Assay Detail
Functional
CHEMBL1780484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat TRPV1 expressed in CHO cells co-expressing aequorin and CRE-luciferase reporter gene assessed as inhibition of capsaicin-induced calcium flux
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| 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
Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.82 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1779676 | — | — | 1 | 8.80 |
| CHEMBL1779687 | — | — | 1 | 8.72 |
| CHEMBL1779840 | — | — | 1 | 8.68 |
| CHEMBL1779668 | — | — | 1 | 8.49 |
| CHEMBL1779665 | — | — | 1 | 8.35 |
| CHEMBL1779839 | — | — | 1 | 8.35 |
| CHEMBL1779683 | — | — | 1 | 8.35 |
| CHEMBL1779666 | — | — | 1 | 8.31 |
| CHEMBL1779841 | — | — | 1 | 8.31 |
| CHEMBL191990 | — | — | 1 | 8.15 |
| CHEMBL1779675 | — | — | 1 | 8.10 |
| CHEMBL1779672 | — | — | 1 | 8.07 |
| CHEMBL1779669 | — | — | 1 | 7.96 |
| CHEMBL1779686 | — | — | 1 | 7.92 |
| CHEMBL1779684 | — | — | 1 | 7.92 |
| CHEMBL1779673 | — | — | 1 | 7.85 |
| CHEMBL1779842 | — | — | 1 | 7.80 |
| CHEMBL1779682 | — | — | 1 | 7.80 |
| CHEMBL1779838 | — | — | 1 | 7.72 |
| CHEMBL1779685 | — | — | 1 | 7.72 |
| CHEMBL1779670 | — | — | 1 | 7.72 |
| CHEMBL1779671 | — | — | 1 | 7.68 |
| CHEMBL1779681 | — | — | 1 | 7.52 |
| CHEMBL1779667 | — | — | 1 | 7.42 |
| CHEMBL1779674 | — | — | 1 | 7.41 |
| CHEMBL342003 | — | — | 1 | 7.28 |
| CHEMBL1779664 | — | — | 1 | 7.19 |
| CHEMBL1779679 | — | — | 1 | 6.57 |
| CHEMBL1779677 | — | — | 1 | 6.28 |
| CHEMBL1779678 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1779676 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1779687 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1779840 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1779668 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1779665 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL1779839 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL1779683 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL1779666 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL1779841 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL191990 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL1779675 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1779672 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL1779669 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1779686 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1779684 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1779673 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1779842 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1779682 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1779838 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1779685 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1779670 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1779671 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1779681 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1779667 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1779674 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL342003 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL1779664 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1779679 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1779677 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL1779678 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL1779837 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1779836 | — | IC50 | - | — | - | |
| CHEMBL1779680 | — | IC50 | > | 1000.0 | nM | - |