Assay Detail
Binding
CHEMBL4050583
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant rat TRPV4 expressed in CHOK1 cells assessed as inhibition of 4alphaPDD-induced activation pretreated for 5 mins followed by 4alphaPDD stimulation measured for 5 mins by FLIPR assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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
Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.49 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4101768 | — | — | 1 | 8.36 |
| CHEMBL4099293 | — | — | 1 | 8.09 |
| CHEMBL3941914 | — | — | 1 | 8.07 |
| CHEMBL4060956 | — | — | 1 | 7.66 |
| CHEMBL4077429 | — | — | 1 | 7.42 |
| CHEMBL4080527 | — | — | 1 | 7.41 |
| CHEMBL4063752 | — | — | 1 | 7.33 |
| CHEMBL4083772 | — | — | 1 | 7.30 |
| CHEMBL4082835 | — | — | 1 | 7.21 |
| CHEMBL4077790 | — | — | 1 | 6.75 |
| CHEMBL2133556 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4101768 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4099293 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3941914 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4060956 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4077429 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4080527 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4063752 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4083772 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4082835 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4077790 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2133556 | — | IC50 | = | 180.0 | nM | 6.75 |