Assay Detail
Functional
CHEMBL874942
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of pH-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
63
Total Activities
62
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 | 63 | 6.62 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL190874 | — | — | 1 | 9.00 |
| CHEMBL191247 | — | — | 1 | 8.89 |
| CHEMBL195115 | — | — | 1 | 8.70 |
| CHEMBL195880 | — | — | 1 | 7.58 |
| CHEMBL439855 | — | — | 1 | 7.40 |
| CHEMBL195546 | — | — | 1 | 7.27 |
| CHEMBL370426 | — | — | 1 | 7.24 |
| CHEMBL195875 | — | — | 1 | 7.15 |
| CHEMBL427181 | — | — | 1 | 7.09 |
| CHEMBL192205 | — | — | 1 | 7.03 |
| CHEMBL370078 | — | — | 1 | 7.00 |
| CHEMBL195876 | — | — | 1 | 6.96 |
| CHEMBL193135 | — | — | 1 | 6.92 |
| CHEMBL195789 | — | — | 2 | 6.82 |
| CHEMBL195803 | — | — | 1 | 6.80 |
| CHEMBL370977 | — | — | 1 | 6.75 |
| CHEMBL191940 | — | — | 1 | 6.66 |
| CHEMBL372930 | — | — | 1 | 6.54 |
| CHEMBL192079 | — | — | 1 | 6.50 |
| CHEMBL192292 | — | — | 1 | 6.43 |
| CHEMBL363632 | — | — | 1 | 6.37 |
| CHEMBL191031 | — | — | 1 | 6.36 |
| CHEMBL195870 | — | — | 1 | 6.33 |
| CHEMBL194449 | — | — | 1 | 6.29 |
| CHEMBL372226 | — | — | 1 | 6.22 |
| CHEMBL191768 | — | — | 1 | 6.18 |
| CHEMBL192201 | — | — | 1 | 6.18 |
| CHEMBL194228 | — | — | 1 | 6.10 |
| CHEMBL191783 | — | — | 1 | 6.07 |
| CHEMBL191807 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL190874 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL191247 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL195115 | — | IC50 | = | 2.02 | nM | 8.70 |
| CHEMBL195880 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL439855 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL195546 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL370426 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL195875 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL427181 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL192205 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL370078 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL195876 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL193135 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL195789 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL195803 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL370977 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL191940 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL372930 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL192079 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL192292 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL363632 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL191031 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL195870 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL194449 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL372226 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL191768 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL192201 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL194228 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL191783 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL191807 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL190818 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL191939 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL194924 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL236139 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL365128 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL191657 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL194280 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL195789 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL192383 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL365354 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL192642 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL192235 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL195374 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL191628 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL192029 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL195112 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL194871 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL192984 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL191782 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL371621 | — | IC50 | > | 4000.0 | nM | - |