Assay Detail
Functional
CHEMBL874818
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
64
Total Activities
63
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 64 | 7.02 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL190874 | — | — | 1 | 9.38 |
| CHEMBL195115 | — | — | 1 | 8.96 |
| CHEMBL191247 | — | — | 1 | 8.72 |
| CHEMBL195875 | — | — | 1 | 8.60 |
| CHEMBL191607 | — | — | 1 | 8.19 |
| CHEMBL195876 | — | — | 1 | 7.85 |
| CHEMBL439855 | — | — | 1 | 7.82 |
| CHEMBL195880 | — | — | 1 | 7.82 |
| CHEMBL192205 | — | — | 1 | 7.80 |
| CHEMBL370426 | — | — | 1 | 7.80 |
| CHEMBL195789 | — | — | 2 | 7.77 |
| CHEMBL193135 | — | — | 1 | 7.70 |
| CHEMBL195085 | — | — | 1 | 7.68 |
| CHEMBL370977 | — | — | 1 | 7.60 |
| CHEMBL195546 | — | — | 1 | 7.57 |
| CHEMBL363810 | — | — | 1 | 7.52 |
| CHEMBL195803 | — | — | 1 | 7.44 |
| CHEMBL372930 | — | — | 1 | 7.44 |
| CHEMBL363632 | — | — | 1 | 7.41 |
| CHEMBL191768 | — | — | 1 | 7.36 |
| CHEMBL370078 | — | — | 1 | 7.34 |
| CHEMBL427181 | — | — | 1 | 7.26 |
| CHEMBL195870 | — | — | 1 | 7.22 |
| CHEMBL190818 | — | — | 1 | 7.21 |
| CHEMBL194449 | — | — | 1 | 7.11 |
| CHEMBL365128 | — | — | 1 | 7.00 |
| CHEMBL372226 | — | — | 1 | 7.00 |
| CHEMBL365121 | — | — | 1 | 6.96 |
| CHEMBL192292 | — | — | 1 | 6.96 |
| CHEMBL195257 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL190874 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL195115 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL191247 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL195875 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL191607 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL195876 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL439855 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL195880 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL370426 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL192205 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL195789 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL193135 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL195085 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL370977 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL195546 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL363810 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL372930 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL195803 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL363632 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL191768 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL370078 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL427181 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL195870 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL190818 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL194449 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL365128 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL372226 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL192292 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL365121 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL195257 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL192201 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL191940 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL195877 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL191031 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL194228 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL191939 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL192079 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL191756 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL236139 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL426634 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL191783 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL191657 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL191807 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL391997 | CAPSAZEPINE | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL194280 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL194443 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL363841 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL192642 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL192383 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL194924 | — | IC50 | = | 870.0 | nM | 6.06 |