Assay Detail
Binding
CHEMBL5544509
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV1 receptor assessed as inhibition of TRPV1 channel activation by calcium uptake assay
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 57 | 6.46 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441472 | — | — | 1 | 8.08 |
| CHEMBL5573946 | — | — | 1 | 7.24 |
| CHEMBL5591375 | — | — | 1 | 7.17 |
| CHEMBL5570509 | — | — | 1 | 7.13 |
| CHEMBL5591234 | — | — | 1 | 7.02 |
| CHEMBL5576003 | — | — | 1 | 7.02 |
| CHEMBL5569362 | — | — | 1 | 6.94 |
| CHEMBL5565868 | — | — | 1 | 6.92 |
| CHEMBL5574803 | — | — | 1 | 6.90 |
| CHEMBL5566958 | — | — | 1 | 6.88 |
| CHEMBL5574492 | — | — | 1 | 6.83 |
| CHEMBL5570886 | — | — | 1 | 6.66 |
| CHEMBL5562683 | — | — | 1 | 6.65 |
| CHEMBL5572535 | — | — | 1 | 6.63 |
| CHEMBL5574300 | — | — | 1 | 6.61 |
| CHEMBL191534 | — | — | 1 | 6.58 |
| CHEMBL5569813 | — | — | 1 | 6.41 |
| CHEMBL5573187 | — | — | 1 | 6.35 |
| CHEMBL5564392 | — | — | 1 | 6.33 |
| CHEMBL5572351 | — | — | 1 | 6.30 |
| CHEMBL5569079 | — | — | 1 | 6.29 |
| CHEMBL5592635 | — | — | 1 | 6.25 |
| CHEMBL5566109 | — | — | 1 | 6.24 |
| CHEMBL5575387 | — | — | 1 | 6.20 |
| CHEMBL5572119 | — | — | 1 | 6.20 |
| CHEMBL5564684 | — | — | 1 | 6.18 |
| CHEMBL5569620 | — | — | 1 | 6.17 |
| CHEMBL5567412 | — | — | 1 | 6.16 |
| CHEMBL5566759 | — | — | 1 | 6.13 |
| CHEMBL5570007 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441472 | — | IC50 | = | 8.32 | nM | 8.08 |
| CHEMBL5573946 | — | IC50 | = | 57.8 | nM | 7.24 |
| CHEMBL5591375 | — | IC50 | = | 66.8 | nM | 7.17 |
| CHEMBL5570509 | — | IC50 | = | 73.5 | nM | 7.13 |
| CHEMBL5591234 | — | IC50 | = | 95.3 | nM | 7.02 |
| CHEMBL5576003 | — | IC50 | = | 94.9 | nM | 7.02 |
| CHEMBL5569362 | — | IC50 | = | 114.8 | nM | 6.94 |
| CHEMBL5565868 | — | IC50 | = | 120.2 | nM | 6.92 |
| CHEMBL5574803 | — | IC50 | = | 126.7 | nM | 6.90 |
| CHEMBL5566958 | — | IC50 | = | 130.9 | nM | 6.88 |
| CHEMBL5574492 | — | IC50 | = | 146.1 | nM | 6.83 |
| CHEMBL5570886 | — | IC50 | = | 216.8 | nM | 6.66 |
| CHEMBL5562683 | — | IC50 | = | 224.4 | nM | 6.65 |
| CHEMBL5572535 | — | IC50 | = | 234.4 | nM | 6.63 |
| CHEMBL5574300 | — | IC50 | = | 248.4 | nM | 6.61 |
| CHEMBL191534 | — | IC50 | = | 261.5 | nM | 6.58 |
| CHEMBL5569813 | — | IC50 | = | 393.6 | nM | 6.41 |
| CHEMBL5573187 | — | IC50 | = | 446.8 | nM | 6.35 |
| CHEMBL5564392 | — | IC50 | = | 469.7 | nM | 6.33 |
| CHEMBL5572351 | — | IC50 | = | 497.7 | nM | 6.30 |
| CHEMBL5569079 | — | IC50 | = | 511.9 | nM | 6.29 |
| CHEMBL5592635 | — | IC50 | = | 557.4 | nM | 6.25 |
| CHEMBL5566109 | — | IC50 | = | 573.2 | nM | 6.24 |
| CHEMBL5575387 | — | IC50 | = | 627.8 | nM | 6.20 |
| CHEMBL5572119 | — | IC50 | = | 638.5 | nM | 6.20 |
| CHEMBL5564684 | — | IC50 | = | 658.3 | nM | 6.18 |
| CHEMBL5569620 | — | IC50 | = | 681.5 | nM | 6.17 |
| CHEMBL5567412 | — | IC50 | = | 693.3 | nM | 6.16 |
| CHEMBL5566759 | — | IC50 | = | 735.4 | nM | 6.13 |
| CHEMBL5570007 | — | IC50 | = | 757.3 | nM | 6.12 |
| CHEMBL5583922 | — | IC50 | = | 796.5 | nM | 6.10 |
| CHEMBL5570863 | — | IC50 | = | 816.9 | nM | 6.09 |
| CHEMBL5568875 | — | IC50 | = | 830.6 | nM | 6.08 |
| CHEMBL5572147 | — | IC50 | = | 877.1 | nM | 6.06 |
| CHEMBL5575114 | — | IC50 | = | 867.2 | nM | 6.06 |
| CHEMBL5567326 | — | IC50 | = | 881.9 | nM | 6.05 |
| CHEMBL5592512 | — | IC50 | = | 909.8 | nM | 6.04 |
| CHEMBL5567613 | — | IC50 | = | 906.8 | nM | 6.04 |
| CHEMBL5564915 | — | IC50 | = | 934.2 | nM | 6.03 |
| CHEMBL5593757 | — | IC50 | = | 1112.0 | nM | 5.95 |
| CHEMBL5569204 | — | IC50 | = | 1617.0 | nM | 5.79 |
| CHEMBL5595034 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5570438 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5567044 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5571589 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5574957 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5571224 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5574855 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5595759 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5572581 | — | IC50 | > | 10000.0 | nM | - |