Assay Detail
Functional
CHEMBL1786668
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Agonist activity at human recombinant P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
30
Total Activities
30
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 | 30 | 6.00 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1198849 | — | — | 1 | 7.55 |
| CHEMBL217803 | — | — | 1 | 7.46 |
| CHEMBL336296 | URIDINE TRIPHOSPHATE | 3.0 | 1 | 7.26 |
| CHEMBL1767408 | DIQUAFOSOL TETRASODIUM | 4.0 | 1 | 6.68 |
| CHEMBL499138 | — | — | 1 | 6.52 |
| CHEMBL1784902 | — | — | 1 | 6.31 |
| CHEMBL1784292 | — | — | 1 | 6.30 |
| CHEMBL1784293 | — | — | 1 | 6.21 |
| CHEMBL1784892 | — | — | 1 | 6.21 |
| CHEMBL1784894 | — | — | 1 | 6.19 |
| CHEMBL1784904 | — | — | 1 | 6.15 |
| CHEMBL1784885 | — | — | 1 | 6.11 |
| CHEMBL1784890 | — | — | 1 | 6.09 |
| CHEMBL1784896 | — | — | 1 | 6.08 |
| CHEMBL444212 | — | — | 1 | 6.03 |
| CHEMBL1784893 | — | — | 1 | 5.92 |
| CHEMBL1784891 | — | — | 1 | 5.82 |
| CHEMBL484105 | — | — | 1 | 5.77 |
| CHEMBL1784889 | — | — | 1 | 5.72 |
| CHEMBL519835 | — | — | 1 | 5.60 |
| CHEMBL1784291 | — | — | 1 | 5.58 |
| CHEMBL1784887 | — | — | 1 | 5.56 |
| CHEMBL474886 | — | — | 1 | 5.56 |
| CHEMBL1784900 | — | — | 1 | 5.48 |
| CHEMBL1784886 | — | — | 1 | 5.43 |
| CHEMBL483502 | — | — | 1 | 5.41 |
| CHEMBL519991 | — | — | 1 | 5.40 |
| CHEMBL1784899 | — | — | 1 | 5.31 |
| CHEMBL1784895 | — | — | 1 | 5.18 |
| CHEMBL1765114 | — | — | 1 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1198849 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL217803 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL336296 | URIDINE TRIPHOSPHATE | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1767408 | DIQUAFOSOL TETRASODIUM | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL499138 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1784902 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL1784292 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1784293 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1784892 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1784894 | — | EC50 | = | 640.0 | nM | 6.19 |
| CHEMBL1784904 | — | EC50 | = | 710.0 | nM | 6.15 |
| CHEMBL1784885 | — | EC50 | = | 770.0 | nM | 6.11 |
| CHEMBL1784890 | — | EC50 | = | 817.0 | nM | 6.09 |
| CHEMBL1784896 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL444212 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL1784893 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1784891 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL484105 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1784889 | — | EC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL519835 | — | EC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL1784291 | — | EC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL1784887 | — | EC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL474886 | — | EC50 | = | 2760.0 | nM | 5.56 |
| CHEMBL1784900 | — | EC50 | = | 3330.0 | nM | 5.48 |
| CHEMBL1784886 | — | EC50 | = | 3720.0 | nM | 5.43 |
| CHEMBL483502 | — | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL519991 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1784899 | — | EC50 | = | 4850.0 | nM | 5.31 |
| CHEMBL1784895 | — | EC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL1765114 | — | EC50 | = | 9600.0 | nM | 5.02 |