Assay Detail
Functional
CHEMBL889188
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV1 by calcium influx assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.82 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL104028 | — | — | 1 | 8.40 |
| CHEMBL230669 | — | — | 1 | 7.77 |
| CHEMBL230561 | — | — | 1 | 7.72 |
| CHEMBL230668 | — | — | 1 | 7.70 |
| CHEMBL389715 | — | — | 1 | 7.66 |
| CHEMBL230457 | — | — | 1 | 7.62 |
| CHEMBL427105 | — | — | 1 | 7.58 |
| CHEMBL231291 | — | — | 1 | 7.39 |
| CHEMBL230667 | — | — | 1 | 7.34 |
| CHEMBL397922 | — | — | 1 | 7.33 |
| CHEMBL397459 | — | — | 1 | 7.14 |
| CHEMBL230983 | — | — | 1 | 7.03 |
| CHEMBL397898 | — | — | 1 | 6.96 |
| CHEMBL396018 | — | — | 1 | 6.91 |
| CHEMBL397896 | — | — | 1 | 6.90 |
| CHEMBL230982 | — | — | 1 | 6.84 |
| CHEMBL230562 | — | — | 1 | 6.83 |
| CHEMBL230774 | — | — | 1 | 6.83 |
| CHEMBL230563 | — | — | 1 | 6.77 |
| CHEMBL395995 | — | — | 1 | 6.61 |
| CHEMBL230881 | — | — | 1 | 6.54 |
| CHEMBL395720 | — | — | 1 | 6.32 |
| CHEMBL397897 | — | — | 1 | 6.22 |
| CHEMBL231392 | — | — | 1 | 6.13 |
| CHEMBL230772 | — | — | 1 | 5.59 |
| CHEMBL231593 | — | — | 1 | 5.43 |
| CHEMBL230773 | — | — | 1 | 4.80 |
| CHEMBL395490 | — | — | 1 | 4.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL104028 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL230669 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL230561 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL230668 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL389715 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL230457 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL427105 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL231291 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL230667 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL397922 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL397459 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL230983 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL397898 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL396018 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL397896 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL230982 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL230562 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL230774 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL230563 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL395995 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL230881 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL395720 | — | IC50 | = | 476.0 | nM | 6.32 |
| CHEMBL397897 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL231392 | — | IC50 | = | 749.0 | nM | 6.13 |
| CHEMBL230772 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL231593 | — | IC50 | = | 3750.0 | nM | 5.43 |
| CHEMBL230773 | — | IC50 | = | 15900.0 | nM | 4.80 |
| CHEMBL395490 | — | IC50 | = | 31000.0 | nM | 4.51 |