Assay Detail
Functional
CHEMBL5442699
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GPCR PRESTO-Tango dose-response in antagonist mode with target: APLNR
37
Total Activities
37
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 |
|---|---|---|---|
| IC50 | 32 | 5.49 | 6.49 |
| EC50 | 5 | 5.48 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL449588 | — | — | 1 | 6.49 |
| CHEMBL2181247 | — | — | 1 | 5.80 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | 4.0 | 1 | 5.66 |
| CHEMBL469695 | — | — | 1 | 5.65 |
| CHEMBL3716980 | — | — | 1 | 5.59 |
| CHEMBL1256876 | — | — | 1 | 5.56 |
| CHEMBL567 | PERPHENAZINE | 4.0 | 1 | 5.49 |
| CHEMBL5089005 | — | — | 1 | 5.47 |
| CHEMBL428504 | — | — | 1 | 5.47 |
| CHEMBL531742 | — | — | 1 | 5.47 |
| CHEMBL1201082 | FLUOXETINE HYDROCHLORIDE | 4.0 | 1 | 5.47 |
| CHEMBL1766103 | — | — | 1 | 5.47 |
| CHEMBL2111101 | PIMAVANSERIN | 4.0 | 1 | 5.46 |
| CHEMBL502182 | ELAGOLIX SODIUM | 4.0 | 1 | 5.45 |
| CHEMBL5076314 | — | — | 1 | 5.45 |
| CHEMBL281350 | SB-224289 | — | 1 | 5.44 |
| CHEMBL5075931 | — | — | 1 | 5.41 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 5.40 |
| CHEMBL103769 | — | — | 1 | 5.39 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 5.35 |
| CHEMBL2018875 | — | — | 1 | 5.26 |
| CHEMBL1474387 | — | — | 1 | 5.18 |
| CHEMBL1256645 | — | — | 1 | 5.18 |
| CHEMBL1938952 | — | — | 1 | 5.07 |
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | - |
| CHEMBL2110370 | — | — | 1 | - |
| CHEMBL1303 | ROTIGOTINE | 4.0 | 1 | - |
| CHEMBL540612 | — | — | 1 | - |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | - |
| CHEMBL419667 | RELCOVAPTAN | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL449588 | — | IC50 | = | 324.85 | nM | 6.49 |
| CHEMBL2181247 | — | IC50 | = | 1572.55 | nM | 5.80 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | EC50 | = | 2188.88 | nM | 5.66 |
| CHEMBL469695 | — | EC50 | = | 2247.36 | nM | 5.65 |
| CHEMBL3716980 | — | IC50 | = | 2554.7 | nM | 5.59 |
| CHEMBL1256876 | — | IC50 | = | 2779.04 | nM | 5.56 |
| CHEMBL567 | PERPHENAZINE | IC50 | = | 3217.72 | nM | 5.49 |
| CHEMBL1201082 | FLUOXETINE HYDROCHLORIDE | IC50 | = | 3397.78 | nM | 5.47 |
| CHEMBL1766103 | — | IC50 | = | 3353.98 | nM | 5.47 |
| CHEMBL531742 | — | IC50 | = | 3417.03 | nM | 5.47 |
| CHEMBL428504 | — | EC50 | = | 3408.99 | nM | 5.47 |
| CHEMBL5089005 | — | IC50 | = | 3411.35 | nM | 5.47 |
| CHEMBL2111101 | PIMAVANSERIN | IC50 | = | 3436.69 | nM | 5.46 |
| CHEMBL502182 | ELAGOLIX SODIUM | EC50 | = | 3575.08 | nM | 5.45 |
| CHEMBL5076314 | — | IC50 | = | 3563.9 | nM | 5.45 |
| CHEMBL281350 | SB-224289 | IC50 | = | 3632.38 | nM | 5.44 |
| CHEMBL5075931 | — | IC50 | = | 3938.26 | nM | 5.41 |
| CHEMBL405355 | NIGULDIPINE | IC50 | = | 4007.71 | nM | 5.40 |
| CHEMBL103769 | — | IC50 | = | 4057.22 | nM | 5.39 |
| CHEMBL1230609 | FORETINIB | IC50 | = | 4432.7 | nM | 5.35 |
| CHEMBL2018875 | — | IC50 | = | 5429.99 | nM | 5.26 |
| CHEMBL1474387 | — | IC50 | = | 6631.98 | nM | 5.18 |
| CHEMBL1256645 | — | EC50 | = | 6540.61 | nM | 5.18 |
| CHEMBL1938952 | — | IC50 | = | 8580.06 | nM | 5.07 |
| CHEMBL273083 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1368758 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL344159 | TOLVAPTAN | IC50 | > | 10000.0 | nM | - |
| CHEMBL329650 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL482950 | PEXACERFONT | IC50 | > | 10000.0 | nM | - |
| CHEMBL3633893 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1384502 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL419667 | RELCOVAPTAN | IC50 | > | 10000.0 | nM | - |
| CHEMBL1722209 | TOLTERODINE TARTRATE | IC50 | > | 10000.0 | nM | - |
| CHEMBL540612 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1303 | ROTIGOTINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL2110370 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL9506 | DEVAZEPIDE | IC50 | > | 10000.0 | nM | - |