Assay Detail
Functional
CHEMBL951240
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization
12
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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
4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.82 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL404165 | — | — | 3 | 9.24 |
| CHEMBL255420 | — | — | 1 | 9.19 |
| CHEMBL229430 | AMG-517 | 1.0 | 1 | 9.12 |
| CHEMBL258054 | — | — | 1 | 8.96 |
| CHEMBL258265 | — | — | 1 | 8.96 |
| CHEMBL258056 | — | — | 1 | 8.85 |
| CHEMBL402637 | — | — | 1 | 8.68 |
| CHEMBL258117 | — | — | 1 | 8.54 |
| CHEMBL403425 | — | — | 1 | 8.00 |
| CHEMBL191990 | — | — | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL404165 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL404165 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL404165 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL255420 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL229430 | AMG-517 | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL258054 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL258265 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL258056 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL402637 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL258117 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL403425 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL191990 | — | IC50 | = | 13.0 | nM | 7.89 |