Assay Detail
Functional
CHEMBL1286696
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium uptake
23
Total Activities
23
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
Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.64 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1277670 | — | — | 1 | 8.55 |
| CHEMBL1277927 | — | — | 1 | 8.47 |
| CHEMBL1277211 | — | — | 1 | 8.40 |
| CHEMBL1277119 | — | — | 1 | 8.39 |
| CHEMBL1277305 | — | — | 1 | 8.37 |
| CHEMBL1276941 | — | — | 1 | 8.37 |
| CHEMBL1277669 | — | — | 1 | 8.06 |
| CHEMBL1276942 | — | — | 1 | 7.97 |
| CHEMBL1277847 | — | — | 1 | 7.87 |
| CHEMBL1277117 | — | — | 1 | 7.76 |
| CHEMBL1277928 | — | — | 1 | 7.72 |
| CHEMBL1277392 | — | — | 1 | 7.32 |
| CHEMBL1278105 | — | — | 1 | 7.28 |
| CHEMBL1276940 | — | — | 1 | 7.14 |
| CHEMBL1277028 | — | — | 1 | 6.97 |
| CHEMBL177809 | — | — | 1 | 6.90 |
| CHEMBL1275621 | — | — | 1 | 6.78 |
| CHEMBL1278197 | — | — | 1 | 6.65 |
| CHEMBL1277303 | — | — | 1 | 6.24 |
| CHEMBL1277576 | — | — | 1 | - |
| CHEMBL1277029 | — | — | 1 | - |
| CHEMBL1277118 | — | — | 1 | - |
| CHEMBL1277026 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1277670 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1277927 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL1277211 | — | Ki | = | 3.96 | nM | 8.40 |
| CHEMBL1277119 | — | Ki | = | 4.09 | nM | 8.39 |
| CHEMBL1277305 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL1276941 | — | Ki | = | 4.26 | nM | 8.37 |
| CHEMBL1277669 | — | Ki | = | 8.77 | nM | 8.06 |
| CHEMBL1276942 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL1277847 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL1277117 | — | Ki | = | 17.2 | nM | 7.76 |
| CHEMBL1277928 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL1277392 | — | Ki | = | 47.9 | nM | 7.32 |
| CHEMBL1278105 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL1276940 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL1277028 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL177809 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL1275621 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL1278197 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL1277303 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL1277576 | — | Ki | - | — | - | |
| CHEMBL1277029 | — | Ki | - | — | - | |
| CHEMBL1277118 | — | Ki | - | — | - | |
| CHEMBL1277026 | — | Ki | - | — | - |