Assay Detail
Functional
CHEMBL1686904
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Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 7.09 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1682261 | — | — | 1 | 7.80 |
| CHEMBL1682264 | — | — | 1 | 7.80 |
| CHEMBL1682269 | — | — | 1 | 7.70 |
| CHEMBL1682262 | — | — | 1 | 7.70 |
| CHEMBL559612 | CP-55940 | — | 1 | 7.70 |
| CHEMBL1209708 | — | — | 1 | 7.60 |
| CHEMBL1682278 | — | — | 1 | 7.50 |
| CHEMBL1682272 | — | — | 1 | 7.40 |
| CHEMBL188 | WIN-552122 | — | 1 | 7.30 |
| CHEMBL1682273 | — | — | 1 | 7.30 |
| CHEMBL1682267 | — | — | 1 | 7.10 |
| CHEMBL1682268 | — | — | 1 | 7.10 |
| CHEMBL1681794 | — | — | 1 | 7.10 |
| CHEMBL1682271 | — | — | 1 | 7.00 |
| CHEMBL1682275 | — | — | 1 | 6.90 |
| CHEMBL1682265 | — | — | 1 | 6.80 |
| CHEMBL1682276 | — | — | 1 | 6.70 |
| CHEMBL1682270 | — | — | 1 | 6.70 |
| CHEMBL1682274 | — | — | 1 | 6.60 |
| CHEMBL1682266 | — | — | 1 | 6.40 |
| CHEMBL1682263 | — | — | 1 | 6.10 |
| CHEMBL1682277 | — | — | 1 | 5.70 |
| CHEMBL1682279 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1682261 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL1682264 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL1682269 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL1682262 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL559612 | CP-55940 | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL1209708 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL1682278 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1682272 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL188 | WIN-552122 | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL1682273 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL1682267 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL1682268 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL1681794 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL1682271 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1682275 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL1682265 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL1682276 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL1682270 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL1682274 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL1682266 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL1682263 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL1682277 | — | EC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL1682279 | — | EC50 | <= | 100.0 | nM | - |