Assay Detail
Functional
CHEMBL4416375
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Allosteric modulator activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of 100 nM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method
31
Total Activities
31
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 | 31 | 6.03 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4590582 | — | — | 1 | 7.08 |
| CHEMBL4581327 | — | — | 1 | 6.58 |
| CHEMBL4464917 | — | — | 1 | 6.57 |
| CHEMBL4580323 | — | — | 1 | 6.53 |
| CHEMBL4572697 | — | — | 1 | 6.37 |
| CHEMBL4584483 | — | — | 1 | 6.35 |
| CHEMBL3341861 | — | — | 1 | 6.34 |
| CHEMBL4527602 | — | — | 1 | 6.28 |
| CHEMBL4452850 | — | — | 1 | 6.27 |
| CHEMBL4544453 | — | — | 1 | 6.26 |
| CHEMBL4591294 | — | — | 1 | 6.22 |
| CHEMBL4528445 | — | — | 1 | 6.18 |
| CHEMBL4565127 | — | — | 1 | 6.11 |
| CHEMBL4542852 | — | — | 1 | 6.05 |
| CHEMBL4438047 | — | — | 1 | 5.93 |
| CHEMBL4450873 | — | — | 1 | 5.76 |
| CHEMBL4442623 | — | — | 1 | 5.70 |
| CHEMBL4577767 | — | — | 1 | 5.60 |
| CHEMBL4577814 | — | — | 1 | 5.56 |
| CHEMBL4554290 | — | — | 1 | 5.49 |
| CHEMBL4513477 | — | — | 1 | 5.48 |
| CHEMBL4472252 | — | — | 1 | 5.46 |
| CHEMBL4450625 | — | — | 1 | 5.30 |
| CHEMBL4474515 | — | — | 1 | 5.20 |
| CHEMBL4542455 | — | — | 1 | - |
| CHEMBL4475934 | — | — | 1 | - |
| CHEMBL4468436 | — | — | 1 | - |
| CHEMBL4539271 | — | — | 1 | - |
| CHEMBL4443540 | — | — | 1 | - |
| CHEMBL4457227 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4590582 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4581327 | — | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL4464917 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL4580323 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL4572697 | — | IC50 | = | 425.0 | nM | 6.37 |
| CHEMBL4584483 | — | IC50 | = | 449.0 | nM | 6.35 |
| CHEMBL3341861 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL4527602 | — | IC50 | = | 524.0 | nM | 6.28 |
| CHEMBL4452850 | — | IC50 | = | 537.0 | nM | 6.27 |
| CHEMBL4544453 | — | IC50 | = | 553.0 | nM | 6.26 |
| CHEMBL4591294 | — | IC50 | = | 604.0 | nM | 6.22 |
| CHEMBL4528445 | — | IC50 | = | 667.0 | nM | 6.18 |
| CHEMBL4565127 | — | IC50 | = | 774.0 | nM | 6.11 |
| CHEMBL4542852 | — | IC50 | = | 888.0 | nM | 6.05 |
| CHEMBL4438047 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL4450873 | — | IC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL4442623 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL4577767 | — | IC50 | = | 2530.0 | nM | 5.60 |
| CHEMBL4577814 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL4554290 | — | IC50 | = | 3230.0 | nM | 5.49 |
| CHEMBL4513477 | — | IC50 | = | 3280.0 | nM | 5.48 |
| CHEMBL4472252 | — | IC50 | = | 3430.0 | nM | 5.46 |
| CHEMBL4450625 | — | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL4474515 | — | IC50 | = | 6330.0 | nM | 5.20 |
| CHEMBL4542455 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4475934 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4468436 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4539271 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4443540 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4457227 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4443032 | — | IC50 | > | 10000.0 | nM | - |