Assay Detail
Functional
CHEMBL974446
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Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | 1321-N1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 6.56 | 6.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL336296 | URIDINE TRIPHOSPHATE | 3.0 | 1 | 6.86 |
| CHEMBL14249 | ADENOSINE TRIPHOSPHATE | 2.0 | 1 | 6.62 |
| CHEMBL221326 | DIQUAFOSOL | 4.0 | 1 | 6.38 |
| CHEMBL339385 | DIADENOSINE TETRAPHOSPHATE | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL336296 | URIDINE TRIPHOSPHATE | EC50 | = | 138.0 | nM | 6.86 |
| CHEMBL14249 | ADENOSINE TRIPHOSPHATE | EC50 | = | 237.0 | nM | 6.62 |
| CHEMBL221326 | DIQUAFOSOL | EC50 | = | 419.0 | nM | 6.38 |
| CHEMBL339385 | DIADENOSINE TETRAPHOSPHATE | EC50 | = | 423.0 | nM | 6.37 |