Assay Detail
Binding
CHEMBL4390204
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NMS from human M2R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 8.75 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4519930 | — | — | 1 | 9.96 |
| CHEMBL4516342 | — | — | 1 | 9.74 |
| CHEMBL4457734 | — | — | 1 | 9.40 |
| CHEMBL551466 | ACLIDINIUM BROMIDE | 4.0 | 1 | 9.37 |
| CHEMBL4440620 | — | — | 1 | 9.31 |
| CHEMBL4450188 | — | — | 1 | 9.31 |
| CHEMBL4461243 | — | — | 1 | 9.17 |
| CHEMBL4436930 | — | — | 1 | 9.16 |
| CHEMBL4448944 | — | — | 1 | 9.14 |
| CHEMBL4545504 | — | — | 1 | 9.04 |
| CHEMBL4483083 | — | — | 1 | 9.00 |
| CHEMBL4590868 | — | — | 1 | 8.96 |
| CHEMBL4463636 | — | — | 1 | 8.85 |
| CHEMBL4539799 | — | — | 1 | 8.80 |
| CHEMBL1201027 | GLYCOPYRRONIUM BROMIDE | 4.0 | 1 | 8.80 |
| CHEMBL1724 | MEPENZOLATE BROMIDE | 4.0 | 1 | 8.68 |
| CHEMBL4452706 | — | — | 1 | 8.68 |
| CHEMBL4540604 | — | — | 1 | 8.64 |
| CHEMBL4521993 | — | — | 1 | 8.59 |
| CHEMBL4436947 | — | — | 1 | 8.15 |
| CHEMBL4470924 | — | — | 1 | 8.04 |
| CHEMBL4576060 | — | — | 1 | 7.92 |
| CHEMBL4474694 | — | — | 1 | 7.92 |
| CHEMBL4567385 | — | — | 1 | 7.92 |
| CHEMBL4591883 | — | — | 1 | 7.68 |
| CHEMBL4514058 | — | — | 1 | 7.17 |
| CHEMBL4442329 | — | — | 1 | - |
| CHEMBL4441041 | — | — | 1 | - |
| CHEMBL4541647 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4519930 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL4516342 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL4457734 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL551466 | ACLIDINIUM BROMIDE | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL4440620 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL4450188 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL4461243 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL4436930 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL4448944 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL4545504 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL4483083 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4590868 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4463636 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL4539799 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1201027 | GLYCOPYRRONIUM BROMIDE | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1724 | MEPENZOLATE BROMIDE | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4452706 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4540604 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL4521993 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL4436947 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL4470924 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL4576060 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4474694 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4567385 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4591883 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4514058 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL4442329 | — | Ki | - | — | - | |
| CHEMBL4441041 | — | Ki | - | — | - | |
| CHEMBL4541647 | — | Ki | - | — | - |