Assay Detail
Functional
CHEMBL4011253
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Antagonist activity at human P2Y2 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 4.95 | 5.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4081274 | — | — | 1 | 5.19 |
| CHEMBL4087247 | — | — | 1 | 5.07 |
| CHEMBL4099292 | — | — | 1 | 4.99 |
| CHEMBL4090874 | — | — | 1 | 4.88 |
| CHEMBL4069492 | — | — | 1 | 4.79 |
| CHEMBL256057 | ACID BLUE 25 | — | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4081274 | — | IC50 | = | 6520.0 | nM | 5.19 |
| CHEMBL4087247 | — | IC50 | = | 8540.0 | nM | 5.07 |
| CHEMBL4099292 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL4090874 | — | IC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL4069492 | — | IC50 | = | 16400.0 | nM | 4.79 |
| CHEMBL256057 | ACID BLUE 25 | IC50 | = | 17100.0 | nM | 4.77 |