Assay Detail
Binding
CHEMBL5031925
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Antagonist activity at rat P2X3 receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.29 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5084053 | — | — | 1 | 8.42 |
| CHEMBL5084939 | — | — | 1 | 8.40 |
| CHEMBL4748113 | — | — | 1 | 8.21 |
| CHEMBL5073093 | — | — | 1 | 8.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5084053 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5084939 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4748113 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5073093 | — | IC50 | = | 7.7 | nM | 8.11 |