Assay Detail
Binding
CHEMBL4424680
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Antagonist activity at human P2X3 receptor expressed in rat C6BU-1 cells measured up to 3 mins by Fluo-3/AM dye-based fluorescence assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists Part 2: Discovery of orally bioavailable compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.35 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439812 | — | — | 1 | 8.10 |
| CHEMBL4439493 | — | — | 1 | 8.00 |
| CHEMBL4466162 | — | — | 1 | 7.96 |
| CHEMBL4592312 | — | — | 1 | 7.96 |
| CHEMBL4437131 | — | — | 1 | 7.89 |
| CHEMBL4537290 | — | — | 1 | 7.89 |
| CHEMBL4466252 | — | — | 1 | 7.89 |
| CHEMBL4572081 | — | — | 1 | 7.82 |
| CHEMBL4454941 | — | — | 1 | 7.80 |
| CHEMBL4459391 | — | — | 1 | 7.80 |
| CHEMBL4465467 | — | — | 1 | 7.80 |
| CHEMBL4457637 | — | — | 1 | 7.80 |
| CHEMBL4127637 | — | — | 1 | 7.60 |
| CHEMBL4562022 | — | — | 1 | 7.46 |
| CHEMBL4458893 | — | — | 1 | 7.36 |
| CHEMBL4557885 | — | — | 1 | 7.31 |
| CHEMBL4585133 | — | — | 1 | 7.28 |
| CHEMBL4459015 | — | — | 1 | 7.14 |
| CHEMBL4445659 | — | — | 1 | 7.13 |
| CHEMBL4565775 | — | — | 1 | 7.09 |
| CHEMBL4544543 | — | — | 1 | 6.85 |
| CHEMBL4532166 | — | — | 1 | 6.69 |
| CHEMBL4444359 | — | — | 1 | 6.26 |
| CHEMBL4456152 | — | — | 1 | 6.16 |
| CHEMBL4459785 | — | — | 1 | 6.00 |
| CHEMBL4526549 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439812 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4439493 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4466162 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4592312 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4437131 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4537290 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4466252 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4572081 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4454941 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4459391 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4465467 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4457637 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4127637 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4562022 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4458893 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4557885 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4585133 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4459015 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4445659 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4565775 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4544543 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4532166 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL4444359 | — | IC50 | = | 553.0 | nM | 6.26 |
| CHEMBL4456152 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4459785 | — | IC50 | = | 999.0 | nM | 6.00 |
| CHEMBL4526549 | — | IC50 | = | 1089.0 | nM | 5.96 |