Assay Detail
Functional
CHEMBL990778
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant TRPV1 expressed in human 1321N1 cells assessed as inhibition of capsaicin-induced calcium influx by FLIPR assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | 1321-N1 |
| 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
Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.36 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441472 | — | — | 1 | 8.30 |
| CHEMBL518979 | — | — | 1 | 8.22 |
| CHEMBL522425 | — | — | 1 | 8.10 |
| CHEMBL491234 | — | — | 1 | 8.00 |
| CHEMBL482835 | — | — | 1 | 8.00 |
| CHEMBL491036 | — | — | 1 | 7.85 |
| CHEMBL520995 | — | — | 1 | 7.85 |
| CHEMBL489400 | — | — | 1 | 7.72 |
| CHEMBL491035 | — | — | 1 | 7.72 |
| CHEMBL482834 | — | — | 1 | 7.62 |
| CHEMBL491034 | — | — | 1 | 7.57 |
| CHEMBL488972 | — | — | 1 | 7.48 |
| CHEMBL523605 | — | — | 1 | 7.46 |
| CHEMBL491241 | — | — | 1 | 7.39 |
| CHEMBL522481 | — | — | 1 | 7.39 |
| CHEMBL183121 | — | — | 1 | 7.38 |
| CHEMBL523307 | — | — | 1 | 7.38 |
| CHEMBL521968 | — | — | 1 | 7.36 |
| CHEMBL489570 | — | — | 1 | 7.17 |
| CHEMBL488782 | — | — | 1 | 7.11 |
| CHEMBL491033 | — | — | 1 | 7.11 |
| CHEMBL489571 | — | — | 1 | 7.02 |
| CHEMBL491225 | — | — | 1 | 6.91 |
| CHEMBL483866 | — | — | 1 | 6.83 |
| CHEMBL491816 | — | — | 1 | 6.71 |
| CHEMBL489399 | — | — | 1 | 6.58 |
| CHEMBL522969 | — | — | 1 | 6.21 |
| CHEMBL491226 | — | — | 1 | 5.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441472 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL518979 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL522425 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL491234 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL482835 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL491036 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL520995 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL489400 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL491035 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL482834 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL491034 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL488972 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL523605 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL491241 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL522481 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL183121 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL523307 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL521968 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL489570 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL488782 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL491033 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL489571 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL491225 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL483866 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL491816 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL489399 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL522969 | — | IC50 | = | 618.0 | nM | 6.21 |
| CHEMBL491226 | — | IC50 | = | 2746.0 | nM | 5.56 |