Assay Detail
Functional
CHEMBL820093
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Functional antagonistic activity against human vanilloid receptor subtype 1 in HEK293 cell membranes was determined as inhibition of agonist-induced increases in intracellular [Ca2+] levels
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
7-Hydroxynaphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.17 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL148920 | — | — | 1 | 8.40 |
| CHEMBL358953 | — | — | 1 | 7.82 |
| CHEMBL348001 | — | — | 1 | 7.77 |
| CHEMBL151442 | — | — | 1 | 7.68 |
| CHEMBL151446 | — | — | 1 | 7.58 |
| CHEMBL147068 | — | — | 1 | 7.57 |
| CHEMBL139989 | — | — | 1 | 7.35 |
| CHEMBL151298 | — | — | 1 | 7.05 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | 7.00 |
| CHEMBL146744 | — | — | 1 | 6.50 |
| CHEMBL440535 | — | — | 1 | 6.11 |
| CHEMBL347492 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL148920 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL358953 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL348001 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL151442 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL151446 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL147068 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL139989 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL151298 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL391997 | CAPSAZEPINE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL146744 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL440535 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL347492 | — | IC50 | = | 6300.0 | nM | 5.20 |