Assay Detail
Binding
CHEMBL5225729
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Antagonist activity at beta-galactosidase fused human GPR55 expressed in CHO cells assessed as inhibition of LPI-induced receptor activation by measuring beta-arrestin 2 recruitment incubated for 90 mins by PathHunter chemiluminescence based assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.46 | 6.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5273189 | — | — | 1 | 6.55 |
| CHEMBL5273001 | — | — | 1 | 6.17 |
| CHEMBL1402920 | — | — | 1 | 5.70 |
| CHEMBL5278819 | — | — | 1 | 5.67 |
| CHEMBL5281110 | — | — | 1 | 5.64 |
| CHEMBL5282587 | — | — | 1 | 5.56 |
| CHEMBL5271818 | — | — | 1 | 5.52 |
| CHEMBL5275607 | — | — | 1 | 5.47 |
| CHEMBL5267293 | — | — | 1 | 5.14 |
| CHEMBL5278170 | — | — | 1 | 5.10 |
| CHEMBL5283686 | — | — | 1 | 5.02 |
| CHEMBL5267388 | — | — | 1 | 4.93 |
| CHEMBL5281025 | — | — | 1 | 4.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5273189 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5273001 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL1402920 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL5278819 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL5281110 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5282587 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL5271818 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5275607 | — | IC50 | = | 3350.0 | nM | 5.47 |
| CHEMBL5267293 | — | IC50 | = | 7160.0 | nM | 5.14 |
| CHEMBL5278170 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL5283686 | — | IC50 | = | 9490.0 | nM | 5.02 |
| CHEMBL5267388 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL5281025 | — | IC50 | = | 29300.0 | nM | 4.53 |