Assay Detail
Functional
CHEMBL4384762
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reversal of heart failure-induced pulmonary edema in Sprague-Dawley rat assessed as inhibition of GSK1016790A-induced increase in lung wet weight to body weight ratio at 0.09 to 0.78 mg/kg, iv bolus loading dose followed by 0.07 to 0.6 ug/kg/min, iv continuous infusion dose for 60 mins prior to agonist administration
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 1 | 6.21 | 6.21 |
| fIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4461475 | — | — | 2 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4461475 | — | IC50 | = | 611.0 | nM | 6.21 |
| CHEMBL4461475 | — | fIC50 | = | 8.5 | nM | - |