Assay Detail
Functional
CHEMBL5442691
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GPCR PRESTO-Tango dose-response in antagonist mode with target: CHRM2
22
Total Activities
22
Compounds Tested
1
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 | 22 | 5.83 | 8.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 8.65 |
| CHEMBL3833319 | REVEFENACIN | 4.0 | 1 | 7.33 |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 6.45 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | 6.36 |
| CHEMBL449588 | — | — | 1 | 6.22 |
| CHEMBL43383 | — | — | 1 | 6.03 |
| CHEMBL3039518 | BATEFENTEROL | 2.0 | 1 | 6.01 |
| CHEMBL1474387 | — | — | 1 | 5.49 |
| CHEMBL281350 | SB-224289 | — | 1 | 5.47 |
| CHEMBL1256876 | — | — | 1 | 5.45 |
| CHEMBL531742 | — | — | 1 | 5.40 |
| CHEMBL543113 | — | — | 1 | 5.38 |
| CHEMBL4743495 | — | — | 1 | 5.38 |
| CHEMBL5075931 | — | — | 1 | 5.37 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 5.36 |
| CHEMBL1766103 | — | — | 1 | 5.34 |
| CHEMBL5089005 | — | — | 1 | 5.32 |
| CHEMBL2018875 | — | — | 1 | 5.26 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 5.21 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | 4.0 | 1 | 5.18 |
| CHEMBL1200681 | MONTELUKAST SODIUM | 4.0 | 1 | - |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | IC50 | = | 2.239 | nM | 8.65 |
| CHEMBL3833319 | REVEFENACIN | IC50 | = | 46.88 | nM | 7.33 |
| CHEMBL517712 | ATROPINE | IC50 | = | 359.11 | nM | 6.45 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | IC50 | = | 433.67 | nM | 6.36 |
| CHEMBL449588 | — | IC50 | = | 602.2 | nM | 6.22 |
| CHEMBL43383 | — | IC50 | = | 931.3 | nM | 6.03 |
| CHEMBL3039518 | BATEFENTEROL | IC50 | = | 986.67 | nM | 6.01 |
| CHEMBL1474387 | — | IC50 | = | 3238.84 | nM | 5.49 |
| CHEMBL281350 | SB-224289 | IC50 | = | 3422.5 | nM | 5.47 |
| CHEMBL1256876 | — | IC50 | = | 3565.57 | nM | 5.45 |
| CHEMBL531742 | — | IC50 | = | 3980.92 | nM | 5.40 |
| CHEMBL543113 | — | IC50 | = | 4175.12 | nM | 5.38 |
| CHEMBL4743495 | — | IC50 | = | 4151.48 | nM | 5.38 |
| CHEMBL5075931 | — | IC50 | = | 4265.16 | nM | 5.37 |
| CHEMBL405355 | NIGULDIPINE | IC50 | = | 4407.27 | nM | 5.36 |
| CHEMBL1766103 | — | IC50 | = | 4601.91 | nM | 5.34 |
| CHEMBL5089005 | — | IC50 | = | 4841.43 | nM | 5.32 |
| CHEMBL2018875 | — | IC50 | = | 5504.08 | nM | 5.26 |
| CHEMBL111 | RIMONABANT | IC50 | = | 6215.16 | nM | 5.21 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | IC50 | = | 6596.49 | nM | 5.18 |
| CHEMBL1200681 | MONTELUKAST SODIUM | IC50 | > | 10000.0 | nM | - |
| CHEMBL1263 | SALMETEROL | IC50 | > | 10000.0 | nM | - |