Assay Detail
Binding
CHEMBL3705932
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FLIPR Assay: The agonistic or antagonistic effect of the substances to be tested on the rat-species vanilloid receptor 1 (VR1/TRPV1) can be determined using the following assay. In this assay, the influx of Ca2+ through the receptor channel is quantified with the aid of a Ca2+-sensitive dye (type Fluo-4, Molecular Probes Europe BV, Leiden, the Netherlands) in a fluorescent imaging plate reader (FLIPR, Molecular Devices, Sunnyvale, USA).Method:Complete medium: 50 ml HAMS F12 nutrient mixture (Gibco Invitrogen GmbH, Karlsruhe, Germany) with10% by volume of FCS (foetal calf serum, Gibco Invitrogen GmbH, Karlsruhe, Germany, heat-inactivated);2 mM L-glutamine (Sigma, Munich, Germany);1% by weight of AA solution (antibiotic/antimyotic solution, PAA, Pasching, Austria) and 25 ng/ml NGF medium (2.5 S, Gibco Invitrogen GmbH, Karlsruhe, Germany).
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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
Substituted phenylureas and phenylamides as vanilloid receptor ligands
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.32 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3689046 | — | — | 1 | 10.00 |
| CHEMBL3689037 | — | — | 1 | 10.00 |
| CHEMBL3689036 | — | — | 1 | 9.70 |
| CHEMBL3684332 | — | — | 1 | 9.46 |
| CHEMBL3689043 | — | — | 1 | 9.40 |
| CHEMBL3689044 | — | — | 1 | 9.40 |
| CHEMBL3689047 | — | — | 1 | 8.92 |
| CHEMBL3689041 | — | — | 1 | 8.92 |
| CHEMBL3689035 | — | — | 1 | 8.60 |
| CHEMBL3689045 | — | — | 1 | 8.29 |
| CHEMBL3684333 | — | — | 1 | 8.23 |
| CHEMBL3689034 | — | — | 1 | 8.14 |
| CHEMBL3684331 | — | — | 1 | 7.84 |
| CHEMBL3689067 | — | — | 1 | 7.59 |
| CHEMBL3689033 | — | — | 1 | 7.59 |
| CHEMBL3689042 | — | — | 1 | 7.37 |
| CHEMBL3689057 | — | — | 1 | 7.07 |
| CHEMBL3689039 | — | — | 1 | 6.09 |
| CHEMBL3689040 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3689046 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3689037 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3689036 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3684332 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL3689043 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3689044 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3689047 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3689041 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3689035 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3689045 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL3684333 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL3689034 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL3684331 | — | Ki | = | 14.5 | nM | 7.84 |
| CHEMBL3689067 | — | Ki | = | 25.5 | nM | 7.59 |
| CHEMBL3689033 | — | Ki | = | 25.9 | nM | 7.59 |
| CHEMBL3689042 | — | Ki | = | 42.7 | nM | 7.37 |
| CHEMBL3689057 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL3689039 | — | Ki | = | 819.0 | nM | 6.09 |
| CHEMBL3689040 | — | Ki | = | 2834.0 | nM | 5.55 |