Assay Detail
Binding
CHEMBL4408644
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Displacement of [3H]RTX from recombinant human TRPV1 expressed in CHO cells incubated for 60 mins by liquid scintillation counter
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.88 | 9.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4471708 | — | — | 1 | 9.34 |
| CHEMBL4553702 | — | — | 1 | 9.17 |
| CHEMBL4438643 | — | — | 1 | 9.02 |
| CHEMBL4562769 | — | — | 1 | 8.78 |
| CHEMBL4586277 | — | — | 1 | 8.42 |
| CHEMBL4453980 | — | — | 1 | 8.13 |
| CHEMBL2177429 | — | — | 1 | 8.10 |
| CHEMBL4438974 | — | — | 1 | 7.97 |
| CHEMBL4442473 | — | — | 1 | 7.91 |
| CHEMBL4459611 | — | — | 1 | 7.85 |
| CHEMBL4536869 | — | — | 1 | 7.82 |
| CHEMBL4571845 | — | — | 1 | 7.79 |
| CHEMBL4555508 | — | — | 1 | 7.55 |
| CHEMBL4457595 | — | — | 1 | 7.38 |
| CHEMBL4457304 | — | — | 1 | 7.21 |
| CHEMBL4448866 | — | — | 1 | 6.96 |
| CHEMBL4476530 | — | — | 1 | 6.58 |
| CHEMBL4483060 | — | — | 1 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4471708 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL4553702 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL4438643 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL4562769 | — | Ki | = | 1.67 | nM | 8.78 |
| CHEMBL4586277 | — | Ki | = | 3.79 | nM | 8.42 |
| CHEMBL4453980 | — | Ki | = | 7.33 | nM | 8.13 |
| CHEMBL2177429 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL4438974 | — | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL4442473 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL4459611 | — | Ki | = | 14.1 | nM | 7.85 |
| CHEMBL4536869 | — | Ki | = | 15.3 | nM | 7.82 |
| CHEMBL4571845 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL4555508 | — | Ki | = | 27.9 | nM | 7.55 |
| CHEMBL4457595 | — | Ki | = | 41.4 | nM | 7.38 |
| CHEMBL4457304 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4448866 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL4476530 | — | Ki | = | 266.0 | nM | 6.58 |
| CHEMBL4483060 | — | Ki | = | 1159.0 | nM | 5.94 |