Assay Detail
Binding
CHEMBL3772450
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced (45)Ca2+ uptake after 5 mins by liquid scintillation counting analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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
2-Sulfonamidopyridine C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 8.18 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177429 | — | — | 1 | 8.90 |
| CHEMBL3770682 | — | — | 1 | 8.74 |
| CHEMBL3770852 | — | — | 1 | 8.67 |
| CHEMBL2177428 | — | — | 1 | 8.65 |
| CHEMBL3770091 | — | — | 1 | 8.52 |
| CHEMBL3771317 | — | — | 1 | 8.50 |
| CHEMBL3770984 | — | — | 1 | 8.41 |
| CHEMBL3769458 | — | — | 1 | 8.26 |
| CHEMBL3769673 | — | — | 1 | 8.24 |
| CHEMBL3770027 | — | — | 1 | 8.23 |
| CHEMBL3770670 | — | — | 1 | 8.22 |
| CHEMBL3771342 | — | — | 1 | 8.22 |
| CHEMBL3771109 | — | — | 1 | 8.21 |
| CHEMBL3770685 | — | — | 1 | 8.15 |
| CHEMBL3771102 | — | — | 1 | 8.13 |
| CHEMBL3770864 | — | — | 1 | 8.10 |
| CHEMBL3769821 | — | — | 1 | 8.07 |
| CHEMBL3770908 | — | — | 1 | 8.00 |
| CHEMBL3770191 | — | — | 1 | 7.93 |
| CHEMBL3770362 | — | — | 1 | 7.92 |
| CHEMBL3771332 | — | — | 1 | 7.60 |
| CHEMBL3769847 | — | — | 1 | 7.56 |
| CHEMBL3770156 | — | — | 1 | 7.00 |
| CHEMBL3770394 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177429 | — | Ki | = | 1.26 | nM | 8.90 |
| CHEMBL3770682 | — | Ki | = | 1.81 | nM | 8.74 |
| CHEMBL3770852 | — | Ki | = | 2.14 | nM | 8.67 |
| CHEMBL2177428 | — | Ki | = | 2.22 | nM | 8.65 |
| CHEMBL3770091 | — | Ki | = | 2.99 | nM | 8.52 |
| CHEMBL3771317 | — | Ki | = | 3.13 | nM | 8.50 |
| CHEMBL3770984 | — | Ki | = | 3.87 | nM | 8.41 |
| CHEMBL3769458 | — | Ki | = | 5.54 | nM | 8.26 |
| CHEMBL3769673 | — | Ki | = | 5.77 | nM | 8.24 |
| CHEMBL3770027 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL3770670 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3771342 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3771109 | — | Ki | = | 6.19 | nM | 8.21 |
| CHEMBL3770685 | — | Ki | = | 7.08 | nM | 8.15 |
| CHEMBL3771102 | — | Ki | = | 7.37 | nM | 8.13 |
| CHEMBL3770864 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL3769821 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL3770908 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3770191 | — | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL3770362 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL3771332 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL3769847 | — | Ki | = | 27.6 | nM | 7.56 |
| CHEMBL3770156 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3770394 | — | Ki | - | — | - |