Assay Detail
Functional
CHEMBL5442702
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4
32
Total Activities
32
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 | 21 | 5.60 | 6.23 |
| IC50 | 11 | 5.43 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1368758 | — | — | 1 | 6.23 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | 4.0 | 1 | 6.03 |
| CHEMBL4202825 | — | — | 1 | 5.93 |
| CHEMBL484929 | — | — | 1 | 5.92 |
| CHEMBL59898 | — | — | 1 | 5.88 |
| CHEMBL540612 | — | — | 1 | 5.83 |
| CHEMBL3311302 | — | — | 1 | 5.82 |
| CHEMBL3342358 | — | — | 1 | 5.67 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | 4.0 | 1 | 5.59 |
| CHEMBL273083 | — | — | 1 | 5.55 |
| CHEMBL469695 | — | — | 1 | 5.54 |
| CHEMBL3633893 | — | — | 1 | 5.52 |
| CHEMBL2110363 | — | — | 1 | 5.49 |
| CHEMBL5089005 | — | — | 1 | 5.48 |
| CHEMBL10284 | SB-222200 | — | 1 | 5.47 |
| CHEMBL502182 | ELAGOLIX SODIUM | 4.0 | 1 | 5.44 |
| CHEMBL428504 | — | — | 1 | 5.41 |
| CHEMBL2018969 | — | — | 1 | 5.39 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | 5.36 |
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | 5.36 |
| CHEMBL419667 | RELCOVAPTAN | 2.0 | 1 | 5.32 |
| CHEMBL1256645 | — | — | 1 | 5.31 |
| CHEMBL344159 | TOLVAPTAN | 4.0 | 1 | 5.29 |
| CHEMBL531742 | — | — | 1 | 4.99 |
| CHEMBL122972 | 2-ARACHIDONOYLGLYCEROL | — | 1 | - |
| CHEMBL518199 | — | — | 1 | - |
| CHEMBL230963 | — | — | 1 | - |
| CHEMBL174588 | — | — | 1 | - |
| CHEMBL2018875 | — | — | 1 | - |
| CHEMBL5084234 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1368758 | — | EC50 | = | 585.29 | nM | 6.23 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | EC50 | = | 944.41 | nM | 6.03 |
| CHEMBL4202825 | — | EC50 | = | 1178.07 | nM | 5.93 |
| CHEMBL484929 | — | EC50 | = | 1210.33 | nM | 5.92 |
| CHEMBL59898 | — | EC50 | = | 1306.47 | nM | 5.88 |
| CHEMBL540612 | — | EC50 | = | 1479.66 | nM | 5.83 |
| CHEMBL3311302 | — | IC50 | = | 1520.57 | nM | 5.82 |
| CHEMBL3342358 | — | EC50 | = | 2116.63 | nM | 5.67 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | EC50 | = | 2571.77 | nM | 5.59 |
| CHEMBL273083 | — | EC50 | = | 2839.56 | nM | 5.55 |
| CHEMBL469695 | — | EC50 | = | 2905.57 | nM | 5.54 |
| CHEMBL3633893 | — | EC50 | = | 3000.42 | nM | 5.52 |
| CHEMBL2110363 | — | EC50 | = | 3234.58 | nM | 5.49 |
| CHEMBL5089005 | — | IC50 | = | 3309.13 | nM | 5.48 |
| CHEMBL10284 | SB-222200 | EC50 | = | 3397.76 | nM | 5.47 |
| CHEMBL502182 | ELAGOLIX SODIUM | EC50 | = | 3615.37 | nM | 5.44 |
| CHEMBL428504 | — | EC50 | = | 3902.61 | nM | 5.41 |
| CHEMBL2018969 | — | EC50 | = | 4114.12 | nM | 5.39 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | EC50 | = | 4324.25 | nM | 5.36 |
| CHEMBL9506 | DEVAZEPIDE | EC50 | = | 4368.18 | nM | 5.36 |
| CHEMBL419667 | RELCOVAPTAN | EC50 | = | 4775.24 | nM | 5.32 |
| CHEMBL1256645 | — | EC50 | = | 4847.96 | nM | 5.31 |
| CHEMBL344159 | TOLVAPTAN | EC50 | = | 5108.13 | nM | 5.29 |
| CHEMBL531742 | — | IC50 | = | 10335.6 | nM | 4.99 |
| CHEMBL122972 | 2-ARACHIDONOYLGLYCEROL | IC50 | > | 10000.0 | nM | - |
| CHEMBL518199 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL230963 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL174588 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018875 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5084234 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5087555 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2110370 | — | IC50 | > | 10000.0 | nM | - |