Assay Detail
Functional
CHEMBL2061887
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Agonist activity at rat TRPV1 expressed in CHO cells assessed as calcium uptake
25
Total Activities
25
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
The SAR analysis of TRPV1 agonists with the α-methylated B-region.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 6.76 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL246648 | — | — | 1 | 8.59 |
| CHEMBL2057857 | — | — | 1 | 7.67 |
| CHEMBL2057846 | — | — | 1 | 7.62 |
| CHEMBL2057856 | — | — | 1 | 7.58 |
| CHEMBL327228 | — | — | 1 | 7.39 |
| CHEMBL314262 | — | — | 1 | 7.21 |
| CHEMBL76961 | — | — | 1 | 7.11 |
| CHEMBL1277026 | — | — | 1 | 7.09 |
| CHEMBL86708 | — | — | 1 | 7.08 |
| CHEMBL2057855 | — | — | 1 | 6.89 |
| CHEMBL356291 | — | — | 1 | 6.88 |
| CHEMBL76903 | OLVANIL | 2.0 | 1 | 6.70 |
| CHEMBL2057845 | — | — | 1 | 6.69 |
| CHEMBL2057847 | — | — | 1 | 6.66 |
| CHEMBL75124 | NONIVAMIDE | 3.0 | 1 | 6.65 |
| CHEMBL2057852 | — | — | 1 | 6.62 |
| CHEMBL2057849 | — | — | 1 | 6.45 |
| CHEMBL2057862 | — | — | 1 | 6.42 |
| CHEMBL2057858 | — | — | 1 | 6.39 |
| CHEMBL328628 | DAVASAICIN | 2.0 | 1 | 6.23 |
| CHEMBL2057859 | — | — | 1 | 6.17 |
| CHEMBL2057215 | — | — | 1 | 6.04 |
| CHEMBL2057861 | — | — | 1 | 5.90 |
| CHEMBL2057860 | — | — | 1 | 5.80 |
| CHEMBL2058155 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL246648 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL2057857 | — | EC50 | = | 21.3 | nM | 7.67 |
| CHEMBL2057846 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2057856 | — | EC50 | = | 26.3 | nM | 7.58 |
| CHEMBL327228 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL314262 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL76961 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL1277026 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL86708 | — | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL2057855 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL356291 | — | EC50 | = | 132.0 | nM | 6.88 |
| CHEMBL76903 | OLVANIL | EC50 | = | 202.0 | nM | 6.70 |
| CHEMBL2057845 | — | EC50 | = | 206.0 | nM | 6.69 |
| CHEMBL2057847 | — | EC50 | = | 221.0 | nM | 6.66 |
| CHEMBL75124 | NONIVAMIDE | EC50 | = | 223.0 | nM | 6.65 |
| CHEMBL2057852 | — | EC50 | = | 238.0 | nM | 6.62 |
| CHEMBL2057849 | — | EC50 | = | 358.0 | nM | 6.45 |
| CHEMBL2057862 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2057858 | — | EC50 | = | 404.0 | nM | 6.39 |
| CHEMBL328628 | DAVASAICIN | EC50 | = | 589.0 | nM | 6.23 |
| CHEMBL2057859 | — | EC50 | = | 678.0 | nM | 6.17 |
| CHEMBL2057215 | — | EC50 | = | 911.0 | nM | 6.04 |
| CHEMBL2057861 | — | EC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL2057860 | — | EC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL2058155 | — | EC50 | = | 5800.0 | nM | 5.24 |