Assay Detail
Binding
CHEMBL4384734
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV4 expressed in HEK 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
6
Total Activities
6
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 | 6 | 7.18 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4533534 | — | — | 1 | 8.10 |
| CHEMBL4468326 | — | — | 1 | 7.60 |
| CHEMBL4465119 | — | — | 1 | 7.50 |
| CHEMBL4534649 | — | — | 1 | 7.30 |
| CHEMBL4444971 | — | — | 1 | 6.80 |
| CHEMBL4469003 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4533534 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4468326 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4465119 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4534649 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4444971 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL4469003 | — | IC50 | = | 1585.0 | nM | 5.80 |