Assay Detail
Binding
CHEMBL820953
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Binding affinity against Vanilloid receptor in dorsal Root Ganglion (DRG) membranes using [3H]RTX binding assay.
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Dorsal root ganglion |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL5102) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Similarities and differences in the structure-activity relationships of capsaicin and resiniferatoxin analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.19 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17976 | RESINIFERATOXIN | 3.0 | 2 | 9.92 |
| CHEMBL99940 | — | — | 1 | 9.77 |
| CHEMBL319214 | — | — | 1 | 9.00 |
| CHEMBL98363 | — | — | 1 | 8.49 |
| CHEMBL317463 | — | — | 1 | 8.37 |
| CHEMBL319078 | — | — | 1 | 8.08 |
| CHEMBL97880 | — | — | 1 | 7.97 |
| CHEMBL98634 | — | — | 1 | 6.22 |
| CHEMBL294199 | CAPSAICIN | 4.0 | 1 | 5.70 |
| CHEMBL329939 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17976 | RESINIFERATOXIN | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL99940 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL319214 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL98363 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL317463 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL17976 | RESINIFERATOXIN | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL319078 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL97880 | — | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL98634 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL294199 | CAPSAICIN | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL329939 | — | Ki | > | 10000.0 | nM | - |