Assay Detail
Functional
CHEMBL3385496
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Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assay
5
Total Activities
5
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
Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 9.42 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3342358 | — | — | 1 | 10.22 |
| CHEMBL3342376 | — | — | 1 | 9.74 |
| CHEMBL3342379 | — | — | 1 | 9.46 |
| CHEMBL3342377 | — | — | 1 | 9.26 |
| CHEMBL1200679 | ZINC CHLORIDE | 4.0 | 1 | 8.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3342358 | — | EC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3342376 | — | EC50 | = | 0.18 | nM | 9.74 |
| CHEMBL3342379 | — | EC50 | = | 0.35 | nM | 9.46 |
| CHEMBL3342377 | — | EC50 | = | 0.55 | nM | 9.26 |
| CHEMBL1200679 | ZINC CHLORIDE | EC50 | = | 3.6 | nM | 8.44 |