Assay Detail
Binding
CHEMBL3705773
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Calcium Flux Assay: Experiments were conducted using the FLIPRTETRA®. On the day prior to the experiment, recombinant HEK293 cells that stably express human and mouse TRPV3 were removed from tissue culture flasks and plated in growth medium at 20,000 cells/well into black-walled clear-bottom 384-well Biocoat poly-D-lysine assay plates (BD Biosciences, Bedford, Mass.) using a Multidrop® dispenser (ThermoScientific, Waltham, Mass.). On the day of the experiment, growth medium was removed, and the no-wash FLIPR® Calcium-4 dye (λEX=470-495 nm, λEM=515-575 nm; Molecular Devices, Sunnyvale, Calif.) was added to each well using the Multidrop® dispenser. Cells were incubated for 90-120 minutes in the dark. Compounds were dissolved in DMSO to prepare a 10 mM stock solution. The intensity of the fluorescence was captured and digitally transferred to an interfaced PC.
291
Total Activities
290
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily V member 3 (CHEMBL5522) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
TRPV3 modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 291 | 6.00 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3696410 | — | — | 1 | 7.10 |
| CHEMBL3696391 | — | — | 1 | 7.10 |
| CHEMBL3692308 | — | — | 1 | 6.96 |
| CHEMBL3692305 | — | — | 1 | 6.92 |
| CHEMBL3696433 | — | — | 1 | 6.92 |
| CHEMBL3696452 | — | — | 1 | 6.92 |
| CHEMBL3696448 | — | — | 1 | 6.89 |
| CHEMBL3692310 | — | — | 1 | 6.85 |
| CHEMBL3696396 | — | — | 1 | 6.85 |
| CHEMBL3696392 | — | — | 1 | 6.85 |
| CHEMBL3692284 | — | — | 1 | 6.85 |
| CHEMBL3696458 | — | — | 1 | 6.80 |
| CHEMBL3696407 | — | — | 1 | 6.80 |
| CHEMBL3696408 | — | — | 1 | 6.80 |
| CHEMBL3696409 | — | — | 1 | 6.80 |
| CHEMBL3696474 | — | — | 1 | 6.77 |
| CHEMBL3696447 | — | — | 1 | 6.77 |
| CHEMBL3696426 | — | — | 1 | 6.77 |
| CHEMBL3692282 | — | — | 1 | 6.75 |
| CHEMBL3696429 | — | — | 1 | 6.75 |
| CHEMBL3692275 | — | — | 1 | 6.72 |
| CHEMBL3696427 | — | — | 1 | 6.72 |
| CHEMBL3692233 | — | — | 1 | 6.70 |
| CHEMBL3696473 | — | — | 1 | 6.66 |
| CHEMBL3692279 | — | — | 1 | 6.66 |
| CHEMBL3692235 | — | — | 1 | 6.64 |
| CHEMBL3696418 | — | — | 1 | 6.64 |
| CHEMBL4115719 | — | — | 1 | 6.64 |
| CHEMBL3696439 | — | — | 1 | 6.60 |
| CHEMBL3692313 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3696391 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3696410 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3692308 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3696452 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3696433 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3692305 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3696448 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3692310 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3696396 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3696392 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3692284 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3696408 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3696458 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3696409 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3696407 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3696426 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3696474 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3696447 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3696429 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3692282 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3692275 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3696427 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3692233 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3696473 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3692279 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4115719 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3692235 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3696418 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3696439 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3692313 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3696442 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3696434 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3692304 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3696450 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3696403 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3692291 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3696421 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3692261 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3692297 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3696423 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3696384 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3692309 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3692242 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3639911 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3692307 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3692262 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3696420 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3692306 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3696385 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3696412 | — | IC50 | = | 350.0 | nM | 6.46 |