Assay Detail
Binding
CHEMBL4408646
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Antagonist activity at recombinant human TRPV1 expressed in CHO cells assessed as as inhibition of capsaicin-induced calcium uptake incubated for 5 mins in presence of 45Ca2+ by liquid scintillation counter
18
Total Activities
18
Compounds Tested
2
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 |
|---|---|---|---|
| EC50 | 17 | 7.58 | 8.65 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177429 | — | — | 1 | 8.65 |
| CHEMBL4586277 | — | — | 1 | 8.09 |
| CHEMBL4553702 | — | — | 1 | 8.06 |
| CHEMBL4471708 | — | — | 1 | 8.05 |
| CHEMBL4438643 | — | — | 1 | 8.00 |
| CHEMBL4442473 | — | — | 1 | 7.73 |
| CHEMBL4571845 | — | — | 1 | 7.60 |
| CHEMBL4562769 | — | — | 1 | 7.51 |
| CHEMBL4457595 | — | — | 1 | 7.50 |
| CHEMBL4438974 | — | — | 1 | 7.50 |
| CHEMBL4459611 | — | — | 1 | 7.38 |
| CHEMBL4453980 | — | — | 1 | 7.25 |
| CHEMBL4555508 | — | — | 1 | 7.09 |
| CHEMBL4476530 | — | — | 1 | 7.07 |
| CHEMBL4536869 | — | — | 1 | 6.92 |
| CHEMBL4457304 | — | — | 1 | 6.81 |
| CHEMBL4483060 | — | — | 1 | - |
| CHEMBL4448866 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177429 | — | EC50 | = | 2.22 | nM | 8.65 |
| CHEMBL4586277 | — | EC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4553702 | — | EC50 | = | 8.8 | nM | 8.06 |
| CHEMBL4471708 | — | EC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4438643 | — | EC50 | = | 10.1 | nM | 8.00 |
| CHEMBL4442473 | — | EC50 | = | 18.68 | nM | 7.73 |
| CHEMBL4571845 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4562769 | — | EC50 | = | 30.6 | nM | 7.51 |
| CHEMBL4457595 | — | EC50 | = | 31.3 | nM | 7.50 |
| CHEMBL4438974 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4459611 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4453980 | — | EC50 | = | 56.1 | nM | 7.25 |
| CHEMBL4555508 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4476530 | — | EC50 | = | 85.9 | nM | 7.07 |
| CHEMBL4536869 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4457304 | — | EC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4483060 | — | Inhibition | - | % | - | |
| CHEMBL4448866 | — | EC50 | - | — | - |