Assay Detail
Binding
CHEMBL1286693
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]RTX from rat TRPV1 expressed in CHO cells
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 44 | 7.09 | 8.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1277669 | — | — | 1 | 8.03 |
| CHEMBL1276941 | — | — | 1 | 8.03 |
| CHEMBL1277211 | — | — | 1 | 8.03 |
| CHEMBL1277305 | — | — | 1 | 7.95 |
| CHEMBL1277576 | — | — | 1 | 7.88 |
| CHEMBL1276940 | — | — | 1 | 7.87 |
| CHEMBL1278105 | — | — | 1 | 7.71 |
| CHEMBL1276942 | — | — | 1 | 7.70 |
| CHEMBL1277928 | — | — | 1 | 7.69 |
| CHEMBL1277848 | — | — | 1 | 7.68 |
| CHEMBL1277847 | — | — | 1 | 7.68 |
| CHEMBL1277670 | — | — | 1 | 7.66 |
| CHEMBL1278012 | — | — | 1 | 7.60 |
| CHEMBL1276855 | — | — | 1 | 7.60 |
| CHEMBL1277762 | — | — | 1 | 7.60 |
| CHEMBL1277577 | — | — | 1 | 7.51 |
| CHEMBL1277119 | — | — | 1 | 7.47 |
| CHEMBL1278013 | — | — | 1 | 7.46 |
| CHEMBL1277761 | — | — | 1 | 7.42 |
| CHEMBL1277394 | — | — | 1 | 7.37 |
| CHEMBL1278106 | — | — | 1 | 7.25 |
| CHEMBL1277210 | — | — | 1 | 7.24 |
| CHEMBL1277927 | — | — | 1 | 7.10 |
| CHEMBL1277306 | — | — | 1 | 7.07 |
| CHEMBL1277117 | — | — | 1 | 7.05 |
| CHEMBL1275621 | — | — | 1 | 7.04 |
| CHEMBL1277392 | — | — | 1 | 7.03 |
| CHEMBL1277029 | — | — | 1 | 6.97 |
| CHEMBL1276854 | — | — | 1 | 6.94 |
| CHEMBL1277027 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1277669 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL1277211 | — | Ki | = | 9.43 | nM | 8.03 |
| CHEMBL1276941 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL1277305 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL1277576 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL1276940 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL1278105 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL1276942 | — | Ki | = | 20.2 | nM | 7.70 |
| CHEMBL1277928 | — | Ki | = | 20.3 | nM | 7.69 |
| CHEMBL1277848 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL1277847 | — | Ki | = | 20.9 | nM | 7.68 |
| CHEMBL1277670 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1278012 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL1277762 | — | Ki | = | 25.3 | nM | 7.60 |
| CHEMBL1276855 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL1277577 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL1277119 | — | Ki | = | 33.5 | nM | 7.47 |
| CHEMBL1278013 | — | Ki | = | 34.9 | nM | 7.46 |
| CHEMBL1277761 | — | Ki | = | 37.6 | nM | 7.42 |
| CHEMBL1277394 | — | Ki | = | 42.9 | nM | 7.37 |
| CHEMBL1278106 | — | Ki | = | 56.4 | nM | 7.25 |
| CHEMBL1277210 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL1277927 | — | Ki | = | 79.1 | nM | 7.10 |
| CHEMBL1277306 | — | Ki | = | 84.5 | nM | 7.07 |
| CHEMBL1277117 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL1275621 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL1277392 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL1277029 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL1276854 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL1277027 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL1277304 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL1277303 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL1277028 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL1277208 | — | Ki | = | 364.0 | nM | 6.44 |
| CHEMBL1277483 | — | Ki | = | 378.0 | nM | 6.42 |
| CHEMBL1277393 | — | Ki | = | 388.0 | nM | 6.41 |
| CHEMBL1277482 | — | Ki | = | 393.0 | nM | 6.41 |
| CHEMBL1277118 | — | Ki | = | 486.0 | nM | 6.31 |
| CHEMBL1277026 | — | Ki | = | 667.0 | nM | 6.18 |
| CHEMBL1277120 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL1277209 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL177809 | — | Ki | = | 1320.0 | nM | 5.88 |
| CHEMBL1278197 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL1278198 | — | Ki | = | 4530.0 | nM | 5.34 |