Assay Detail
Binding
CHEMBL5736723
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Scintillation Proximity Assay (SPA: The scintillation proximity assay (SPA) was run in white polystyrene flat-bottom 384-well plates (Greiner, cat. No. 781075). Assays were carried out in 40 i1 reaction volumes. Various concentrations of test ligands in 0.4 microlitres of DMSO were added to assay plates using an acoustic liquid dispenser. 4 nM purified Nâ(HN)6-GST-TCS-hRORγ (258-518) was mixed with 40 micrograms Yttrium oxide (YOx) glutathione SPA imaging beads in assay buffer (20 mM Tris, 150 mM NaCl, 10% Glycerol, 0.25% CHAPS, 1 mM TCEP) prior to adding 30 microlitres to test ligands. Assay plates were incubated for one hour at room temperature before adding 10 microlitres tritiated 2-(4-(ethylsulfonyl)phenyl)-N-(4-(2-(methoxymethyl)phenyl)thiophen-2-yl)acetamide to test plates in assay buffer (final concentration, 25 nM). Test plates were incubated for 16 hours and read using a LEADseeker Multimodality imaging instrument.
465
Total Activities
136
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 155 | 6.75 | 7.50 |
| kon | 155 | - | - |
| k_off | 155 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5938751 | — | — | 3 | 7.50 |
| CHEMBL4857395 | — | — | 3 | 7.50 |
| CHEMBL4877500 | — | — | 9 | 7.40 |
| CHEMBL4857284 | — | — | 3 | 7.40 |
| CHEMBL5996139 | — | — | 3 | 7.40 |
| CHEMBL4864990 | — | — | 3 | 7.30 |
| CHEMBL4868864 | — | — | 3 | 7.30 |
| CHEMBL5812242 | — | — | 3 | 7.30 |
| CHEMBL4855387 | — | — | 3 | 7.30 |
| CHEMBL6026656 | — | — | 3 | 7.30 |
| CHEMBL5865301 | — | — | 3 | 7.30 |
| CHEMBL4847761 | — | — | 3 | 7.30 |
| CHEMBL4865776 | — | — | 3 | 7.20 |
| CHEMBL4878173 | — | — | 3 | 7.20 |
| CHEMBL6056242 | — | — | 3 | 7.20 |
| CHEMBL5960515 | — | — | 3 | 7.20 |
| CHEMBL4856430 | — | — | 3 | 7.20 |
| CHEMBL5819478 | — | — | 3 | 7.20 |
| CHEMBL5828228 | — | — | 3 | 7.20 |
| CHEMBL6056459 | — | — | 3 | 7.20 |
| CHEMBL5921331 | — | — | 3 | 7.20 |
| CHEMBL4869175 | — | — | 3 | 7.20 |
| CHEMBL4870856 | — | — | 3 | 7.20 |
| CHEMBL4876902 | — | — | 3 | 7.20 |
| CHEMBL5835688 | — | — | 3 | 7.20 |
| CHEMBL4865352 | — | — | 9 | 7.20 |
| CHEMBL5745189 | — | — | 3 | 7.20 |
| CHEMBL4872141 | — | — | 3 | 7.10 |
| CHEMBL5739946 | — | — | 3 | 7.10 |
| CHEMBL5800395 | — | — | 3 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4857395 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL5938751 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL5996139 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL4877500 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL4877500 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL4857284 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL4855387 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL4868864 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL5812242 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL6026656 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL5865301 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL4847761 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL4864990 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL4878173 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4865352 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4870856 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4865776 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4856430 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL6056242 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5960515 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5921331 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5819478 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4869175 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4876902 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL6056459 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5745189 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5835688 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4877500 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5828228 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4846059 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL5800395 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL4848388 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL4850359 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL5987712 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL6008825 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL5827930 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL4872141 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL5983750 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL6008577 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL6018849 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL5739946 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL5776829 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL6026771 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL6018927 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5878673 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL6000337 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5766992 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5967906 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5880723 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL6005326 | — | IC50 | = | 100.0 | nM | 7.00 |