Assay Detail
Functional
CHEMBL828115
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonistic activity on VR1 receptor in [Ca2+] influx assay in rat dorsal root ganglion
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Dorsal root ganglion |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL5102) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.29 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183121 | — | — | 1 | 7.51 |
| CHEMBL180138 | — | — | 1 | 7.51 |
| CHEMBL183795 | — | — | 1 | 7.42 |
| CHEMBL183752 | — | — | 1 | 7.26 |
| CHEMBL181478 | — | — | 1 | 7.22 |
| CHEMBL183045 | — | — | 1 | 7.22 |
| CHEMBL180902 | — | — | 1 | 6.85 |
| CHEMBL183623 | — | — | 1 | 6.82 |
| CHEMBL183835 | — | — | 1 | 6.55 |
| CHEMBL181755 | — | — | 1 | 6.00 |
| CHEMBL360453 | — | — | 1 | 5.89 |
| CHEMBL181498 | — | — | 1 | 5.70 |
| CHEMBL183761 | — | — | 1 | 5.64 |
| CHEMBL183797 | — | — | 1 | 5.44 |
| CHEMBL183093 | — | — | 1 | 5.10 |
| CHEMBL361865 | — | — | 1 | 5.00 |
| CHEMBL183657 | — | — | 1 | 5.00 |
| CHEMBL182484 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183121 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL180138 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL183795 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL183752 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL181478 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL183045 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL180902 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL183623 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL183835 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL181755 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL360453 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL181498 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL183761 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL183797 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL183093 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL361865 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL183657 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL182484 | — | IC50 | = | 10000.0 | nM | 5.00 |