Assay Detail
Binding
CHEMBL3096841
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human P2X3 receptor expressed in Xenopus oocytes assessed as inhibition of ATP-induced ion current preincubated for 20 mins followed by ATP addition by two-electrode voltage clamp assay
22
Total Activities
22
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
Design and synthesis of potent and selective P2X₃ receptor antagonists derived from PPADS as potential pain modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.25 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL596234 | A-317491 | — | 1 | 7.46 |
| CHEMBL3091630 | — | — | 1 | 7.22 |
| CHEMBL3091628 | — | — | 1 | 6.84 |
| CHEMBL3091631 | — | — | 1 | 6.44 |
| CHEMBL3091632 | — | — | 1 | 6.42 |
| CHEMBL3091610 | — | — | 1 | 6.34 |
| CHEMBL3091607 | — | — | 1 | 6.34 |
| CHEMBL3091619 | — | — | 1 | 6.32 |
| CHEMBL3091620 | — | — | 1 | 6.23 |
| CHEMBL3091629 | — | — | 1 | 6.20 |
| CHEMBL3091633 | — | — | 1 | 6.20 |
| CHEMBL3091635 | — | — | 1 | 6.19 |
| CHEMBL3091625 | — | — | 1 | 6.14 |
| CHEMBL3091605 | — | — | 1 | 6.10 |
| CHEMBL3091618 | — | — | 1 | 6.08 |
| CHEMBL3091634 | — | — | 1 | 6.07 |
| CHEMBL3091606 | — | — | 1 | 6.04 |
| CHEMBL3091627 | — | — | 1 | 6.03 |
| CHEMBL3091622 | — | — | 1 | 5.98 |
| CHEMBL3091617 | — | — | 1 | 5.90 |
| CHEMBL3091623 | — | — | 1 | 5.53 |
| CHEMBL3091621 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL596234 | A-317491 | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3091630 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3091628 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL3091631 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL3091632 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL3091610 | — | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL3091607 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3091619 | — | IC50 | = | 474.0 | nM | 6.32 |
| CHEMBL3091620 | — | IC50 | = | 587.0 | nM | 6.23 |
| CHEMBL3091629 | — | IC50 | = | 636.0 | nM | 6.20 |
| CHEMBL3091633 | — | IC50 | = | 638.0 | nM | 6.20 |
| CHEMBL3091635 | — | IC50 | = | 652.0 | nM | 6.19 |
| CHEMBL3091625 | — | IC50 | = | 723.0 | nM | 6.14 |
| CHEMBL3091605 | — | IC50 | = | 797.0 | nM | 6.10 |
| CHEMBL3091618 | — | IC50 | = | 824.0 | nM | 6.08 |
| CHEMBL3091634 | — | IC50 | = | 856.0 | nM | 6.07 |
| CHEMBL3091606 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL3091627 | — | IC50 | = | 928.0 | nM | 6.03 |
| CHEMBL3091622 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL3091617 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL3091623 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL3091621 | — | IC50 | = | 3300.0 | nM | 5.48 |