Assay Detail
Binding
CHEMBL2061886
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Displacement of [3H]RTX from rat TRPV1 expressed in CHO cells
30
Total Activities
30
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
The SAR analysis of TRPV1 agonists with the α-methylated B-region.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.30 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2057848 | — | — | 1 | 7.48 |
| CHEMBL246648 | — | — | 1 | 7.23 |
| CHEMBL356291 | — | — | 1 | 7.08 |
| CHEMBL2057845 | — | — | 1 | 6.88 |
| CHEMBL76903 | OLVANIL | 2.0 | 1 | 6.85 |
| CHEMBL2057856 | — | — | 1 | 6.80 |
| CHEMBL2057857 | — | — | 1 | 6.75 |
| CHEMBL2057847 | — | — | 1 | 6.75 |
| CHEMBL2057862 | — | — | 1 | 6.71 |
| CHEMBL2057859 | — | — | 1 | 6.65 |
| CHEMBL314262 | — | — | 1 | 6.62 |
| CHEMBL2057846 | — | — | 1 | 6.51 |
| CHEMBL327228 | — | — | 1 | 6.45 |
| CHEMBL2057854 | — | — | 1 | 6.42 |
| CHEMBL2057852 | — | — | 1 | 6.30 |
| CHEMBL2057858 | — | — | 1 | 6.29 |
| CHEMBL1277026 | — | — | 1 | 6.18 |
| CHEMBL2057855 | — | — | 1 | 6.13 |
| CHEMBL2057215 | — | — | 1 | 6.09 |
| CHEMBL76961 | — | — | 1 | 6.07 |
| CHEMBL86708 | — | — | 1 | 6.06 |
| CHEMBL328628 | DAVASAICIN | 2.0 | 1 | 6.03 |
| CHEMBL75124 | NONIVAMIDE | 3.0 | 1 | 5.91 |
| CHEMBL2057849 | — | — | 1 | 5.91 |
| CHEMBL2058155 | — | — | 1 | 5.84 |
| CHEMBL2057853 | — | — | 1 | 5.67 |
| CHEMBL2057851 | — | — | 1 | 5.61 |
| CHEMBL2057861 | — | — | 1 | 5.48 |
| CHEMBL2057860 | — | — | 1 | 5.37 |
| CHEMBL2057850 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2057848 | — | Ki | = | 33.1 | nM | 7.48 |
| CHEMBL246648 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL356291 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL2057845 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL76903 | OLVANIL | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL2057856 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL2057857 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL2057847 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL2057862 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL2057859 | — | Ki | = | 226.0 | nM | 6.65 |
| CHEMBL314262 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL2057846 | — | Ki | = | 308.0 | nM | 6.51 |
| CHEMBL327228 | — | Ki | = | 354.0 | nM | 6.45 |
| CHEMBL2057854 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL2057852 | — | Ki | = | 504.0 | nM | 6.30 |
| CHEMBL2057858 | — | Ki | = | 518.0 | nM | 6.29 |
| CHEMBL1277026 | — | Ki | = | 667.0 | nM | 6.18 |
| CHEMBL2057855 | — | Ki | = | 744.0 | nM | 6.13 |
| CHEMBL2057215 | — | Ki | = | 808.0 | nM | 6.09 |
| CHEMBL76961 | — | Ki | = | 848.0 | nM | 6.07 |
| CHEMBL86708 | — | Ki | = | 864.0 | nM | 6.06 |
| CHEMBL328628 | DAVASAICIN | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL75124 | NONIVAMIDE | Ki | = | 1223.0 | nM | 5.91 |
| CHEMBL2057849 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL2058155 | — | Ki | = | 1430.0 | nM | 5.84 |
| CHEMBL2057853 | — | Ki | = | 2160.0 | nM | 5.67 |
| CHEMBL2057851 | — | Ki | = | 2470.0 | nM | 5.61 |
| CHEMBL2057861 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL2057860 | — | Ki | = | 4275.0 | nM | 5.37 |
| CHEMBL2057850 | — | Ki | = | 10100.0 | nM | 5.00 |