Assay Detail
Binding
CHEMBL2446589
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV1 expressed in CHOK1 cells assessed as inhibition of capsaicin-induced activity by FLIPR assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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
TRPV1 antagonist with high analgesic efficacy: 2-Thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 8.45 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177429 | — | — | 1 | 9.70 |
| CHEMBL2442912 | — | — | 1 | 9.40 |
| CHEMBL2442916 | — | — | 1 | 9.30 |
| CHEMBL2442897 | — | — | 1 | 9.15 |
| CHEMBL2442894 | — | — | 1 | 9.15 |
| CHEMBL2442911 | — | — | 1 | 9.05 |
| CHEMBL2442918 | — | — | 1 | 9.00 |
| CHEMBL2442910 | — | — | 1 | 8.92 |
| CHEMBL2442928 | — | — | 1 | 8.72 |
| CHEMBL2442917 | — | — | 1 | 8.72 |
| CHEMBL2442920 | — | — | 1 | 8.64 |
| CHEMBL2442900 | — | — | 1 | 8.64 |
| CHEMBL2442923 | — | — | 1 | 8.64 |
| CHEMBL2442895 | — | — | 1 | 8.60 |
| CHEMBL2442919 | — | — | 1 | 8.59 |
| CHEMBL2442905 | — | — | 1 | 8.54 |
| CHEMBL2442904 | — | — | 1 | 8.52 |
| CHEMBL2442922 | — | — | 1 | 8.49 |
| CHEMBL2442903 | — | — | 1 | 8.48 |
| CHEMBL2442925 | — | — | 1 | 8.41 |
| CHEMBL2442898 | — | — | 1 | 8.37 |
| CHEMBL2442924 | — | — | 1 | 8.31 |
| CHEMBL2442896 | — | — | 1 | 8.25 |
| CHEMBL2442899 | — | — | 1 | 8.15 |
| CHEMBL2442921 | — | — | 1 | 8.06 |
| CHEMBL2442926 | — | — | 1 | 7.84 |
| CHEMBL2442927 | — | — | 1 | 7.82 |
| CHEMBL2442902 | — | — | 1 | 7.56 |
| CHEMBL2042399 | — | — | 1 | 7.55 |
| CHEMBL2442913 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177429 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2442912 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2442916 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL2442897 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2442894 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2442911 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL2442918 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2442910 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2442928 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL2442917 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL2442920 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL2442923 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL2442900 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL2442895 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL2442919 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL2442905 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL2442904 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2442922 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL2442903 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL2442925 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL2442898 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL2442924 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL2442896 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL2442899 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2442921 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL2442926 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL2442927 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2442902 | — | Ki | = | 27.4 | nM | 7.56 |
| CHEMBL2042399 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2442913 | — | Ki | = | 43.5 | nM | 7.36 |
| CHEMBL2442908 | — | Ki | = | 48.2 | nM | 7.32 |
| CHEMBL2442909 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL2442901 | — | Ki | - | — | - | |
| CHEMBL2442906 | — | Ki | - | — | - | |
| CHEMBL2442907 | — | Ki | - | — | - | |
| CHEMBL2442914 | — | Ki | - | — | - | |
| CHEMBL2442915 | — | Ki | - | — | - |