Assay Detail
Binding
CHEMBL5045601
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
42
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y<sub>14</sub>R Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 7.26 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5085823 | — | — | 2 | 8.51 |
| CHEMBL5074765 | — | — | 1 | 8.06 |
| CHEMBL5087295 | — | — | 1 | 8.01 |
| CHEMBL5083619 | — | — | 1 | 7.97 |
| CHEMBL5085145 | — | — | 1 | 7.90 |
| CHEMBL5092515 | — | — | 1 | 7.81 |
| CHEMBL5086827 | — | — | 1 | 7.75 |
| CHEMBL4645216 | — | — | 1 | 7.70 |
| CHEMBL5078197 | — | — | 1 | 7.68 |
| CHEMBL5079102 | — | — | 1 | 7.67 |
| CHEMBL5084539 | — | — | 1 | 7.62 |
| CHEMBL5074947 | — | — | 1 | 7.60 |
| CHEMBL5091500 | — | — | 1 | 7.59 |
| CHEMBL5075741 | — | — | 2 | 7.53 |
| CHEMBL5094130 | — | — | 1 | 7.50 |
| CHEMBL5078289 | — | — | 1 | 7.46 |
| CHEMBL5083773 | — | — | 1 | 7.43 |
| CHEMBL5078543 | — | — | 1 | 7.42 |
| CHEMBL5076127 | — | — | 1 | 7.40 |
| CHEMBL5081216 | — | — | 1 | 7.37 |
| CHEMBL5079780 | — | — | 1 | 7.35 |
| CHEMBL5077557 | — | — | 1 | 7.34 |
| CHEMBL5076678 | — | — | 1 | 7.30 |
| CHEMBL5079653 | — | — | 1 | 7.23 |
| CHEMBL5080028 | — | — | 1 | 7.21 |
| CHEMBL5093569 | — | — | 1 | 7.00 |
| CHEMBL5093465 | — | — | 1 | 7.00 |
| CHEMBL5081782 | — | — | 1 | 7.00 |
| CHEMBL5079515 | — | — | 1 | 6.99 |
| CHEMBL5074788 | — | — | 1 | 6.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5085823 | — | IC50 | = | 3.11 | nM | 8.51 |
| CHEMBL5085823 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL5074765 | — | IC50 | = | 8.62 | nM | 8.06 |
| CHEMBL5087295 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL5083619 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL5085145 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL5092515 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL5086827 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL4645216 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5078197 | — | IC50 | = | 20.9 | nM | 7.68 |
| CHEMBL5079102 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL5084539 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL5074947 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL5091500 | — | IC50 | = | 25.9 | nM | 7.59 |
| CHEMBL5075741 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL5094130 | — | IC50 | = | 31.5 | nM | 7.50 |
| CHEMBL5078289 | — | IC50 | = | 34.9 | nM | 7.46 |
| CHEMBL5083773 | — | IC50 | = | 37.3 | nM | 7.43 |
| CHEMBL5078543 | — | IC50 | = | 38.3 | nM | 7.42 |
| CHEMBL5076127 | — | IC50 | = | 39.5 | nM | 7.40 |
| CHEMBL5081216 | — | IC50 | = | 42.4 | nM | 7.37 |
| CHEMBL5079780 | — | IC50 | = | 44.6 | nM | 7.35 |
| CHEMBL5077557 | — | IC50 | = | 45.5 | nM | 7.34 |
| CHEMBL5076678 | — | IC50 | = | 49.6 | nM | 7.30 |
| CHEMBL5079653 | — | IC50 | = | 58.6 | nM | 7.23 |
| CHEMBL5080028 | — | IC50 | = | 61.8 | nM | 7.21 |
| CHEMBL5075741 | — | IC50 | = | 64.1 | nM | 7.19 |
| CHEMBL5093569 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5081782 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL5093465 | — | IC50 | = | 99.3 | nM | 7.00 |
| CHEMBL5079515 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL5074788 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL5083835 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL5077574 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL5087161 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL5089848 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL5086761 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL5081827 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL5075522 | — | IC50 | = | 466.0 | nM | 6.33 |
| CHEMBL5090079 | — | IC50 | = | 497.0 | nM | 6.30 |
| CHEMBL5092333 | — | IC50 | = | 696.0 | nM | 6.16 |
| CHEMBL5084659 | — | IC50 | = | 8900.0 | nM | 5.05 |