Assay Detail
Functional
CHEMBL5385290
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Antagonist activity at human P2Y12R expressed in HEK293 cells assessed as inhibition of MeSADP-induced cAMP production preincubated for 0.5 hrs followed by MeSADP stimulation by cAMP-glo analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Selective P2Y<sub>6</sub>R Antagonists with High Affinity and <i>In Vivo</i> Efficacy for Inflammatory Disease Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 1 | 5.85 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL398435 | TICAGRELOR | 4.0 | 1 | 5.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL398435 | TICAGRELOR | IC50 | = | 1398.0 | nM | 5.85 |