Assay Detail
Functional
CHEMBL5442689
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
44
Total Activities
44
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 | 31 | 6.46 | 9.67 |
| EC50 | 13 | 5.51 | 6.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL499 | TIMOLOL | 4.0 | 1 | 9.67 |
| CHEMBL1256784 | — | — | 1 | 8.83 |
| CHEMBL1256864 | — | — | 1 | 8.71 |
| CHEMBL500 | PINDOLOL | 4.0 | 1 | 8.66 |
| CHEMBL1671 | PROPRANOLOL HYDROCHLORIDE | 4.0 | 1 | 8.65 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 7.83 |
| CHEMBL24778 | SILODOSIN | 4.0 | 1 | 6.67 |
| CHEMBL1691 | BETAXOLOL HYDROCHLORIDE | 4.0 | 1 | 6.20 |
| CHEMBL314639 | — | — | 1 | 6.12 |
| CHEMBL273083 | — | — | 1 | 6.04 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | 4.0 | 1 | 5.87 |
| CHEMBL484929 | — | — | 1 | 5.84 |
| CHEMBL2181247 | — | — | 1 | 5.82 |
| CHEMBL1329567 | XAMOTEROL FUMARATE | -1.0 | 1 | 5.81 |
| CHEMBL1256876 | — | — | 1 | 5.78 |
| CHEMBL4531673 | — | — | 1 | 5.62 |
| CHEMBL5084234 | — | — | 1 | 5.58 |
| CHEMBL2074611 | — | — | 1 | 5.56 |
| CHEMBL567 | PERPHENAZINE | 4.0 | 1 | 5.56 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | 4.0 | 1 | 5.55 |
| CHEMBL5075931 | — | — | 1 | 5.53 |
| CHEMBL79834 | SPIRAMIDE | 2.0 | 1 | 5.52 |
| CHEMBL2178422 | RIMEGEPANT | 4.0 | 1 | 5.50 |
| CHEMBL344159 | TOLVAPTAN | 4.0 | 1 | 5.47 |
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | 5.42 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | 5.41 |
| CHEMBL3342358 | — | — | 1 | 5.37 |
| CHEMBL4743495 | — | — | 1 | 5.36 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 5.35 |
| CHEMBL2111101 | PIMAVANSERIN | 4.0 | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL499 | TIMOLOL | IC50 | = | 0.2153 | nM | 9.67 |
| CHEMBL1256784 | — | IC50 | = | 1.493 | nM | 8.83 |
| CHEMBL1256864 | — | IC50 | = | 1.96 | nM | 8.71 |
| CHEMBL500 | PINDOLOL | IC50 | = | 2.192 | nM | 8.66 |
| CHEMBL1671 | PROPRANOLOL HYDROCHLORIDE | IC50 | = | 2.262 | nM | 8.65 |
| CHEMBL1263 | SALMETEROL | IC50 | = | 14.93 | nM | 7.83 |
| CHEMBL24778 | SILODOSIN | IC50 | = | 214.13 | nM | 6.67 |
| CHEMBL1691 | BETAXOLOL HYDROCHLORIDE | IC50 | = | 627.7 | nM | 6.20 |
| CHEMBL314639 | — | IC50 | = | 750.22 | nM | 6.12 |
| CHEMBL273083 | — | EC50 | = | 917.0 | nM | 6.04 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | EC50 | = | 1336.92 | nM | 5.87 |
| CHEMBL484929 | — | EC50 | = | 1438.21 | nM | 5.84 |
| CHEMBL2181247 | — | IC50 | = | 1508.69 | nM | 5.82 |
| CHEMBL1329567 | XAMOTEROL FUMARATE | IC50 | = | 1546.7 | nM | 5.81 |
| CHEMBL1256876 | — | IC50 | = | 1644.1 | nM | 5.78 |
| CHEMBL4531673 | — | IC50 | = | 2378.77 | nM | 5.62 |
| CHEMBL5084234 | — | IC50 | = | 2661.78 | nM | 5.58 |
| CHEMBL2074611 | — | IC50 | = | 2728.0 | nM | 5.56 |
| CHEMBL567 | PERPHENAZINE | IC50 | = | 2777.1 | nM | 5.56 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | EC50 | = | 2830.0 | nM | 5.55 |
| CHEMBL5075931 | — | IC50 | = | 2932.72 | nM | 5.53 |
| CHEMBL79834 | SPIRAMIDE | IC50 | = | 3044.66 | nM | 5.52 |
| CHEMBL2178422 | RIMEGEPANT | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL344159 | TOLVAPTAN | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL9506 | DEVAZEPIDE | EC50 | = | 3830.0 | nM | 5.42 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | EC50 | = | 3910.0 | nM | 5.41 |
| CHEMBL3342358 | — | EC50 | = | 4226.62 | nM | 5.37 |
| CHEMBL4743495 | — | IC50 | = | 4327.23 | nM | 5.36 |
| CHEMBL267777 | RITANSERIN | EC50 | = | 4435.71 | nM | 5.35 |
| CHEMBL2111101 | PIMAVANSERIN | IC50 | = | 4549.68 | nM | 5.34 |
| CHEMBL1256645 | — | EC50 | = | 4570.0 | nM | 5.34 |
| CHEMBL4803066 | — | IC50 | = | 4677.38 | nM | 5.33 |
| CHEMBL1938952 | — | IC50 | = | 4918.12 | nM | 5.31 |
| CHEMBL502182 | ELAGOLIX SODIUM | EC50 | = | 5480.62 | nM | 5.26 |
| CHEMBL469695 | — | EC50 | = | 5806.46 | nM | 5.24 |
| CHEMBL2331803 | — | IC50 | = | 6138.89 | nM | 5.21 |
| CHEMBL1384502 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2105510 | ZINTEROL HYDROCHLORIDE | IC50 | > | 10000.0 | nM | - |
| CHEMBL2110363 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL475903 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018969 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL405355 | NIGULDIPINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL5094754 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5089005 | — | IC50 | > | 10000.0 | nM | - |