Assay Detail
Binding
CHEMBL3760352
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 7.52 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3758877 | — | — | 1 | 8.68 |
| CHEMBL3341861 | — | — | 1 | 8.42 |
| CHEMBL1553629 | — | — | 1 | 8.04 |
| CHEMBL3758325 | — | — | 1 | 7.55 |
| CHEMBL3758817 | — | — | 1 | 7.55 |
| CHEMBL3759542 | — | — | 1 | 7.37 |
| CHEMBL3758424 | — | — | 1 | 7.19 |
| CHEMBL3758782 | — | — | 1 | 6.68 |
| CHEMBL3758973 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3758877 | — | EC50 | = | 2.09 | nM | 8.68 |
| CHEMBL3341861 | — | EC50 | = | 3.84 | nM | 8.42 |
| CHEMBL1553629 | — | EC50 | = | 9.05 | nM | 8.04 |
| CHEMBL3758325 | — | EC50 | = | 28.2 | nM | 7.55 |
| CHEMBL3758817 | — | EC50 | = | 28.2 | nM | 7.55 |
| CHEMBL3759542 | — | EC50 | = | 42.9 | nM | 7.37 |
| CHEMBL3758424 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3758782 | — | EC50 | = | 209.0 | nM | 6.68 |
| CHEMBL3758973 | — | EC50 | = | 683.0 | nM | 6.17 |