Assay Detail
Functional
CHEMBL1113607
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsazepine-induced calcium mobilization by FLIPR assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.21 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1092853 | — | — | 1 | 9.68 |
| CHEMBL1214342 | — | — | 1 | 9.64 |
| CHEMBL1089824 | — | — | 1 | 9.20 |
| CHEMBL1092852 | — | — | 1 | 9.08 |
| CHEMBL456571 | — | — | 1 | 9.07 |
| CHEMBL214796 | NGD-8243 | 2.0 | 1 | 8.96 |
| CHEMBL1093132 | — | — | 1 | 8.78 |
| CHEMBL1089119 | — | — | 1 | 8.66 |
| CHEMBL1089118 | — | — | 1 | 8.21 |
| CHEMBL1204401 | — | — | 1 | 8.15 |
| CHEMBL3349452 | — | — | 1 | 7.54 |
| CHEMBL3349451 | — | — | 1 | 7.10 |
| CHEMBL1089117 | — | — | 1 | 6.51 |
| CHEMBL3349453 | — | — | 1 | 6.34 |
| CHEMBL1093131 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1092853 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL1214342 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL1089824 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL1092852 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL456571 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL214796 | NGD-8243 | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1093132 | — | IC50 | = | 1.65 | nM | 8.78 |
| CHEMBL1089119 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1089118 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL1204401 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3349452 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3349451 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL1089117 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL3349453 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL1093131 | — | IC50 | = | 665.0 | nM | 6.18 |