Assay Detail
Binding
CHEMBL4731299
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Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis
18
Total Activities
18
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
Discovery of Tricyclic Xanthines as Agonists of the Cannabinoid-Activated Orphan G-Protein-Coupled Receptor GPR18.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 5.95 | 6.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4758188 | — | — | 1 | 6.34 |
| CHEMBL239232 | — | — | 1 | 6.25 |
| CHEMBL4780863 | — | — | 1 | 5.25 |
| CHEMBL499876 | — | — | 1 | - |
| CHEMBL4752691 | — | — | 1 | - |
| CHEMBL1584113 | — | — | 1 | - |
| CHEMBL4755420 | — | — | 1 | - |
| CHEMBL4755181 | — | — | 1 | - |
| CHEMBL4745658 | — | — | 1 | - |
| CHEMBL4793383 | — | — | 1 | - |
| CHEMBL161343 | ARACHIDONOYL GLYCINE | — | 1 | - |
| CHEMBL239864 | — | — | 1 | - |
| CHEMBL239230 | — | — | 1 | - |
| CHEMBL392941 | — | — | 1 | - |
| CHEMBL392335 | — | — | 1 | - |
| CHEMBL4781871 | — | — | 1 | - |
| CHEMBL239234 | — | — | 1 | - |
| CHEMBL241617 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4758188 | — | EC50 | = | 454.0 | nM | 6.34 |
| CHEMBL239232 | — | EC50 | = | 562.0 | nM | 6.25 |
| CHEMBL4780863 | — | EC50 | = | 5680.0 | nM | 5.25 |
| CHEMBL499876 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4752691 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1584113 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4755420 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4755181 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4745658 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4793383 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL161343 | ARACHIDONOYL GLYCINE | EC50 | > | 10000.0 | nM | - |
| CHEMBL239864 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL239230 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL392941 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL392335 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4781871 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL239234 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL241617 | — | EC50 | > | 10000.0 | nM | - |