Assay Detail
Functional
CHEMBL5043709
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Antagonist activity at N-terminal tagged human CB1 receptor transfected with HEK293 cells assessed as forskolin-stimulated cAMP level in presence of CP55940 by BRET assay
19
Total Activities
19
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
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 |
|---|---|---|---|
| IC50 | 19 | 5.66 | 6.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5092369 | — | — | 1 | 6.17 |
| CHEMBL5086597 | — | — | 1 | 6.14 |
| CHEMBL5093337 | — | — | 1 | 6.06 |
| CHEMBL5079805 | — | — | 1 | 6.04 |
| CHEMBL5088172 | — | — | 1 | 5.94 |
| CHEMBL5080578 | — | — | 1 | 5.87 |
| CHEMBL5080045 | — | — | 1 | 5.82 |
| CHEMBL5077926 | — | — | 1 | 5.77 |
| CHEMBL5087480 | — | — | 1 | 5.75 |
| CHEMBL5084600 | — | — | 1 | 5.69 |
| CHEMBL5087483 | — | — | 1 | 5.49 |
| CHEMBL1360165 | — | — | 1 | 5.46 |
| CHEMBL1289260 | — | — | 1 | 5.38 |
| CHEMBL5077368 | — | — | 1 | 5.36 |
| CHEMBL5081586 | — | — | 1 | 5.18 |
| CHEMBL5082643 | — | — | 1 | 5.11 |
| CHEMBL5089573 | — | — | 1 | 4.97 |
| CHEMBL2299364 | — | — | 1 | - |
| CHEMBL5087934 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5092369 | — | IC50 | = | 676.08 | nM | 6.17 |
| CHEMBL5086597 | — | IC50 | = | 724.44 | nM | 6.14 |
| CHEMBL5093337 | — | IC50 | = | 870.96 | nM | 6.06 |
| CHEMBL5079805 | — | IC50 | = | 912.01 | nM | 6.04 |
| CHEMBL5088172 | — | IC50 | = | 1148.15 | nM | 5.94 |
| CHEMBL5080578 | — | IC50 | = | 1348.96 | nM | 5.87 |
| CHEMBL5080045 | — | IC50 | = | 1513.56 | nM | 5.82 |
| CHEMBL5077926 | — | IC50 | = | 1698.24 | nM | 5.77 |
| CHEMBL5087480 | — | IC50 | = | 1778.28 | nM | 5.75 |
| CHEMBL5084600 | — | IC50 | = | 2041.74 | nM | 5.69 |
| CHEMBL5087483 | — | IC50 | = | 3235.94 | nM | 5.49 |
| CHEMBL1360165 | — | IC50 | = | 3467.37 | nM | 5.46 |
| CHEMBL1289260 | — | IC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL5077368 | — | IC50 | = | 4365.16 | nM | 5.36 |
| CHEMBL5081586 | — | IC50 | = | 6606.93 | nM | 5.18 |
| CHEMBL5082643 | — | IC50 | = | 7762.47 | nM | 5.11 |
| CHEMBL5089573 | — | IC50 | = | 10715.19 | nM | 4.97 |
| CHEMBL2299364 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5087934 | — | IC50 | > | 10000.0 | nM | - |