Assay Detail
Functional
CHEMBL1017975
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat P2X3 receptor expressed in CHO cells by FLIPR
28
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.39 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL494161 | — | — | 1 | 8.70 |
| CHEMBL523173 | — | — | 1 | 8.20 |
| CHEMBL494353 | — | — | 1 | 8.20 |
| CHEMBL494160 | — | — | 1 | 8.10 |
| CHEMBL494582 | — | — | 1 | 8.00 |
| CHEMBL492933 | — | — | 1 | 8.00 |
| CHEMBL526307 | — | — | 2 | 8.00 |
| CHEMBL494158 | — | — | 1 | 8.00 |
| CHEMBL492300 | — | — | 1 | 8.00 |
| CHEMBL494159 | — | — | 1 | 7.90 |
| CHEMBL492907 | — | — | 1 | 7.80 |
| CHEMBL492934 | — | — | 1 | 7.80 |
| CHEMBL443930 | — | — | 1 | 7.30 |
| CHEMBL492745 | — | — | 1 | 7.20 |
| CHEMBL492703 | — | — | 1 | 7.20 |
| CHEMBL493741 | — | — | 1 | 7.10 |
| CHEMBL492299 | — | — | 1 | 7.00 |
| CHEMBL494581 | — | — | 1 | 7.00 |
| CHEMBL493547 | — | — | 1 | 6.90 |
| CHEMBL493546 | — | — | 1 | 6.80 |
| CHEMBL492935 | — | — | 1 | 6.80 |
| CHEMBL523000 | — | — | 1 | 6.60 |
| CHEMBL492729 | — | — | 1 | 6.60 |
| CHEMBL492789 | — | — | 1 | 6.40 |
| CHEMBL492744 | — | — | 1 | 6.40 |
| CHEMBL493740 | — | — | 1 | 5.60 |
| CHEMBL523840 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL494161 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL523173 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL494353 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL494160 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL494582 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL492300 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL492933 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL526307 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL494158 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL494159 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL526307 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL492907 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL492934 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL443930 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL492745 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL492703 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL493741 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL492299 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL494581 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL493547 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL493546 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL492935 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL523000 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL492729 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL492789 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL492744 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL493740 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL523840 | — | IC50 | > | 10000.0 | nM | - |