| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA925845 | B | Inhibition of human URAT1-mediated urate uptake in HEK293 cells | Homo sapiens | 4 | cell-based format | Scientific Literature | ||
| 2. | ALA925846 | B | Inhibition of human URAT1-mediated urate uptake in HEK293 cells at 2 uM | Homo sapiens | 2 | cell-based format | Scientific Literature | ||
| 3. | ALA925847 | B | Inhibition of human URAT1-mediated urate uptake in HEK293 cells by competitive inhibition assay | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 4. | ALA1638722 | B | Inhibition of human URAT-1 assessed as increase in renal uric acid excretion | Homo sapiens | 1 | tissue-based format | Scientific Literature | ||
| 5. | ALA1767807 | B | Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake at 50 uM after 60 mins by liquid scintillation counting | Homo sapiens | 42 | assay format | Scientific Literature | ||
| 6. | ALA1767808 | B | Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting | Homo sapiens | 42 | assay format | Scientific Literature | ||
| 7. | ALA1767809 | B | Inhibition of human URAT1 expressed in human MDCK cells | Homo sapiens | 2 | cell-based format | Scientific Literature | ||
| 8. | ALA3706173 | B | Inhibition Assay: URAT1 (Uric Acid Transporter 1) is expressed on the apical membrane in renal tubules. It mediates the re-uptake of uric acid from the urine into the blood. Inhibition of URAT1 leads to increased excretion of uric acid in the urine, and is therefore a potential mode of action for drugs that lower serum uric acid concentrations. Probenecid and Benzbromarone, for example, have been used clinically for treatment of gout and hyperuricemia, and they both act on URAT1 to reduce uric acid reuptake. However, benzbromarone was withdrawn from the market due to liver toxicity via mechanisms independent of URAT1, and probenecid acts on numerous transporter proteins, resulting in interactions with a variety of other drugs.An in vitro URAT1 assay is useful for identifying compounds with potential activity in lowering serum uric acid. A suitable assay involves transfection of cells (e g human embryonic kidney cells "HEK") with a vector encoding human URAT1. | 7 | cell-based format | BindingDB Database | |||
| 9. | ALA3705755 | B | Inhibition Assay: It was introduced human URAT1 full-length cDNA into an expression vector pcDNA5 / FRT / V5-His TOPO (registered trademark) (Invitrogen). The resulting expression plasmids, the liposome method using Lipofectamine LTX (Invitrogen), Chinese hamster ovary cells (hereinafter, referred to as CHO cells) was introduced into, by culturing in a selective medium containing hygromycin and human URAT1 stable The expression cell line we were prepared.Human URAT1 expression CHO cells, 10% fetal calf serum, D-MEM / F-12 containing the hygromycin (1: 1) using a mixed medium, 37 C, were cultured in the presence of 5% CO2. Cells were seeded in 96-well plates (Corning Incorporated) in 0.8x10E+5 cells / well, were subjected to the following uric acid transport inhibition test after 24 hours.After removal of the medium by aspiration, sodium gluconate of cells 125mM, potassium gluconate of 4.8mM, potassium dihydrogen phosphate of 1.2mM, magnesium sulfate of 1.2mM, calcium gluconate of 1.3mM, 5. washed once. | 72 | cell-based format | BindingDB Database | |||
| 10. | ALA3706306 | B | Inhibition Assay: Assay compound plates were prepared by diluting the compounds of formula (I) with chloride-free buffer (125 mM Na-gluconate, 4.8 mM K-gluconate, 1.3 mM Ca-gluconate, 1.2 mM KH2PO4, 1.2 mM MgSO4, 5.6 mM D-glucose, 25 mM HEPES, pH 7.4 with NaOH) in 100% DMSO to a final concentration of 1% DMSO. [14C]-Uric Uric acid working stock was made by addition of radiolabeled compound to a final concentration of 120 nM in chloride-free buffer. In all wells, the final assay concentration of solvent (DMSO) was 0.25%; the final assay concentration of [14C]-uric acid was 30 nM in chloride-free buffer and the final compound of formula (I) concentrations ranged from 0 to 10 uM. The vehicle comparator was DMSO (i.e. no inhibition of uric acid transport) and the pharmacological blockade (i.e. 100% inhibition of uric acid transport) was defined by benzbromarone at 10 uM final assay concentration.After pre-incubation, cells were washed with 50 uL of chloride-free buffer. | 241 | assay format | BindingDB Database | |||
| 11. | ALA3750816 | B | Inhibition of human URAT1 expressed in HEK293 cells assessed as [14C]uric acid uptake after 12 mins by scintillation counter | Homo sapiens | 35 | cell-based format | Scientific Literature | ||
| 12. | ALA3853443 | B | Inhibition of human C-terminal eGFP-tagged URAT1 long isoform expressed in CHO cells assessed as decrease in [14C]-uric acid uptake preincubated for 15 mins followed by [14C]-uric acid addition and incubated in dark for 3 hrs by scintillation counting method | Homo sapiens | 25 | cell-based format | Scientific Literature | ||
| 13. | ALA3853546 | B | Inhibition of URAT1 (unknown origin) | Homo sapiens | 6 | single protein format | Scientific Literature | ||
| 14. | ALA3853547 | B | Inhibition of URAT1 (unknown origin) expressed in HEK293 cells assessed as suppression of [14C]-uric acid uptake preincubated for 15 mins followed by [14C]-uric acid addition measured after 2 mins by liquid scintillation counting | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 15. | ALA3853552 | B | Inhibition of human C-terminal eGFP-tagged URAT1 long isoform expressed in CHO cells assessed as decrease in [14C]-uric acid uptake preincubated for 15 mins followed by [14C]-uric acid addition and incubated in dark for 3 hrs by scintillation counting method | Homo sapiens | 36 | cell-based format | Scientific Literature | ||
| 16. | ALA3870269 | B | Inhibition of URAT1 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]-uric acid uptake at 100 uM preincubated for 30 mins followed by [14C]-uric acid addition by liquid scintillation counting analysis relative to control | Homo sapiens | 10 | cell-based format | Scientific Literature | ||
| 17. | ALA3888910 | B | Cellular Uptake 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.). 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). | 4 | cell-based format | BindingDB Database | |||
| 18. | ALA4002435 | B | 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 | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 19. | ALA4015147 | B | 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 | Homo sapiens | 22 | cell-based format | Scientific Literature | ||
| 20. | ALA4015161 | B | Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake at 30 uM after 5 mins by liquid scintillation counting method relative to control | Homo sapiens | 1 | cell-based format | Scientific Literature |
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