Assay Detail
Functional
CHEMBL4416382
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Allosteric modulator activity at human CB1 receptor expressed in HEK293 cells assessed as suppression of 100 nM CP55,940-induced reduction in forskolin-stimulated cAMP production pre-incubated for 25 mins before forskolin and CP55,940 addition and measured after 22 mins by BRET CAMYEL cAMP assay
20
Total Activities
20
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
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.65 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4464917 | — | — | 1 | 5.92 |
| CHEMBL4527602 | — | — | 1 | 5.75 |
| CHEMBL4581327 | — | — | 1 | 5.75 |
| CHEMBL4584483 | — | — | 1 | 5.73 |
| CHEMBL4590582 | — | — | 1 | 5.64 |
| CHEMBL3341861 | — | — | 1 | 5.58 |
| CHEMBL4513477 | — | — | 1 | 5.20 |
| CHEMBL4572697 | — | — | 1 | - |
| CHEMBL4580323 | — | — | 1 | - |
| CHEMBL4450625 | — | — | 1 | - |
| CHEMBL4438047 | — | — | 1 | - |
| CHEMBL4452850 | — | — | 1 | - |
| CHEMBL4442623 | — | — | 1 | - |
| CHEMBL4554290 | — | — | 1 | - |
| CHEMBL4577767 | — | — | 1 | - |
| CHEMBL4472252 | — | — | 1 | - |
| CHEMBL4474515 | — | — | 1 | - |
| CHEMBL4450873 | — | — | 1 | - |
| CHEMBL4565127 | — | — | 1 | - |
| CHEMBL4544453 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4464917 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL4527602 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL4581327 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4584483 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL4590582 | — | IC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL3341861 | — | IC50 | = | 2620.0 | nM | 5.58 |
| CHEMBL4513477 | — | IC50 | = | 6350.0 | nM | 5.20 |
| CHEMBL4572697 | — | IC50 | - | — | - | |
| CHEMBL4580323 | — | IC50 | - | — | - | |
| CHEMBL4450625 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4438047 | — | IC50 | - | — | - | |
| CHEMBL4452850 | — | IC50 | - | — | - | |
| CHEMBL4442623 | — | IC50 | - | — | - | |
| CHEMBL4554290 | — | IC50 | - | — | - | |
| CHEMBL4577767 | — | IC50 | - | — | - | |
| CHEMBL4472252 | — | IC50 | - | — | - | |
| CHEMBL4474515 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4450873 | — | IC50 | - | — | - | |
| CHEMBL4565127 | — | IC50 | - | — | - | |
| CHEMBL4544453 | — | IC50 | - | — | - |