Assay Detail
Binding
CHEMBL3615486
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV4 receptor expressed in HEK293 cells assessed as inhibition of EC80 of 4alpha-PDD-stimulated calcium flux after 10 mins
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Identification of orally-bioavailable antagonists of the TRPV4 ion-channel.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.96 | 6.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3613639 | — | — | 1 | 6.58 |
| CHEMBL3613640 | — | — | 1 | 6.42 |
| CHEMBL3613628 | — | — | 1 | 6.41 |
| CHEMBL3613642 | — | — | 1 | 6.38 |
| CHEMBL3613641 | — | — | 1 | 6.27 |
| CHEMBL3613629 | — | — | 1 | 6.15 |
| CHEMBL3613638 | — | — | 1 | 6.10 |
| CHEMBL3613636 | — | — | 1 | 6.04 |
| CHEMBL3613643 | — | — | 1 | 6.03 |
| CHEMBL3613627 | — | — | 1 | 6.03 |
| CHEMBL3613637 | — | — | 1 | 5.89 |
| CHEMBL3613634 | — | — | 1 | 5.88 |
| CHEMBL3613635 | — | — | 1 | 5.68 |
| CHEMBL3613630 | — | — | 1 | 5.66 |
| CHEMBL3613633 | — | — | 1 | 5.38 |
| CHEMBL3613626 | — | — | 1 | 5.31 |
| CHEMBL3613625 | — | — | 1 | 5.07 |
| CHEMBL3613631 | — | — | 1 | - |
| CHEMBL3613632 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3613639 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3613640 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3613628 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3613642 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3613641 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3613629 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL3613638 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3613636 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3613643 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL3613627 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL3613637 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL3613634 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL3613635 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL3613630 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL3613633 | — | IC50 | = | 4220.0 | nM | 5.38 |
| CHEMBL3613626 | — | IC50 | = | 4930.0 | nM | 5.31 |
| CHEMBL3613625 | — | IC50 | = | 8530.0 | nM | 5.07 |
| CHEMBL3613631 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3613632 | — | IC50 | > | 10000.0 | nM | - |