Assay Detail
Binding
CHEMBL4387490
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat TRPV4 expressed in HEK293 cells assessed as reduction in Ca2+ influx incubated for 30 mins by Fluo4-AM dye based
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily V member 4 (CHEMBL2775) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of a novel orally active TRPV4 inhibitor: Part 1. Optimization from an HTS hit.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.61 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4578182 | — | — | 1 | 9.49 |
| CHEMBL4465116 | — | — | 1 | 9.14 |
| CHEMBL4459940 | — | — | 1 | 8.96 |
| CHEMBL4553265 | — | — | 1 | 6.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4578182 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4465116 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL4459940 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4553265 | — | IC50 | = | 137.0 | nM | 6.86 |