Assay Detail
Binding
CHEMBL4390203
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NMS from human M3R 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 | 8.51 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4440620 | — | — | 1 | 9.70 |
| CHEMBL4483083 | — | — | 1 | 9.40 |
| CHEMBL4448944 | — | — | 1 | 9.36 |
| CHEMBL4519930 | — | — | 1 | 9.29 |
| CHEMBL551466 | ACLIDINIUM BROMIDE | 4.0 | 1 | 9.25 |
| CHEMBL4457734 | — | — | 1 | 9.19 |
| CHEMBL1201027 | GLYCOPYRRONIUM BROMIDE | 4.0 | 1 | 9.09 |
| CHEMBL4590868 | — | — | 1 | 9.07 |
| CHEMBL4540604 | — | — | 1 | 9.07 |
| CHEMBL4461243 | — | — | 1 | 9.06 |
| CHEMBL4436930 | — | — | 1 | 8.96 |
| CHEMBL4521993 | — | — | 1 | 8.82 |
| CHEMBL4450188 | — | — | 1 | 8.77 |
| CHEMBL4463636 | — | — | 1 | 8.72 |
| CHEMBL4516342 | — | — | 1 | 8.64 |
| CHEMBL4539799 | — | — | 1 | 8.59 |
| CHEMBL4442329 | — | — | 1 | 8.55 |
| CHEMBL4541647 | — | — | 1 | 8.42 |
| CHEMBL4474694 | — | — | 1 | 8.33 |
| CHEMBL1724 | MEPENZOLATE BROMIDE | 4.0 | 1 | 8.28 |
| CHEMBL4452706 | — | — | 1 | 8.19 |
| CHEMBL4545504 | — | — | 1 | 8.11 |
| CHEMBL4436947 | — | — | 1 | 7.77 |
| CHEMBL4441041 | — | — | 1 | 7.72 |
| CHEMBL4470924 | — | — | 1 | 7.70 |
| CHEMBL4576060 | — | — | 1 | 7.39 |
| CHEMBL4567385 | — | — | 1 | 7.38 |
| CHEMBL4591883 | — | — | 1 | 7.09 |
| CHEMBL4514058 | — | — | 1 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4440620 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4483083 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4448944 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL4519930 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL551466 | ACLIDINIUM BROMIDE | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL4457734 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL1201027 | GLYCOPYRRONIUM BROMIDE | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL4590868 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL4540604 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL4461243 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL4436930 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4521993 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL4450188 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL4463636 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL4516342 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL4539799 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL4442329 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL4541647 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL4474694 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL1724 | MEPENZOLATE BROMIDE | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL4452706 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4545504 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL4436947 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4441041 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4470924 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4576060 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL4567385 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4591883 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL4514058 | — | Ki | = | 184.0 | nM | 6.74 |