Assay Detail
Functional
CHEMBL830059
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity in pH 5.5-induced FLIPR assays in HEK293 cells expressing human TRPV1
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
4-(2-Pyridyl)piperazine-1-benzimidazoles as potent TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.86 | 6.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254779 | — | — | 1 | 6.98 |
| CHEMBL403013 | — | — | 1 | 6.22 |
| CHEMBL180852 | — | — | 1 | 5.85 |
| CHEMBL359880 | — | — | 1 | 5.77 |
| CHEMBL254984 | — | — | 1 | 5.75 |
| CHEMBL451491 | — | — | 1 | 5.44 |
| CHEMBL183321 | — | — | 1 | 5.00 |
| CHEMBL180802 | — | — | 1 | - |
| CHEMBL183897 | — | — | 1 | - |
| CHEMBL183416 | — | — | 1 | - |
| CHEMBL180026 | — | — | 1 | - |
| CHEMBL183016 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254779 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL403013 | — | IC50 | = | 597.0 | nM | 6.22 |
| CHEMBL180852 | — | IC50 | = | 1409.0 | nM | 5.85 |
| CHEMBL359880 | — | IC50 | = | 1688.0 | nM | 5.77 |
| CHEMBL254984 | — | IC50 | = | 1778.0 | nM | 5.75 |
| CHEMBL451491 | — | IC50 | = | 3608.0 | nM | 5.44 |
| CHEMBL183321 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL180802 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL183897 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL183416 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL180026 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL183016 | — | IC50 | > | 10000.0 | nM | - |