Assay Detail
Binding
CHEMBL4384769
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV4 expressed in BHK/AC9 cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10 mins followed by agonist addition by Fluo-4-AM dye-based FLIPR assay
12
Total Activities
12
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 |
Target
Transient receptor potential cation channel subfamily V member 4 (CHEMBL3119) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 12 | 8.32 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4456312 | — | — | 1 | 9.52 |
| CHEMBL4547537 | — | — | 1 | 9.30 |
| CHEMBL4461475 | — | — | 1 | 9.30 |
| CHEMBL4439448 | — | — | 1 | 8.70 |
| CHEMBL4586959 | — | — | 1 | 8.70 |
| CHEMBL4547101 | — | — | 1 | 8.49 |
| CHEMBL4439190 | — | — | 1 | 8.49 |
| CHEMBL4437115 | — | — | 1 | 8.30 |
| CHEMBL4441860 | — | — | 1 | 7.70 |
| CHEMBL4467225 | — | — | 1 | 7.70 |
| CHEMBL4473984 | — | — | 1 | 7.40 |
| CHEMBL4453093 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4456312 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4547537 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4461475 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4439448 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4586959 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4547101 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4439190 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4437115 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4441860 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4467225 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4473984 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4453093 | — | IC50 | = | 631.0 | nM | 6.20 |