Assay Detail
Functional
CHEMBL3384907
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Agonist activity at human 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 | 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 | 22 | 7.30 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3342370 | — | — | 1 | 9.10 |
| CHEMBL3342358 | — | — | 1 | 9.10 |
| CHEMBL3342379 | — | — | 1 | 9.00 |
| CHEMBL3342376 | — | — | 1 | 8.52 |
| CHEMBL3342377 | — | — | 1 | 8.30 |
| CHEMBL3342366 | — | — | 1 | 7.96 |
| CHEMBL3342374 | — | — | 1 | 7.89 |
| CHEMBL3342367 | — | — | 1 | 7.82 |
| CHEMBL3342373 | — | — | 1 | 7.60 |
| CHEMBL3342378 | — | — | 1 | 7.52 |
| CHEMBL3342375 | — | — | 1 | 7.44 |
| CHEMBL3342371 | — | — | 1 | 7.22 |
| CHEMBL3342365 | — | — | 1 | 7.14 |
| CHEMBL3342372 | — | — | 1 | 7.09 |
| CHEMBL3342368 | — | — | 1 | 7.06 |
| CHEMBL3342359 | — | — | 1 | 6.79 |
| CHEMBL3342362 | — | — | 1 | 6.22 |
| CHEMBL3342369 | — | — | 1 | 5.93 |
| CHEMBL3342361 | — | — | 1 | 5.66 |
| CHEMBL3342360 | — | — | 1 | 5.30 |
| CHEMBL3342363 | — | — | 1 | 4.66 |
| CHEMBL3342364 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3342370 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3342358 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3342379 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3342376 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3342377 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3342366 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3342374 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3342367 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3342373 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3342378 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3342375 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3342371 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3342365 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3342372 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3342368 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3342359 | — | EC50 | = | 164.0 | nM | 6.79 |
| CHEMBL3342362 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3342369 | — | EC50 | = | 1181.0 | nM | 5.93 |
| CHEMBL3342361 | — | EC50 | = | 2204.0 | nM | 5.66 |
| CHEMBL3342360 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3342363 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL3342364 | — | EC50 | > | 25000.0 | nM | - |