Assay Detail
Binding
CHEMBL5337356
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin induced intracellular Ca2+ ions by fluorometric imaging plate reader analysis
37
Total Activities
37
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 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of N-(1-(2-hydroxyethyl)quinolin-2-one)-N'-(1-phenyl-1H-pyrazol-5-yl)methyl) urea as Mode-Selective TRPV1 antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 8.67 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4781687 | — | — | 1 | 9.57 |
| CHEMBL5406113 | — | — | 1 | 9.34 |
| CHEMBL5426914 | — | — | 1 | 9.09 |
| CHEMBL5409442 | — | — | 1 | 8.99 |
| CHEMBL5412992 | — | — | 1 | 8.97 |
| CHEMBL5430115 | — | — | 1 | 8.94 |
| CHEMBL5419861 | — | — | 1 | 8.94 |
| CHEMBL5403769 | — | — | 1 | 8.94 |
| CHEMBL5434483 | — | — | 1 | 8.93 |
| CHEMBL5400968 | — | — | 1 | 8.91 |
| CHEMBL5427113 | — | — | 1 | 8.89 |
| CHEMBL5408353 | — | — | 1 | 8.88 |
| CHEMBL5413293 | — | — | 1 | 8.87 |
| CHEMBL5426292 | — | — | 1 | 8.87 |
| CHEMBL5414267 | — | — | 1 | 8.84 |
| CHEMBL5394003 | — | — | 1 | 8.82 |
| CHEMBL5418891 | — | — | 1 | 8.76 |
| CHEMBL5439218 | — | — | 1 | 8.73 |
| CHEMBL5432992 | — | — | 1 | 8.72 |
| CHEMBL5432397 | — | — | 1 | 8.65 |
| CHEMBL5418316 | — | — | 1 | 8.64 |
| CHEMBL5440062 | — | — | 1 | 8.60 |
| CHEMBL5429834 | — | — | 1 | 8.58 |
| CHEMBL5428310 | — | — | 1 | 8.54 |
| CHEMBL5411659 | — | — | 1 | 8.53 |
| CHEMBL5397357 | — | — | 1 | 8.51 |
| CHEMBL5435141 | — | — | 1 | 8.51 |
| CHEMBL5434166 | — | — | 1 | 8.48 |
| CHEMBL5405791 | — | — | 1 | 8.37 |
| CHEMBL5401266 | — | — | 1 | 8.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4781687 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL5406113 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL5426914 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL5409442 | — | IC50 | = | 1.02 | nM | 8.99 |
| CHEMBL5412992 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL5430115 | — | IC50 | = | 1.14 | nM | 8.94 |
| CHEMBL5419861 | — | IC50 | = | 1.16 | nM | 8.94 |
| CHEMBL5403769 | — | IC50 | = | 1.15 | nM | 8.94 |
| CHEMBL5434483 | — | IC50 | = | 1.18 | nM | 8.93 |
| CHEMBL5400968 | — | IC50 | = | 1.23 | nM | 8.91 |
| CHEMBL5427113 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5408353 | — | IC50 | = | 1.31 | nM | 8.88 |
| CHEMBL5413293 | — | IC50 | = | 1.34 | nM | 8.87 |
| CHEMBL5426292 | — | IC50 | = | 1.35 | nM | 8.87 |
| CHEMBL5414267 | — | IC50 | = | 1.45 | nM | 8.84 |
| CHEMBL5394003 | — | IC50 | = | 1.51 | nM | 8.82 |
| CHEMBL5418891 | — | IC50 | = | 1.73 | nM | 8.76 |
| CHEMBL5439218 | — | IC50 | = | 1.86 | nM | 8.73 |
| CHEMBL5432992 | — | IC50 | = | 1.92 | nM | 8.72 |
| CHEMBL5432397 | — | IC50 | = | 2.24 | nM | 8.65 |
| CHEMBL5418316 | — | IC50 | = | 2.31 | nM | 8.64 |
| CHEMBL5440062 | — | IC50 | = | 2.49 | nM | 8.60 |
| CHEMBL5429834 | — | IC50 | = | 2.63 | nM | 8.58 |
| CHEMBL5428310 | — | IC50 | = | 2.85 | nM | 8.54 |
| CHEMBL5411659 | — | IC50 | = | 2.93 | nM | 8.53 |
| CHEMBL5397357 | — | IC50 | = | 3.11 | nM | 8.51 |
| CHEMBL5435141 | — | IC50 | = | 3.11 | nM | 8.51 |
| CHEMBL5434166 | — | IC50 | = | 3.27 | nM | 8.48 |
| CHEMBL5405791 | — | IC50 | = | 4.29 | nM | 8.37 |
| CHEMBL5401266 | — | IC50 | = | 4.72 | nM | 8.33 |
| CHEMBL5419961 | — | IC50 | = | 5.81 | nM | 8.24 |
| CHEMBL5440413 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5409855 | — | IC50 | = | 7.17 | nM | 8.14 |
| CHEMBL5433444 | — | IC50 | = | 7.38 | nM | 8.13 |
| CHEMBL5407936 | — | IC50 | = | 83.1 | nM | 7.08 |
| CHEMBL5429426 | — | IC50 | > | 160.0 | nM | - |
| CHEMBL5398884 | — | IC50 | > | 160.0 | nM | - |