Assay Detail
Binding
CHEMBL3396779
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Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced effect by FLIPR assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.25 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3393837 | — | — | 1 | 9.70 |
| CHEMBL3393836 | — | — | 1 | 9.40 |
| CHEMBL3393838 | — | — | 1 | 9.15 |
| CHEMBL3393840 | — | — | 1 | 8.74 |
| CHEMBL3393826 | — | — | 1 | 8.15 |
| CHEMBL3393828 | — | — | 1 | 8.14 |
| CHEMBL3393833 | — | — | 1 | 8.11 |
| CHEMBL3393827 | — | — | 1 | 8.08 |
| CHEMBL3393832 | — | — | 1 | 8.05 |
| CHEMBL3393830 | — | — | 1 | 8.02 |
| CHEMBL323134 | — | — | 1 | 7.86 |
| CHEMBL104028 | — | — | 1 | 7.74 |
| CHEMBL3393842 | — | — | 1 | 7.32 |
| CHEMBL3393835 | — | — | 1 | 7.04 |
| CHEMBL3393834 | — | — | 1 | - |
| CHEMBL3393839 | — | — | 1 | - |
| CHEMBL3393825 | — | — | 1 | - |
| CHEMBL3393841 | — | — | 1 | - |
| CHEMBL3393843 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3393837 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3393836 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3393838 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3393840 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3393826 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL3393828 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL3393833 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL3393827 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL3393832 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL3393830 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL323134 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL104028 | — | Ki | = | 18.3 | nM | 7.74 |
| CHEMBL3393842 | — | Ki | = | 48.1 | nM | 7.32 |
| CHEMBL3393835 | — | Ki | = | 91.6 | nM | 7.04 |
| CHEMBL3393834 | — | Ki | - | — | - | |
| CHEMBL3393839 | — | Ki | - | — | - | |
| CHEMBL3393825 | — | Ki | - | — | - | |
| CHEMBL3393841 | — | Ki | - | — | - | |
| CHEMBL3393843 | — | Ki | - | — | - |