Assay Detail
Functional
CHEMBL3385494
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Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| 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 | 22 | 7.20 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3342370 | — | — | 1 | 9.30 |
| CHEMBL3342371 | — | — | 1 | 9.00 |
| CHEMBL3342377 | — | — | 1 | 8.70 |
| CHEMBL3342367 | — | — | 1 | 8.52 |
| CHEMBL3342374 | — | — | 1 | 8.15 |
| CHEMBL3342378 | — | — | 1 | 8.10 |
| CHEMBL3342376 | — | — | 1 | 8.10 |
| CHEMBL3342366 | — | — | 1 | 8.00 |
| CHEMBL3342372 | — | — | 1 | 7.77 |
| CHEMBL3342362 | — | — | 1 | 7.66 |
| CHEMBL3342373 | — | — | 1 | 7.47 |
| CHEMBL3342359 | — | — | 1 | 6.94 |
| CHEMBL3342375 | — | — | 1 | 6.73 |
| CHEMBL3342368 | — | — | 1 | 6.52 |
| CHEMBL3342365 | — | — | 1 | 6.44 |
| CHEMBL3342360 | — | — | 1 | 5.82 |
| CHEMBL3342369 | — | — | 1 | 5.58 |
| CHEMBL3342364 | — | — | 1 | 5.17 |
| CHEMBL3342361 | — | — | 1 | 5.00 |
| CHEMBL3342363 | — | — | 1 | 5.00 |
| CHEMBL3342358 | — | — | 1 | - |
| CHEMBL3342379 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3342370 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3342371 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3342377 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3342367 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3342374 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3342378 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3342376 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3342366 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3342372 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3342362 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3342373 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3342359 | — | EC50 | = | 115.0 | nM | 6.94 |
| CHEMBL3342375 | — | EC50 | = | 185.0 | nM | 6.73 |
| CHEMBL3342368 | — | EC50 | = | 304.0 | nM | 6.52 |
| CHEMBL3342365 | — | EC50 | = | 365.0 | nM | 6.44 |
| CHEMBL3342360 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3342369 | — | EC50 | = | 2612.0 | nM | 5.58 |
| CHEMBL3342364 | — | EC50 | = | 6716.0 | nM | 5.17 |
| CHEMBL3342361 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3342363 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3342358 | — | EC50 | - | — | - | |
| CHEMBL3342379 | — | EC50 | - | — | - |