducing uric acid levels (2021)

ChEMBL data shown on this page come from version 36:

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]