Assay Detail
Binding
CHEMBL4387487
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TRPV4 expressed in HEK293 cells assessed as reduction in Ca2+ influx incubated for 30 mins by Fluo4-AM dye based
29
Total Activities
29
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
Discovery of a novel orally active TRPV4 inhibitor: Part 1. Optimization from an HTS hit.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.11 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4459940 | — | — | 1 | 9.07 |
| CHEMBL4578182 | — | — | 1 | 8.92 |
| CHEMBL4460657 | — | — | 1 | 8.72 |
| CHEMBL4465116 | — | — | 1 | 8.48 |
| CHEMBL4574043 | — | — | 1 | 7.96 |
| CHEMBL4538643 | — | — | 1 | 7.96 |
| CHEMBL4531567 | — | — | 1 | 7.82 |
| CHEMBL4519618 | — | — | 1 | 7.66 |
| CHEMBL4526382 | — | — | 1 | 7.52 |
| CHEMBL4551456 | — | — | 1 | 7.29 |
| CHEMBL4519974 | — | — | 1 | 7.11 |
| CHEMBL4462976 | — | — | 1 | 7.09 |
| CHEMBL4579045 | — | — | 1 | 7.08 |
| CHEMBL4446542 | — | — | 1 | 7.08 |
| CHEMBL4586243 | — | — | 1 | 7.07 |
| CHEMBL4467623 | — | — | 1 | 7.00 |
| CHEMBL4589218 | — | — | 1 | 6.92 |
| CHEMBL4553265 | — | — | 1 | 6.84 |
| CHEMBL4459428 | — | — | 1 | 6.62 |
| CHEMBL4434654 | — | — | 1 | 6.62 |
| CHEMBL4441221 | — | — | 1 | 6.54 |
| CHEMBL4463312 | — | — | 1 | 6.51 |
| CHEMBL4534599 | — | — | 1 | 6.14 |
| CHEMBL4550407 | — | — | 1 | 6.08 |
| CHEMBL4470016 | — | — | 1 | 6.06 |
| CHEMBL4450094 | — | — | 1 | 5.77 |
| CHEMBL4553226 | — | — | 1 | 5.75 |
| CHEMBL4463653 | — | — | 1 | 5.44 |
| CHEMBL4458628 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4459940 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL4578182 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4460657 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4465116 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4574043 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4538643 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4531567 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4519618 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4526382 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4551456 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4519974 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4462976 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4579045 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4446542 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4586243 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4467623 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4589218 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4553265 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4459428 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4434654 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4441221 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4463312 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4534599 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4550407 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4470016 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4450094 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4553226 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4463653 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4458628 | — | IC50 | > | 10000.0 | nM | - |