Assay Detail
Functional
CHEMBL890240
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV1 receptor by calcium influx assay
49
Total Activities
49
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
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 7.53 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL104028 | — | — | 1 | 8.68 |
| CHEMBL231518 | — | — | 1 | 8.55 |
| CHEMBL387996 | — | — | 1 | 8.48 |
| CHEMBL231206 | — | — | 1 | 8.48 |
| CHEMBL427266 | — | — | 1 | 8.42 |
| CHEMBL397272 | — | — | 1 | 8.34 |
| CHEMBL230998 | — | — | 1 | 8.33 |
| CHEMBL230896 | — | — | 1 | 8.28 |
| CHEMBL427111 | — | — | 1 | 8.28 |
| CHEMBL231517 | — | — | 1 | 8.24 |
| CHEMBL230997 | — | — | 1 | 8.14 |
| CHEMBL231104 | — | — | 1 | 8.03 |
| CHEMBL231619 | — | — | 1 | 8.03 |
| CHEMBL387579 | — | — | 1 | 8.01 |
| CHEMBL231535 | — | — | 1 | 7.99 |
| CHEMBL395262 | — | — | 1 | 7.90 |
| CHEMBL231422 | — | — | 1 | 7.85 |
| CHEMBL439007 | — | — | 1 | 7.85 |
| CHEMBL231227 | — | — | 1 | 7.83 |
| CHEMBL397273 | — | — | 1 | 7.81 |
| CHEMBL231519 | — | — | 1 | 7.75 |
| CHEMBL231437 | — | — | 1 | 7.72 |
| CHEMBL231436 | — | — | 1 | 7.70 |
| CHEMBL396960 | — | — | 1 | 7.69 |
| CHEMBL230919 | — | — | 1 | 7.67 |
| CHEMBL437165 | — | — | 1 | 7.65 |
| CHEMBL231106 | — | — | 1 | 7.62 |
| CHEMBL437195 | — | — | 1 | 7.59 |
| CHEMBL231225 | — | — | 1 | 7.57 |
| CHEMBL438656 | — | — | 1 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL104028 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL231518 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL231206 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL387996 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL427266 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL397272 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL230998 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL230896 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL427111 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL231517 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL230997 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL231104 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL231619 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL387579 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL231535 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL395262 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL231422 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL439007 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL231227 | — | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL397273 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL231519 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL231437 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL231436 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL396960 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL230919 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL437165 | — | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL231106 | — | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL437195 | — | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL231225 | — | IC50 | = | 26.9 | nM | 7.57 |
| CHEMBL438656 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL388032 | — | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL231438 | — | IC50 | = | 35.3 | nM | 7.45 |
| CHEMBL396713 | — | IC50 | = | 39.3 | nM | 7.41 |
| CHEMBL231226 | — | IC50 | = | 43.2 | nM | 7.37 |
| CHEMBL231520 | — | IC50 | = | 54.5 | nM | 7.26 |
| CHEMBL396714 | — | IC50 | = | 58.8 | nM | 7.23 |
| CHEMBL231019 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL231105 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL230485 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL230689 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL231020 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL387995 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL230380 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL387578 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL388870 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL231238 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL388871 | — | IC50 | = | 902.0 | nM | 6.04 |
| CHEMBL442070 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL230379 | — | IC50 | = | 7360.0 | nM | 5.13 |