Assay Detail
Functional
CHEMBL5442701
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GPCR PRESTO-Tango dose-response in antagonist mode with target: GLP1R
25
Total Activities
25
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 |
Publication
EUbOPEN Chemogenomics Library - GPCR Dose-Respose
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 5.55 | 6.31 |
| IC50 | 12 | 5.50 | 5.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1368758 | — | — | 1 | 6.31 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | 4.0 | 1 | 5.95 |
| CHEMBL1256876 | — | — | 1 | 5.84 |
| CHEMBL484929 | — | — | 1 | 5.64 |
| CHEMBL273083 | — | — | 1 | 5.63 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | 4.0 | 1 | 5.62 |
| CHEMBL2181247 | — | — | 1 | 5.61 |
| CHEMBL469695 | — | — | 1 | 5.53 |
| CHEMBL5075931 | — | — | 1 | 5.52 |
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | 5.49 |
| CHEMBL3342358 | — | — | 1 | 5.49 |
| CHEMBL502182 | ELAGOLIX SODIUM | 4.0 | 1 | 5.44 |
| CHEMBL5089005 | — | — | 1 | 5.42 |
| CHEMBL567 | PERPHENAZINE | 4.0 | 1 | 5.41 |
| CHEMBL531742 | — | — | 1 | 5.41 |
| CHEMBL344159 | TOLVAPTAN | 4.0 | 1 | 5.33 |
| CHEMBL2018875 | — | — | 1 | 5.29 |
| CHEMBL1256645 | — | — | 1 | 5.29 |
| CHEMBL1384502 | — | — | 1 | 5.26 |
| CHEMBL2110370 | — | — | 1 | 5.12 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | - |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | - |
| CHEMBL540612 | — | — | 1 | - |
| CHEMBL2164551 | — | — | 1 | - |
| CHEMBL2018969 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1368758 | — | EC50 | = | 490.58 | nM | 6.31 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | EC50 | = | 1136.31 | nM | 5.95 |
| CHEMBL1256876 | — | IC50 | = | 1458.46 | nM | 5.84 |
| CHEMBL484929 | — | EC50 | = | 2265.15 | nM | 5.64 |
| CHEMBL273083 | — | EC50 | = | 2335.55 | nM | 5.63 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | EC50 | = | 2404.63 | nM | 5.62 |
| CHEMBL2181247 | — | IC50 | = | 2478.9 | nM | 5.61 |
| CHEMBL469695 | — | EC50 | = | 2949.46 | nM | 5.53 |
| CHEMBL5075931 | — | IC50 | = | 3021.68 | nM | 5.52 |
| CHEMBL9506 | DEVAZEPIDE | EC50 | = | 3269.66 | nM | 5.49 |
| CHEMBL3342358 | — | EC50 | = | 3222.64 | nM | 5.49 |
| CHEMBL502182 | ELAGOLIX SODIUM | EC50 | = | 3635.69 | nM | 5.44 |
| CHEMBL5089005 | — | IC50 | = | 3821.03 | nM | 5.42 |
| CHEMBL567 | PERPHENAZINE | IC50 | = | 3931.05 | nM | 5.41 |
| CHEMBL531742 | — | IC50 | = | 3864.8 | nM | 5.41 |
| CHEMBL344159 | TOLVAPTAN | EC50 | = | 4643.58 | nM | 5.33 |
| CHEMBL2018875 | — | IC50 | = | 5093.53 | nM | 5.29 |
| CHEMBL1256645 | — | EC50 | = | 5181.06 | nM | 5.29 |
| CHEMBL1384502 | — | EC50 | = | 5541.16 | nM | 5.26 |
| CHEMBL2110370 | — | EC50 | = | 7501.09 | nM | 5.12 |
| CHEMBL267777 | RITANSERIN | IC50 | > | 10000.0 | nM | - |
| CHEMBL1722209 | TOLTERODINE TARTRATE | IC50 | > | 10000.0 | nM | - |
| CHEMBL540612 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2164551 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018969 | — | IC50 | > | 10000.0 | nM | - |