Assay Detail
Binding
CHEMBL4011255
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Antagonist activity at human P2Y12 receptor expressed in CHO cells assessed as inhibition of 2-MeSADP-induced beta-arrestin translocation preincubated for 30 mins followed by 2-MeSADP addition measured after 90 mins by luminescence-based topcount method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Potent and Selective Antagonists for the UTP-Activated P2Y4 Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.83 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4069492 | — | — | 1 | 7.22 |
| CHEMBL4099292 | — | — | 1 | 5.63 |
| CHEMBL4087247 | — | — | 1 | 5.62 |
| CHEMBL4081274 | — | — | 1 | 5.53 |
| CHEMBL256057 | ACID BLUE 25 | — | 1 | 5.51 |
| CHEMBL4090874 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4069492 | — | IC50 | = | 60.4 | nM | 7.22 |
| CHEMBL4099292 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL4087247 | — | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL4081274 | — | IC50 | = | 2960.0 | nM | 5.53 |
| CHEMBL256057 | ACID BLUE 25 | IC50 | = | 3120.0 | nM | 5.51 |
| CHEMBL4090874 | — | IC50 | = | 3590.0 | nM | 5.45 |