Assay Detail
Binding
CHEMBL4125101
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human TRPV1 expressed in CHOK1 cells assessed as reduction in capsaicin-induced Ca2+ flux after 15 mins by fluo-4-based FLIPR assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 2-(3,5-difluoro-4-methylsulfonaminophenyl)propanamides as potent TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 8.48 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4125690 | — | — | 1 | 9.70 |
| CHEMBL4129132 | — | — | 1 | 9.52 |
| CHEMBL4127673 | — | — | 1 | 9.22 |
| CHEMBL4127070 | — | — | 1 | 9.15 |
| CHEMBL4129439 | — | — | 1 | 9.10 |
| CHEMBL4129041 | — | — | 1 | 8.92 |
| CHEMBL4125837 | — | — | 1 | 8.80 |
| CHEMBL4129195 | — | — | 1 | 8.64 |
| CHEMBL4129405 | — | — | 1 | 8.62 |
| CHEMBL4130073 | — | — | 1 | 8.57 |
| CHEMBL4127798 | — | — | 1 | 8.49 |
| CHEMBL4128156 | — | — | 1 | 8.36 |
| CHEMBL4125699 | — | — | 1 | 8.06 |
| CHEMBL4127559 | — | — | 1 | 7.92 |
| CHEMBL4126335 | — | — | 1 | 7.64 |
| CHEMBL4126808 | — | — | 1 | 7.38 |
| CHEMBL4128473 | — | — | 1 | 7.36 |
| CHEMBL4127710 | — | — | 1 | 7.26 |
| CHEMBL4127408 | — | — | 1 | - |
| CHEMBL4128954 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4125690 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4129132 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4127673 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4127070 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL4129439 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL4129041 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4125837 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL4129195 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL4129405 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL4130073 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4127798 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL4128156 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL4125699 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL4127559 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL4126335 | — | Ki | = | 22.7 | nM | 7.64 |
| CHEMBL4126808 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4128473 | — | Ki | = | 43.7 | nM | 7.36 |
| CHEMBL4127710 | — | Ki | = | 55.5 | nM | 7.26 |
| CHEMBL4127408 | — | Ki | - | — | - | |
| CHEMBL4128954 | — | Ki | - | — | - |