Assay Detail
Binding
CHEMBL4322927
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at BacMam virus expressing human TRPV4 transduced in BHK/AC9 or HEK MSR2 cells assessed as inhibition of GSK634775-induced Ca2+ flux preincubated for 10 mins followed by agonist addition by Fluo-4 AM dye based FLIPR assay
11
Total Activities
11
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
Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.37 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4517101 | — | — | 1 | 8.46 |
| CHEMBL4454801 | — | — | 1 | 8.42 |
| CHEMBL4533534 | — | — | 1 | 8.10 |
| CHEMBL4550510 | — | — | 1 | 7.92 |
| CHEMBL4173887 | — | — | 1 | 7.48 |
| CHEMBL4437649 | — | — | 1 | 7.47 |
| CHEMBL4468250 | — | — | 1 | 7.28 |
| CHEMBL4453088 | — | — | 1 | 7.00 |
| CHEMBL4459916 | — | — | 1 | 6.76 |
| CHEMBL4440858 | — | — | 1 | 6.72 |
| CHEMBL4466785 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4517101 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4454801 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4533534 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4550510 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4173887 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4437649 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4468250 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4453088 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4459916 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL4440858 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4466785 | — | IC50 | = | 3800.0 | nM | 5.42 |