Assay Detail
Functional
CHEMBL5043705
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Allosteric antagonist activity against mouse CB1 receptor expressed in HEK293 cells membrane measured after 60 mins by [35S]GTPgammaS binding assay
19
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of 3-(4-Chlorophenyl)-1-(phenethyl)urea Analogues as Allosteric Modulators of the Cannabinoid Type-1 Receptor: RTICBM-189 is Brain Penetrant and Attenuates Reinstatement of Cocaine-Seeking Behavior.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| pIC50 | 11 | - | - |
| IC50 | 8 | 5.88 | 6.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080045 | — | — | 1 | 6.25 |
| CHEMBL5092369 | — | — | 1 | 6.12 |
| CHEMBL5087480 | — | — | 1 | 6.11 |
| CHEMBL5077926 | — | — | 1 | 6.05 |
| CHEMBL5080578 | — | — | 1 | 5.82 |
| CHEMBL1289260 | — | — | 1 | 5.43 |
| CHEMBL5079805 | — | — | 1 | 5.38 |
| CHEMBL5087934 | — | — | 1 | - |
| CHEMBL5082643 | — | — | 1 | - |
| CHEMBL2299364 | — | — | 1 | - |
| CHEMBL5084600 | — | — | 1 | - |
| CHEMBL5088172 | — | — | 1 | - |
| CHEMBL5081586 | — | — | 1 | - |
| CHEMBL5093337 | — | — | 1 | - |
| CHEMBL5086597 | — | — | 1 | - |
| CHEMBL5087483 | — | — | 1 | - |
| CHEMBL5089573 | — | — | 1 | - |
| CHEMBL1360165 | — | — | 1 | - |
| CHEMBL5077368 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080045 | — | IC50 | = | 562.34 | nM | 6.25 |
| CHEMBL5092369 | — | IC50 | = | 758.58 | nM | 6.12 |
| CHEMBL5087480 | — | IC50 | = | 776.25 | nM | 6.11 |
| CHEMBL5077926 | — | IC50 | = | 891.25 | nM | 6.05 |
| CHEMBL5080578 | — | IC50 | = | 1513.56 | nM | 5.82 |
| CHEMBL1289260 | — | IC50 | = | 3715.35 | nM | 5.43 |
| CHEMBL5079805 | — | IC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL5087934 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5082643 | — | pIC50 | - | — | - | |
| CHEMBL2299364 | — | pIC50 | - | — | - | |
| CHEMBL5084600 | — | pIC50 | - | — | - | |
| CHEMBL5088172 | — | pIC50 | - | — | - | |
| CHEMBL5081586 | — | pIC50 | - | — | - | |
| CHEMBL5093337 | — | pIC50 | - | — | - | |
| CHEMBL5086597 | — | pIC50 | - | — | - | |
| CHEMBL5087483 | — | pIC50 | - | — | - | |
| CHEMBL5089573 | — | pIC50 | - | — | - | |
| CHEMBL1360165 | — | pIC50 | - | — | - | |
| CHEMBL5077368 | — | pIC50 | - | — | - |