Assay Detail
Binding
CHEMBL5554615
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2X2/3R expressed in HEK293 cells incubated for 18 hrs by Fluo-4 dye based microplate reader assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
P2X2/P2X3 heterotrimeric receptor (CHEMBL3831281) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of Triazolopyrimidine Derivatives as Selective P2X3 Receptor Antagonists Binding to an Unprecedented Allosteric Site as Evidenced by Cryo-Electron Microscopy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.92 | 7.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL526307 | — | — | 1 | 7.71 |
| CHEMBL5573155 | — | — | 1 | 6.05 |
| CHEMBL5574288 | — | — | 1 | 5.93 |
| CHEMBL5594973 | — | — | 1 | 5.93 |
| CHEMBL5574915 | — | — | 1 | 5.89 |
| CHEMBL5572710 | — | — | 1 | 5.84 |
| CHEMBL5590914 | — | — | 1 | 5.69 |
| CHEMBL5574190 | — | — | 1 | 5.65 |
| CHEMBL5207245 | — | — | 1 | 5.30 |
| CHEMBL5564655 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL526307 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL5573155 | — | IC50 | = | 881.0 | nM | 6.05 |
| CHEMBL5574288 | — | IC50 | = | 1186.0 | nM | 5.93 |
| CHEMBL5594973 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL5574915 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL5572710 | — | IC50 | = | 1451.0 | nM | 5.84 |
| CHEMBL5590914 | — | IC50 | = | 2028.0 | nM | 5.69 |
| CHEMBL5574190 | — | IC50 | = | 2254.0 | nM | 5.65 |
| CHEMBL5207245 | — | IC50 | = | 5060.0 | nM | 5.30 |
| CHEMBL5564655 | — | IC50 | = | 5978.0 | nM | 5.22 |