Assay Detail
Binding
CHEMBL828688
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Inhibition of 100 nM capsaicin effect on intracellular [Ca2+] concentration in HEK293 cells expressing human TRPV1
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
The taming of capsaicin. Reversal of the vanilloid activity of N-acylvanillamines by aromatic iodination.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.43 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL408581 | — | — | 1 | 9.40 |
| CHEMBL177809 | — | — | 1 | 8.00 |
| CHEMBL190554 | — | — | 1 | 7.79 |
| CHEMBL190707 | — | — | 1 | 7.46 |
| CHEMBL187993 | — | — | 1 | 7.30 |
| CHEMBL373333 | — | — | 1 | 7.29 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | 7.25 |
| CHEMBL365972 | — | — | 1 | 6.90 |
| CHEMBL414663 | — | — | 1 | 6.60 |
| CHEMBL190452 | — | — | 1 | 6.45 |
| CHEMBL190051 | — | — | 1 | 6.41 |
| CHEMBL191184 | — | — | 1 | 6.20 |
| CHEMBL193046 | — | — | 1 | 5.56 |
| CHEMBL190052 | — | — | 1 | 5.47 |
| CHEMBL191117 | — | — | 1 | 5.47 |
| CHEMBL191098 | — | — | 1 | 5.41 |
| CHEMBL189913 | — | — | 1 | 5.02 |
| CHEMBL426272 | — | — | 1 | 4.98 |
| CHEMBL190663 | — | — | 1 | 4.96 |
| CHEMBL191198 | — | — | 1 | 4.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL408581 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL177809 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL190554 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL190707 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL187993 | — | IC50 | = | 50.3 | nM | 7.30 |
| CHEMBL373333 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL391997 | CAPSAZEPINE | IC50 | = | 56.2 | nM | 7.25 |
| CHEMBL365972 | — | IC50 | = | 126.2 | nM | 6.90 |
| CHEMBL414663 | — | IC50 | = | 251.6 | nM | 6.60 |
| CHEMBL190452 | — | IC50 | = | 355.3 | nM | 6.45 |
| CHEMBL190051 | — | IC50 | = | 389.6 | nM | 6.41 |
| CHEMBL191184 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL193046 | — | IC50 | = | 2740.0 | nM | 5.56 |
| CHEMBL190052 | — | IC50 | = | 3402.0 | nM | 5.47 |
| CHEMBL191117 | — | IC50 | = | 3383.0 | nM | 5.47 |
| CHEMBL191098 | — | IC50 | = | 3932.0 | nM | 5.41 |
| CHEMBL189913 | — | IC50 | = | 9544.0 | nM | 5.02 |
| CHEMBL426272 | — | IC50 | = | 10380.0 | nM | 4.98 |
| CHEMBL190663 | — | IC50 | = | 10970.0 | nM | 4.96 |
| CHEMBL191198 | — | IC50 | = | 17490.0 | nM | 4.76 |