Assay Detail
Functional
CHEMBL917101
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Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
18
Total Activities
18
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 | Expert |
Publication
Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 6.37 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL373780 | — | — | 1 | 8.10 |
| CHEMBL217803 | — | — | 1 | 7.46 |
| CHEMBL336296 | URIDINE TRIPHOSPHATE | 3.0 | 1 | 7.31 |
| CHEMBL385098 | — | — | 1 | 7.21 |
| CHEMBL14249 | ADENOSINE TRIPHOSPHATE | 2.0 | 1 | 7.07 |
| CHEMBL221326 | DIQUAFOSOL | 4.0 | 1 | 6.68 |
| CHEMBL220200 | — | — | 1 | 6.62 |
| CHEMBL507282 | DENUFOSOL | 3.0 | 1 | 6.57 |
| CHEMBL221162 | — | — | 1 | 6.33 |
| CHEMBL220940 | THYMIDINE_TRIPHOSPHATE | — | 1 | 6.32 |
| CHEMBL384527 | — | — | 1 | 6.12 |
| CHEMBL220398 | — | — | 1 | 6.08 |
| CHEMBL374361 | — | — | 1 | 5.97 |
| CHEMBL219779 | — | — | 1 | 5.75 |
| CHEMBL410594 | — | — | 1 | 5.73 |
| CHEMBL220011 | — | — | 1 | 5.25 |
| CHEMBL376430 | — | — | 1 | 5.19 |
| CHEMBL220337 | — | — | 1 | 4.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL373780 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL217803 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL336296 | URIDINE TRIPHOSPHATE | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL385098 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL14249 | ADENOSINE TRIPHOSPHATE | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL221326 | DIQUAFOSOL | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL220200 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL507282 | DENUFOSOL | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL221162 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL220940 | THYMIDINE_TRIPHOSPHATE | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL384527 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL220398 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL374361 | — | EC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL219779 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL410594 | — | EC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL220011 | — | EC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL376430 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL220337 | — | EC50 | = | 14300.0 | nM | 4.84 |