Assay Detail
Functional
CHEMBL1913617
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 9.27 | 10.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1910848 | — | — | 1 | 10.31 |
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 10.29 |
| CHEMBL1910852 | — | — | 1 | 9.80 |
| CHEMBL1910857 | — | — | 1 | 9.74 |
| CHEMBL1908368 | — | — | 1 | 9.72 |
| CHEMBL1910856 | PF-03635659 | 2.0 | 1 | 9.70 |
| CHEMBL1910851 | — | — | 1 | 9.68 |
| CHEMBL1910862 | — | — | 1 | 9.66 |
| CHEMBL1910846 | — | — | 1 | 9.60 |
| CHEMBL1910865 | — | — | 1 | 9.59 |
| CHEMBL1910849 | — | — | 1 | 9.57 |
| CHEMBL1910850 | — | — | 1 | 9.29 |
| CHEMBL1910860 | — | — | 1 | 9.25 |
| CHEMBL1910863 | — | — | 1 | 9.22 |
| CHEMBL1910866 | — | — | 1 | 9.15 |
| CHEMBL1910858 | — | — | 1 | 9.14 |
| CHEMBL1910853 | — | — | 1 | 9.12 |
| CHEMBL1910847 | — | — | 1 | 8.80 |
| CHEMBL1910861 | — | — | 1 | 8.72 |
| CHEMBL1910859 | — | — | 1 | 8.70 |
| CHEMBL1910854 | — | — | 1 | 8.64 |
| CHEMBL1910845 | — | — | 1 | 8.62 |
| CHEMBL1910864 | — | — | 1 | 8.14 |
| CHEMBL1910855 | — | — | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1910848 | — | Ki | = | 0.049 | nM | 10.31 |
| CHEMBL3545181 | TIOTROPIUM BROMIDE | Ki | = | 0.051 | nM | 10.29 |
| CHEMBL1910852 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL1910857 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL1908368 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL1910856 | PF-03635659 | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL1910851 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL1910862 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL1910846 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL1910865 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL1910849 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL1910850 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL1910860 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL1910863 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1910866 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL1910858 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL1910853 | — | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL1910847 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1910861 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL1910859 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1910854 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL1910845 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL1910864 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL1910855 | — | Ki | = | 11.0 | nM | 7.96 |