Assay Detail
Functional
CHEMBL2032795
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
26
Total Activities
26
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 |
Publication
N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 7.39 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2029727 | — | — | 1 | 8.72 |
| CHEMBL2029719 | — | — | 1 | 8.54 |
| CHEMBL2029722 | — | — | 1 | 8.21 |
| CHEMBL2029731 | — | — | 1 | 8.01 |
| CHEMBL2029732 | — | — | 1 | 7.89 |
| CHEMBL2029718 | — | — | 1 | 7.79 |
| CHEMBL2029728 | — | — | 1 | 7.62 |
| CHEMBL2029733 | — | — | 1 | 7.51 |
| CHEMBL2029725 | — | — | 1 | 7.40 |
| CHEMBL2029734 | — | — | 1 | 7.36 |
| CHEMBL1950351 | — | — | 1 | 7.31 |
| CHEMBL2029729 | — | — | 1 | 7.29 |
| CHEMBL2029735 | — | — | 1 | 7.21 |
| CHEMBL2029739 | — | — | 1 | 7.15 |
| CHEMBL244403 | — | — | 1 | 7.14 |
| CHEMBL2029736 | — | — | 1 | 7.10 |
| CHEMBL2029724 | — | — | 1 | 7.10 |
| CHEMBL2029721 | — | — | 1 | 7.02 |
| CHEMBL2029737 | — | — | 1 | 7.00 |
| CHEMBL188 | WIN-552122 | — | 1 | 6.95 |
| CHEMBL2029738 | — | — | 1 | 6.76 |
| CHEMBL2029899 | — | — | 1 | 6.54 |
| CHEMBL2029726 | — | — | 1 | 6.35 |
| CHEMBL2029730 | — | — | 1 | - |
| CHEMBL2029720 | — | — | 1 | - |
| CHEMBL2029723 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2029727 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2029719 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2029722 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL2029731 | — | EC50 | = | 9.8 | nM | 8.01 |
| CHEMBL2029732 | — | EC50 | = | 12.9 | nM | 7.89 |
| CHEMBL2029718 | — | EC50 | = | 16.2 | nM | 7.79 |
| CHEMBL2029728 | — | EC50 | = | 24.2 | nM | 7.62 |
| CHEMBL2029733 | — | EC50 | = | 30.7 | nM | 7.51 |
| CHEMBL2029725 | — | EC50 | = | 39.9 | nM | 7.40 |
| CHEMBL2029734 | — | EC50 | = | 43.7 | nM | 7.36 |
| CHEMBL1950351 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2029729 | — | EC50 | = | 51.4 | nM | 7.29 |
| CHEMBL2029735 | — | EC50 | = | 61.4 | nM | 7.21 |
| CHEMBL2029739 | — | EC50 | = | 70.6 | nM | 7.15 |
| CHEMBL244403 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2029736 | — | EC50 | = | 78.7 | nM | 7.10 |
| CHEMBL2029724 | — | EC50 | = | 78.9 | nM | 7.10 |
| CHEMBL2029721 | — | EC50 | = | 95.3 | nM | 7.02 |
| CHEMBL2029737 | — | EC50 | = | 101.0 | nM | 7.00 |
| CHEMBL188 | WIN-552122 | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL2029738 | — | EC50 | = | 173.0 | nM | 6.76 |
| CHEMBL2029899 | — | EC50 | = | 291.0 | nM | 6.54 |
| CHEMBL2029726 | — | EC50 | = | 446.0 | nM | 6.35 |
| CHEMBL2029730 | — | EC50 | - | — | - | |
| CHEMBL2029720 | — | EC50 | - | — | - | |
| CHEMBL2029723 | — | EC50 | - | — | - |