Assay Detail
Binding
CHEMBL4124030
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2X3 receptor expressed in C6-BU-1 cells assessed as inhibition of calcium flux after 1 hr by Fluo-3AM dye based FLIPR assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | C6-BU-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 1: Initial structure-activity relationship studies of a hit from a high throughput screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.68 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4126267 | — | — | 1 | 8.05 |
| CHEMBL4129184 | — | — | 1 | 8.00 |
| CHEMBL4129491 | — | — | 1 | 7.72 |
| CHEMBL4130242 | — | — | 1 | 7.70 |
| CHEMBL4128213 | — | — | 1 | 7.70 |
| CHEMBL4128106 | — | — | 1 | 7.68 |
| CHEMBL4127637 | — | — | 1 | 7.60 |
| CHEMBL4126833 | — | — | 1 | 7.52 |
| CHEMBL4126038 | — | — | 1 | 7.14 |
| CHEMBL4127346 | — | — | 1 | 7.05 |
| CHEMBL596234 | A-317491 | — | 1 | 7.04 |
| CHEMBL4127133 | — | — | 1 | 7.00 |
| CHEMBL4126971 | — | — | 1 | 6.89 |
| CHEMBL4127788 | — | — | 1 | 6.89 |
| CHEMBL4129357 | — | — | 1 | 6.87 |
| CHEMBL4129031 | — | — | 1 | 6.85 |
| CHEMBL4130133 | — | — | 1 | 6.58 |
| CHEMBL4127171 | — | — | 1 | 6.44 |
| CHEMBL4129977 | — | — | 1 | 6.43 |
| CHEMBL4127905 | — | — | 1 | 6.25 |
| CHEMBL4129705 | — | — | 1 | 5.99 |
| CHEMBL4126274 | — | — | 1 | 5.86 |
| CHEMBL4129638 | — | — | 1 | 5.48 |
| CHEMBL4128222 | — | — | 1 | 5.41 |
| CHEMBL4127573 | — | — | 1 | 5.37 |
| CHEMBL1456917 | — | — | 1 | 5.32 |
| CHEMBL4128051 | — | — | 1 | 5.23 |
| CHEMBL4129448 | — | — | 1 | 5.01 |
| CHEMBL4128476 | — | — | 1 | - |
| CHEMBL4125741 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4126267 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4129184 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4129491 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4130242 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4128213 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4128106 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4127637 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4126833 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4126038 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4127346 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL596234 | A-317491 | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4127133 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4126971 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4127788 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4129357 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4129031 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4130133 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4127171 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4129977 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4127905 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4129705 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4126274 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL4129638 | — | IC50 | = | 3280.0 | nM | 5.48 |
| CHEMBL4128222 | — | IC50 | = | 3930.0 | nM | 5.41 |
| CHEMBL4127573 | — | IC50 | = | 4240.0 | nM | 5.37 |
| CHEMBL1456917 | — | IC50 | = | 4790.0 | nM | 5.32 |
| CHEMBL4128051 | — | IC50 | = | 5920.0 | nM | 5.23 |
| CHEMBL4129448 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL4128476 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4125741 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4128559 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4126976 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4129182 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4126198 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4129722 | — | IC50 | > | 10000.0 | nM | - |