Assay Detail
Functional
CHEMBL960836
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat recombinant P2X3 receptor expressed in CHO cells by FLIPR assay
36
Total Activities
36
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 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.75 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL495204 | — | — | 1 | 8.20 |
| CHEMBL526307 | — | — | 1 | 8.00 |
| CHEMBL495203 | — | — | 1 | 7.70 |
| CHEMBL494833 | — | — | 1 | 7.60 |
| CHEMBL448525 | — | — | 1 | 7.60 |
| CHEMBL521983 | — | — | 1 | 7.40 |
| CHEMBL494176 | — | — | 1 | 7.40 |
| CHEMBL502618 | — | — | 1 | 7.30 |
| CHEMBL523043 | — | — | 1 | 7.10 |
| CHEMBL492967 | — | — | 1 | 7.00 |
| CHEMBL521820 | — | — | 1 | 7.00 |
| CHEMBL446310 | — | — | 1 | 7.00 |
| CHEMBL494772 | — | — | 1 | 6.90 |
| CHEMBL492968 | — | — | 1 | 6.80 |
| CHEMBL494832 | — | — | 1 | 6.80 |
| CHEMBL500550 | — | — | 1 | 6.80 |
| CHEMBL444469 | — | — | 1 | 6.40 |
| CHEMBL494181 | — | — | 1 | 6.30 |
| CHEMBL492562 | — | — | 1 | 6.20 |
| CHEMBL495195 | — | — | 1 | 6.00 |
| CHEMBL494239 | — | — | 1 | 5.90 |
| CHEMBL494761 | — | — | 1 | 5.80 |
| CHEMBL504607 | — | — | 1 | 5.80 |
| CHEMBL522184 | — | — | 1 | 5.60 |
| CHEMBL494940 | — | — | 1 | 5.50 |
| CHEMBL494834 | — | — | 1 | 5.40 |
| CHEMBL494760 | ORMETOPRIM | 2.0 | 1 | - |
| CHEMBL524043 | — | — | 1 | - |
| CHEMBL494240 | — | — | 1 | - |
| CHEMBL495370 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL495204 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL526307 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL495203 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL494833 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL448525 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL521983 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL494176 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL502618 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL523043 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL521820 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL446310 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL492967 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL494772 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL500550 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL494832 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL492968 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL444469 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL494181 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL492562 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL495195 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL494239 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL494761 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL504607 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL522184 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL494940 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL494834 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL492969 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL494849 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL510124 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL492788 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL492787 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL492786 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL495370 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL494240 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL524043 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL494760 | ORMETOPRIM | IC50 | > | 10000.0 | nM | - |