Assay Detail
Functional
CHEMBL1070096
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Antagonist activity at TRPV1 in Sprague-Dawley rat DRG neuron assessed as reduction of capsaicin-stimulated intracellular 45Ca2+ influx by scintillation counting
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL5102) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Silicon switch approach in TRPV1 antagonist MK-056 and its analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.54 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388824 | — | — | 1 | 7.40 |
| CHEMBL412885 | — | — | 1 | 7.30 |
| CHEMBL228451 | — | — | 1 | 6.96 |
| CHEMBL606239 | — | — | 1 | 6.82 |
| CHEMBL604370 | — | — | 1 | 6.80 |
| CHEMBL590999 | — | — | 1 | 6.68 |
| CHEMBL589786 | — | — | 1 | 6.17 |
| CHEMBL591956 | — | — | 1 | 5.92 |
| CHEMBL590026 | — | — | 1 | 5.82 |
| CHEMBL590998 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388824 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL412885 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL228451 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL606239 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL604370 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL590999 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL589786 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL591956 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL590026 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL590998 | — | IC50 | = | 3100.0 | nM | 5.51 |