Assay Detail
Binding
CHEMBL3706306
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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.
243
Total Activities
241
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Chemical compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 243 | 6.81 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3688197 | — | — | 1 | 9.00 |
| CHEMBL3688190 | — | — | 1 | 8.70 |
| CHEMBL3688192 | — | — | 1 | 8.52 |
| CHEMBL3683365 | — | — | 2 | 8.15 |
| CHEMBL3688188 | — | — | 1 | 8.10 |
| CHEMBL3688185 | — | — | 1 | 7.92 |
| CHEMBL3683287 | — | — | 1 | 7.89 |
| CHEMBL3683388 | — | — | 1 | 7.82 |
| CHEMBL3683364 | — | — | 1 | 7.72 |
| CHEMBL3948311 | — | — | 1 | 7.68 |
| CHEMBL3683399 | — | — | 1 | 7.62 |
| CHEMBL3683356 | — | — | 1 | 7.60 |
| CHEMBL3683348 | — | — | 1 | 7.57 |
| CHEMBL3683357 | — | — | 1 | 7.57 |
| CHEMBL3683383 | — | — | 1 | 7.54 |
| CHEMBL3683481 | — | — | 1 | 7.43 |
| CHEMBL3683482 | — | — | 1 | 7.43 |
| CHEMBL3683416 | — | — | 1 | 7.42 |
| CHEMBL3683347 | — | — | 1 | 7.41 |
| CHEMBL3683428 | — | — | 1 | 7.40 |
| CHEMBL3683363 | — | — | 1 | 7.37 |
| CHEMBL3683425 | — | — | 1 | 7.37 |
| CHEMBL3683297 | — | — | 1 | 7.33 |
| CHEMBL3683333 | — | — | 1 | 7.30 |
| CHEMBL3683436 | — | — | 1 | 7.30 |
| CHEMBL3683451 | — | — | 1 | 7.30 |
| CHEMBL3683441 | — | — | 1 | 7.29 |
| CHEMBL3683329 | — | — | 1 | 7.28 |
| CHEMBL3683432 | — | — | 1 | 7.28 |
| CHEMBL3683479 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3688197 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3688190 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3688192 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3683365 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3688188 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3688185 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3683365 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3683287 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3683388 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3683364 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3948311 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3683399 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3683356 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3683357 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3683348 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3683383 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3683482 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3683481 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3683416 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3683347 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3683428 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3683363 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3683425 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3683297 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3683451 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3683333 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3683436 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3683441 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3688184 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3683432 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3683479 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3683329 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3683324 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3683312 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3683305 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3683391 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3683362 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3688183 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3683293 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3683398 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3683395 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3683480 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3683299 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3683426 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3683358 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL3683317 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL3683320 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3683427 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3683325 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3683307 | — | IC50 | = | 84.0 | nM | 7.08 |