Assay Detail
Binding
CHEMBL4014238
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Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
20
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Probable G-protein coupled receptor 34 (CHEMBL3562165) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Probing the Hydrophobic Binding Pocket of G-Protein-Coupled Lysophosphatidylserine Receptor GPR34/LPS1 by Docking-Aided Structure-Activity Analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 7.03 | 7.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4095241 | — | — | 2 | 7.83 |
| CHEMBL4096239 | — | — | 2 | 7.57 |
| CHEMBL4098603 | — | — | 2 | 7.39 |
| CHEMBL4090880 | — | — | 2 | 7.11 |
| CHEMBL4072692 | — | — | 2 | 7.05 |
| CHEMBL3814092 | — | — | 2 | 6.82 |
| CHEMBL4084094 | — | — | 2 | 6.75 |
| CHEMBL4068969 | — | — | 2 | 6.64 |
| CHEMBL1742484 | — | — | 2 | 6.61 |
| CHEMBL4089962 | — | — | 2 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4095241 | — | EC50 | = | 14.79 | nM | 7.83 |
| CHEMBL4095241 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4096239 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4096239 | — | EC50 | = | 26.92 | nM | 7.57 |
| CHEMBL4098603 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4098603 | — | EC50 | = | 40.74 | nM | 7.39 |
| CHEMBL4090880 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4090880 | — | EC50 | = | 77.62 | nM | 7.11 |
| CHEMBL4072692 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4072692 | — | EC50 | = | 95.5 | nM | 7.02 |
| CHEMBL3814092 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3814092 | — | EC50 | = | 151.36 | nM | 6.82 |
| CHEMBL4084094 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4084094 | — | EC50 | = | 181.97 | nM | 6.74 |
| CHEMBL4068969 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4068969 | — | EC50 | = | 229.09 | nM | 6.64 |
| CHEMBL1742484 | — | EC50 | = | 245.47 | nM | 6.61 |
| CHEMBL1742484 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4089962 | — | EC50 | = | 295.12 | nM | 6.53 |
| CHEMBL4089962 | — | EC50 | = | 300.0 | nM | 6.52 |