Assay Detail
Binding
CHEMBL1291431
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
36
Total Activities
36
Compounds Tested
2
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 | Autocuration |
Publication
The discovery of new spirocyclic muscarinic M3 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.73 | 10.50 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 10.50 |
| CHEMBL551466 | ACLIDINIUM BROMIDE | 4.0 | 1 | 9.90 |
| CHEMBL1201027 | GLYCOPYRRONIUM BROMIDE | 4.0 | 1 | 9.30 |
| CHEMBL1289653 | — | — | 1 | 8.90 |
| CHEMBL1290184 | — | — | 1 | 8.60 |
| CHEMBL1289545 | — | — | 1 | 8.50 |
| CHEMBL1289654 | — | — | 1 | 8.50 |
| CHEMBL1290183 | — | — | 1 | 8.40 |
| CHEMBL1290294 | — | — | 1 | 8.20 |
| CHEMBL1289983 | — | — | 1 | 8.00 |
| CHEMBL1289758 | — | — | 1 | 7.90 |
| CHEMBL1289866 | — | — | 1 | 7.80 |
| CHEMBL1290410 | — | — | 1 | 7.80 |
| CHEMBL1289082 | — | — | 1 | 7.70 |
| CHEMBL1289982 | — | — | 1 | 7.60 |
| CHEMBL1289081 | — | — | 1 | 7.60 |
| CHEMBL1289865 | — | — | 1 | 7.50 |
| CHEMBL1290752 | — | — | 1 | 7.50 |
| CHEMBL1289314 | — | — | 1 | 7.40 |
| CHEMBL1290753 | — | — | 1 | 7.30 |
| CHEMBL1289544 | — | — | 1 | 7.30 |
| CHEMBL1289202 | — | — | 1 | 7.20 |
| CHEMBL1289432 | — | — | 1 | 7.10 |
| CHEMBL1290634 | — | — | 1 | 7.10 |
| CHEMBL1290409 | — | — | 1 | 7.10 |
| CHEMBL1290295 | — | — | 1 | 7.10 |
| CHEMBL1289315 | — | — | 1 | 6.90 |
| CHEMBL1289201 | — | — | 1 | 6.90 |
| CHEMBL1290635 | — | — | 1 | 6.90 |
| CHEMBL1290520 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | IC50 | = | 0.03162 | nM | 10.50 |
| CHEMBL551466 | ACLIDINIUM BROMIDE | IC50 | = | 0.1259 | nM | 9.90 |
| CHEMBL1201027 | GLYCOPYRRONIUM BROMIDE | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL1289653 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL1290184 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL1289545 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL1289654 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL1290183 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL1290294 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL1289983 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1289758 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL1289866 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL1290410 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL1289082 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL1289081 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL1289982 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL1289865 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1290752 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1289314 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL1289544 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL1290753 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL1289202 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL1289432 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL1290634 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL1290409 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL1290295 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL1289201 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL1290635 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL1289315 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL1290520 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL1290519 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL1290077 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL1289433 | — | pIC50 | - | — | - | |
| CHEMBL1289759 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1290078 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1290185 | — | IC50 | > | 1000.0 | nM | - |