Assay Detail
Functional
CHEMBL5442694
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR119
27
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HTLA |
| Category | GPCR beta-arrestin recruitment assay |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glucose-dependent insulinotropic receptor (CHEMBL5652) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
EUbOPEN Chemogenomics Library - GPCR Dose-Respose
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.40 | 5.73 |
| EC50 | 9 | 5.81 | 6.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1368758 | — | — | 1 | 6.97 |
| CHEMBL484929 | — | — | 1 | 6.26 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | 4.0 | 1 | 6.23 |
| CHEMBL1256876 | — | — | 1 | 5.73 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | 4.0 | 1 | 5.72 |
| CHEMBL469695 | — | — | 1 | 5.62 |
| CHEMBL273083 | — | — | 1 | 5.50 |
| CHEMBL259656 | — | — | 1 | 5.50 |
| CHEMBL103769 | — | — | 1 | 5.48 |
| CHEMBL4743495 | — | — | 1 | 5.47 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 5.46 |
| CHEMBL52 | NORDIHYDROGUAIARETIC ACID | — | 1 | 5.45 |
| CHEMBL5089005 | — | — | 1 | 5.42 |
| CHEMBL531742 | — | — | 1 | 5.40 |
| CHEMBL344159 | TOLVAPTAN | 4.0 | 1 | 5.40 |
| CHEMBL1766103 | — | — | 1 | 5.38 |
| CHEMBL502182 | ELAGOLIX SODIUM | 4.0 | 1 | 5.35 |
| CHEMBL494803 | — | — | 1 | 5.35 |
| CHEMBL567 | PERPHENAZINE | 4.0 | 1 | 5.29 |
| CHEMBL5075931 | — | — | 1 | 5.29 |
| CHEMBL1474387 | — | — | 1 | 5.26 |
| CHEMBL1256645 | — | — | 1 | 5.22 |
| CHEMBL2018875 | — | — | 1 | 5.05 |
| CHEMBL3342358 | — | — | 1 | - |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | - |
| CHEMBL2110370 | — | — | 1 | - |
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1368758 | — | EC50 | = | 107.73 | nM | 6.97 |
| CHEMBL484929 | — | EC50 | = | 553.25 | nM | 6.26 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | EC50 | = | 588.7 | nM | 6.23 |
| CHEMBL1256876 | — | IC50 | = | 1865.75 | nM | 5.73 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | EC50 | = | 1914.23 | nM | 5.72 |
| CHEMBL469695 | — | EC50 | = | 2393.89 | nM | 5.62 |
| CHEMBL273083 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL259656 | — | IC50 | = | 3129.2 | nM | 5.50 |
| CHEMBL103769 | — | IC50 | = | 3330.63 | nM | 5.48 |
| CHEMBL4743495 | — | IC50 | = | 3381.96 | nM | 5.47 |
| CHEMBL405355 | NIGULDIPINE | IC50 | = | 3437.79 | nM | 5.46 |
| CHEMBL52 | NORDIHYDROGUAIARETIC ACID | IC50 | = | 3545.26 | nM | 5.45 |
| CHEMBL5089005 | — | IC50 | = | 3809.7 | nM | 5.42 |
| CHEMBL531742 | — | IC50 | = | 4007.06 | nM | 5.40 |
| CHEMBL344159 | TOLVAPTAN | EC50 | = | 4018.74 | nM | 5.40 |
| CHEMBL1766103 | — | IC50 | = | 4167.43 | nM | 5.38 |
| CHEMBL502182 | ELAGOLIX SODIUM | EC50 | = | 4496.51 | nM | 5.35 |
| CHEMBL494803 | — | IC50 | = | 4423.95 | nM | 5.35 |
| CHEMBL567 | PERPHENAZINE | IC50 | = | 5164.56 | nM | 5.29 |
| CHEMBL5075931 | — | IC50 | = | 5172.91 | nM | 5.29 |
| CHEMBL1474387 | — | IC50 | = | 5484.65 | nM | 5.26 |
| CHEMBL1256645 | — | EC50 | = | 5991.24 | nM | 5.22 |
| CHEMBL2018875 | — | IC50 | = | 8847.84 | nM | 5.05 |
| CHEMBL3342358 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1722209 | TOLTERODINE TARTRATE | IC50 | > | 10000.0 | nM | - |
| CHEMBL2110370 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL9506 | DEVAZEPIDE | IC50 | > | 10000.0 | nM | - |