Assay Detail
Binding
CHEMBL3705232
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FLIPR Assay: The FLIPR protocol consists of 2 substance additions. First the compounds to be tested (10 μM) are pipetted onto the cells and the Ca2+ influx is compared with the control (capsaicin 10 μM). This provides the result in % activation based on the Ca2+ signal after the addition of 10 μM of capsaicin (CP). After 5 minutes incubation, 100 nM of capsaicin are applied and the Ca2+ influx is also determined. Desensitising agonists and antagonists lead to suppression of the Ca2+ influx. The % inhibition is calculated compared to the maximum achievable inhibition with 10 μM of capsazepine. Starting from the percentage displacement caused by different concentrations of the compounds to be tested of general formula I, IC50 inhibitory concentrations which cause a 50-percent displacement of capsaicin were calculated. K1 values for the test substances were obtained by conversion by means of the Cheng-Prusoff equation (Cheng, Prusoff; Biochem. Pharmacol. 22, 3099-3108, 1973).
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Amine substituted methanesulfonamide derivatives as vanilloid receptor ligands
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.82 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3694612 | — | — | 1 | 9.00 |
| CHEMBL3694614 | — | — | 1 | 9.00 |
| CHEMBL3694615 | — | — | 1 | 8.40 |
| CHEMBL3694599 | — | — | 1 | 8.40 |
| CHEMBL3694610 | — | — | 1 | 8.40 |
| CHEMBL3694601 | — | — | 1 | 8.30 |
| CHEMBL3694603 | — | — | 1 | 8.30 |
| CHEMBL3694608 | — | — | 1 | 8.30 |
| CHEMBL3694600 | — | — | 1 | 7.96 |
| CHEMBL3694605 | — | — | 1 | 7.92 |
| CHEMBL3694597 | — | — | 1 | 7.70 |
| CHEMBL3694613 | — | — | 1 | 7.70 |
| CHEMBL3694598 | — | — | 1 | 7.58 |
| CHEMBL3694607 | — | — | 1 | 7.34 |
| CHEMBL3694606 | — | — | 1 | 7.30 |
| CHEMBL3694616 | — | — | 1 | 7.26 |
| CHEMBL3694609 | — | — | 1 | 7.12 |
| CHEMBL3694602 | — | — | 1 | 7.10 |
| CHEMBL3694611 | — | — | 1 | 7.07 |
| CHEMBL3694604 | — | — | 1 | 7.06 |
| CHEMBL3694596 | — | — | 1 | 6.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3694612 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3694614 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3694615 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3694599 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3694610 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3694601 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3694603 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3694608 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3694600 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3694605 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3694597 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3694613 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3694598 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3694607 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL3694606 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL3694616 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL3694609 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL3694602 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL3694611 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL3694604 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL3694596 | — | Ki | = | 102.0 | nM | 6.99 |