Assay Detail
Binding
CHEMBL1913621
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Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 | 6 | 9.76 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1910856 | PF-03635659 | 2.0 | 1 | 9.89 |
| CHEMBL1910865 | — | — | 1 | 9.79 |
| CHEMBL1910851 | — | — | 1 | 9.74 |
| CHEMBL1910850 | — | — | 1 | 9.70 |
| CHEMBL1908368 | — | — | 1 | 9.67 |
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1910856 | PF-03635659 | Ki | = | 0.128 | nM | 9.89 |
| CHEMBL1910865 | — | Ki | = | 0.163 | nM | 9.79 |
| CHEMBL1910851 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL1910850 | — | Ki | = | 0.201 | nM | 9.70 |
| CHEMBL1908368 | — | Ki | = | 0.213 | nM | 9.67 |
| CHEMBL3545181 | TIOTROPIUM BROMIDE | Ki | = | 0.0098 | nM | - |