Assay Detail
Binding
CHEMBL1058942
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 9.16 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL551466 | ACLIDINIUM BROMIDE | 4.0 | 1 | 9.77 |
| CHEMBL556635 | — | — | 1 | 9.74 |
| CHEMBL564057 | — | — | 1 | 9.70 |
| CHEMBL551729 | — | — | 1 | 9.64 |
| CHEMBL551327 | — | — | 1 | 9.62 |
| CHEMBL556221 | — | — | 1 | 9.62 |
| CHEMBL556222 | — | — | 1 | 9.60 |
| CHEMBL564515 | — | — | 1 | 9.55 |
| CHEMBL564747 | — | — | 1 | 9.51 |
| CHEMBL559106 | — | — | 1 | 9.51 |
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 9.46 |
| CHEMBL551063 | — | — | 1 | 9.43 |
| CHEMBL562642 | — | — | 1 | 9.41 |
| CHEMBL549784 | — | — | 1 | 9.41 |
| CHEMBL556426 | — | — | 1 | 9.38 |
| CHEMBL554725 | — | — | 1 | 9.35 |
| CHEMBL564765 | — | — | 1 | 9.32 |
| CHEMBL561187 | — | — | 1 | 9.23 |
| CHEMBL560327 | — | — | 1 | 9.22 |
| CHEMBL551731 | — | — | 1 | 9.21 |
| CHEMBL561870 | — | — | 1 | 9.15 |
| CHEMBL554699 | — | — | 1 | 9.15 |
| CHEMBL549577 | — | — | 1 | 9.12 |
| CHEMBL558910 | — | — | 1 | 9.05 |
| CHEMBL563887 | — | — | 1 | 9.04 |
| CHEMBL559931 | — | — | 1 | 9.02 |
| CHEMBL562655 | — | — | 1 | 8.98 |
| CHEMBL562890 | — | — | 1 | 8.98 |
| CHEMBL549986 | — | — | 1 | 8.79 |
| CHEMBL563996 | — | — | 1 | 8.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL551466 | ACLIDINIUM BROMIDE | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL556635 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL564057 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL551729 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL551327 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL556221 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL556222 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL564515 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL564747 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL559106 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL3545181 | TIOTROPIUM BROMIDE | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL551063 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL562642 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL549784 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL556426 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL554725 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL564765 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL561187 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL560327 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL551731 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL561870 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL554699 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL549577 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL558910 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL563887 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL559931 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL562655 | — | IC50 | = | 1.04 | nM | 8.98 |
| CHEMBL562890 | — | IC50 | = | 1.04 | nM | 8.98 |
| CHEMBL549986 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL563996 | — | IC50 | = | 1.68 | nM | 8.78 |
| CHEMBL1908368 | — | IC50 | = | 2.07 | nM | 8.68 |
| CHEMBL551525 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL556634 | — | IC50 | = | 200.0 | nM | 6.70 |