Assay Detail
Functional
CHEMBL995216
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Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.30 | 7.80 |
| pKb | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL526009 | — | — | 1 | 7.80 |
| CHEMBL505452 | — | — | 1 | 7.70 |
| CHEMBL502000 | — | — | 1 | 5.80 |
| CHEMBL505453 | — | — | 1 | 5.50 |
| CHEMBL501727 | — | — | 1 | 4.70 |
| CHEMBL540359 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL526009 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL505452 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL502000 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL505453 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL501727 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL540359 | — | pKb | = | 10.1 | — | - |