Assay Detail
Functional
CHEMBL1786670
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Agonist activity at human recombinant P2Y6 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
23
Total Activities
23
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
Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate δ-ester modifications as selective agonists of the P2Y(4) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 5.69 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1198849 | — | — | 1 | 6.89 |
| CHEMBL1784892 | — | — | 1 | 6.64 |
| CHEMBL1784894 | — | — | 1 | 6.13 |
| CHEMBL1784890 | — | — | 1 | 6.06 |
| CHEMBL1784904 | — | — | 1 | 6.02 |
| CHEMBL1784885 | — | — | 1 | 5.93 |
| CHEMBL1784893 | — | — | 1 | 5.92 |
| CHEMBL1784292 | — | — | 1 | 5.84 |
| CHEMBL217803 | — | — | 1 | 5.82 |
| CHEMBL1784293 | — | — | 1 | 5.79 |
| CHEMBL1784902 | — | — | 1 | 5.78 |
| CHEMBL1784896 | — | — | 1 | 5.43 |
| CHEMBL1784887 | — | — | 1 | 5.31 |
| CHEMBL1784889 | — | — | 1 | 5.26 |
| CHEMBL1784291 | — | — | 1 | 5.12 |
| CHEMBL483502 | — | — | 1 | 5.12 |
| CHEMBL499138 | — | — | 1 | 5.11 |
| CHEMBL444212 | — | — | 1 | 5.09 |
| CHEMBL1784886 | — | — | 1 | 4.92 |
| CHEMBL1784895 | — | — | 1 | - |
| CHEMBL484105 | — | — | 1 | - |
| CHEMBL519991 | — | — | 1 | - |
| CHEMBL336296 | URIDINE TRIPHOSPHATE | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1198849 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1784892 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1784894 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL1784890 | — | EC50 | = | 877.0 | nM | 6.06 |
| CHEMBL1784904 | — | EC50 | = | 950.0 | nM | 6.02 |
| CHEMBL1784885 | — | EC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL1784893 | — | EC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL1784292 | — | EC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL217803 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1784293 | — | EC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL1784902 | — | EC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL1784896 | — | EC50 | = | 3690.0 | nM | 5.43 |
| CHEMBL1784887 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL1784889 | — | EC50 | = | 5460.0 | nM | 5.26 |
| CHEMBL1784291 | — | EC50 | = | 7510.0 | nM | 5.12 |
| CHEMBL483502 | — | EC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL499138 | — | EC50 | = | 7830.0 | nM | 5.11 |
| CHEMBL444212 | — | EC50 | = | 8190.0 | nM | 5.09 |
| CHEMBL1784886 | — | EC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL1784895 | — | EC50 | - | — | - | |
| CHEMBL484105 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL519991 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL336296 | URIDINE TRIPHOSPHATE | EC50 | > | 10000.0 | nM | - |