Assay Detail
Binding
CHEMBL5733259
Review assay metadata, readout intent, target linkage, and publication context from the same page.
calcium assay: Capsaicin (0.3 μM) caused an increase in [Ca2+] in the vast majority (95%) of dorsal root ganglia neurons, which were thereby identified as TRPV1 expressing neurons. All synthesized derivatives were tested and all were able to inhibit the calcium uptake and several compounds exhibited more than 80% inhibition, e.g. compounds of Examples 1, 3, 4, 5, 6, 10, 11, 12, 13, 16, 19, 23, 31, 32, 35, 36, 39, 41, 45, 46, 47, 48, 51, 53, 67, 68, 69, 70, 71, 74, 75, 78, 80, 81, 82, 86, 87 and 89. Among them, derivatives such as compounds of Examples 4, 5, 6, 13, 19, 31, 36, 39, 45, 46, 47, 48, 51, 52, 53, 67, 70, 71, 74, 75, 78, 80, 81, 86 and 87, appeared the most potent TRPV1 antagonists exhibiting a complete abolition of capsaicin response (around 100%) at 300 nM.
75
Total Activities
25
Compounds Tested
3
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 1 (CHEMBL5102) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
TRPV1 vanilloid receptor antagonists with a bicyclic portion
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.35 | 10.00 |
| kon | 25 | - | - |
| k_off | 25 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6042549 | — | — | 3 | 10.00 |
| CHEMBL5945302 | — | — | 3 | 9.89 |
| CHEMBL6030464 | — | — | 3 | 9.29 |
| CHEMBL5818861 | — | — | 3 | 9.21 |
| CHEMBL5797308 | — | — | 3 | 9.15 |
| CHEMBL5937077 | — | — | 3 | 9.08 |
| CHEMBL6009909 | — | — | 3 | 9.00 |
| CHEMBL6009304 | — | — | 3 | 8.74 |
| CHEMBL6012343 | — | — | 3 | 8.74 |
| CHEMBL5765420 | — | — | 3 | 8.72 |
| CHEMBL5973765 | — | — | 3 | 8.52 |
| CHEMBL5892655 | — | — | 3 | 8.39 |
| CHEMBL5759204 | — | — | 3 | 8.22 |
| CHEMBL5765985 | — | — | 3 | 8.22 |
| CHEMBL5866538 | — | — | 3 | 8.05 |
| CHEMBL5913103 | — | — | 3 | 8.02 |
| CHEMBL6055195 | — | — | 3 | 7.92 |
| CHEMBL6004883 | — | — | 3 | 7.92 |
| CHEMBL6013464 | — | — | 3 | 7.77 |
| CHEMBL5900327 | — | — | 3 | 7.70 |
| CHEMBL5921112 | — | — | 3 | 7.70 |
| CHEMBL5762838 | — | — | 3 | 7.27 |
| CHEMBL6005455 | — | — | 3 | 7.10 |
| CHEMBL5965313 | — | — | 3 | 7.04 |
| CHEMBL5747901 | — | — | 3 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6042549 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5945302 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL6030464 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL5818861 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL5797308 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5937077 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL6009909 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6012343 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL6009304 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5765420 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5973765 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5892655 | — | IC50 | = | 4.07 | nM | 8.39 |
| CHEMBL5765985 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5759204 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5866538 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5913103 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL6004883 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL6055195 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL6013464 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5921112 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL5900327 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5762838 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL6005455 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5965313 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL5747901 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL5762838 | — | kon | = | - | — | - |
| CHEMBL5762838 | — | k_off | = | - | s-1 | - |
| CHEMBL6013464 | — | kon | = | - | — | - |
| CHEMBL6013464 | — | k_off | = | - | s-1 | - |
| CHEMBL5866538 | — | kon | = | - | — | - |
| CHEMBL5866538 | — | k_off | = | - | s-1 | - |
| CHEMBL5921112 | — | kon | = | - | — | - |
| CHEMBL5921112 | — | k_off | = | - | s-1 | - |
| CHEMBL5747901 | — | kon | = | - | — | - |
| CHEMBL5892655 | — | kon | = | - | — | - |
| CHEMBL5892655 | — | k_off | = | - | s-1 | - |
| CHEMBL6009909 | — | kon | = | - | — | - |
| CHEMBL5818861 | — | k_off | = | - | s-1 | - |
| CHEMBL5818861 | — | kon | = | - | — | - |
| CHEMBL5945302 | — | kon | = | - | — | - |
| CHEMBL5937077 | — | kon | = | - | — | - |
| CHEMBL6012343 | — | k_off | = | - | s-1 | - |
| CHEMBL6012343 | — | kon | = | - | — | - |
| CHEMBL5937077 | — | k_off | = | - | s-1 | - |
| CHEMBL5965313 | — | kon | = | - | — | - |
| CHEMBL5765985 | — | k_off | = | - | s-1 | - |
| CHEMBL5965313 | — | k_off | = | - | s-1 | - |
| CHEMBL6055195 | — | kon | = | - | — | - |
| CHEMBL6055195 | — | k_off | = | - | s-1 | - |
| CHEMBL5765985 | — | kon | = | - | — | - |