Assay Detail
Functional
CHEMBL1775788
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR119 by melanophore assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glucose-dependent insulinotropic receptor (CHEMBL5652) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 32 | 8.04 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1773283 | — | — | 1 | 9.30 |
| CHEMBL1773292 | — | — | 1 | 9.22 |
| CHEMBL461384 | — | — | 1 | 9.19 |
| CHEMBL1773293 | — | — | 1 | 9.15 |
| CHEMBL1775178 | — | — | 1 | 9.05 |
| CHEMBL1775169 | — | — | 1 | 8.96 |
| CHEMBL1775179 | — | — | 1 | 8.57 |
| CHEMBL1773287 | — | — | 1 | 8.47 |
| CHEMBL1773281 | — | — | 1 | 8.47 |
| CHEMBL1775171 | — | — | 1 | 8.46 |
| CHEMBL1775170 | — | — | 1 | 8.42 |
| CHEMBL1775173 | — | — | 1 | 8.38 |
| CHEMBL462196 | — | — | 1 | 8.29 |
| CHEMBL1773282 | — | — | 1 | 8.25 |
| CHEMBL1773280 | — | — | 1 | 8.20 |
| CHEMBL1773286 | — | — | 1 | 8.14 |
| CHEMBL1773291 | — | — | 1 | 8.13 |
| CHEMBL1775172 | — | — | 1 | 8.12 |
| CHEMBL1775176 | — | — | 1 | 8.09 |
| CHEMBL1773279 | — | — | 1 | 7.94 |
| CHEMBL1773294 | — | — | 1 | 7.85 |
| CHEMBL1775174 | — | — | 1 | 7.84 |
| CHEMBL1773288 | — | — | 1 | 7.82 |
| CHEMBL1773290 | — | — | 1 | 7.48 |
| CHEMBL1773295 | — | — | 1 | 7.38 |
| CHEMBL1773289 | — | — | 1 | 6.94 |
| CHEMBL1773277 | — | — | 1 | 6.60 |
| CHEMBL1773278 | — | — | 1 | 6.58 |
| CHEMBL1775175 | — | — | 1 | 6.36 |
| CHEMBL1773284 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1773283 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1773292 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL461384 | — | EC50 | = | 0.65 | nM | 9.19 |
| CHEMBL1773293 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL1775178 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1775169 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1775179 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL1773287 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL1773281 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL1775171 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1775170 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL1775173 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL462196 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL1773282 | — | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL1773280 | — | EC50 | = | 6.3 | nM | 8.20 |
| CHEMBL1773286 | — | EC50 | = | 7.3 | nM | 8.14 |
| CHEMBL1773291 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1775172 | — | EC50 | = | 7.5 | nM | 8.12 |
| CHEMBL1775176 | — | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL1773279 | — | EC50 | = | 11.6 | nM | 7.94 |
| CHEMBL1773294 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1775174 | — | EC50 | = | 14.6 | nM | 7.84 |
| CHEMBL1773288 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1773290 | — | EC50 | = | 33.4 | nM | 7.48 |
| CHEMBL1773295 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1773289 | — | EC50 | = | 116.0 | nM | 6.94 |
| CHEMBL1773277 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1773278 | — | EC50 | = | 265.0 | nM | 6.58 |
| CHEMBL1775175 | — | EC50 | = | 435.0 | nM | 6.36 |
| CHEMBL1773284 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1775177 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1773285 | — | EC50 | > | 10000.0 | nM | - |