Assay Detail
Functional
CHEMBL1015373
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
22
Total Activities
22
Compounds Tested
1
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 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 22 | 9.56 | 10.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489212 | — | — | 1 | 10.60 |
| CHEMBL523299 | UMECLIDINIUM BROMIDE | 4.0 | 1 | 10.50 |
| CHEMBL490237 | — | — | 1 | 10.40 |
| CHEMBL523957 | — | — | 1 | 10.40 |
| CHEMBL489211 | — | — | 1 | 10.40 |
| CHEMBL522081 | — | — | 1 | 10.20 |
| CHEMBL523474 | — | — | 1 | 10.20 |
| CHEMBL521781 | — | — | 1 | 10.10 |
| CHEMBL476434 | — | — | 1 | 10.00 |
| CHEMBL524119 | — | — | 1 | 9.90 |
| CHEMBL489625 | — | — | 1 | 9.60 |
| CHEMBL489032 | — | — | 1 | 9.40 |
| CHEMBL523598 | — | — | 1 | 9.40 |
| CHEMBL490243 | — | — | 1 | 9.40 |
| CHEMBL484475 | — | — | 1 | 9.30 |
| CHEMBL490244 | — | — | 1 | 9.30 |
| CHEMBL522418 | — | — | 1 | 9.10 |
| CHEMBL519652 | — | — | 1 | 8.70 |
| CHEMBL490236 | — | — | 1 | 8.50 |
| CHEMBL490242 | — | — | 1 | 8.50 |
| CHEMBL491246 | — | — | 1 | 8.40 |
| CHEMBL490651 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489212 | — | Kd | = | 0.02512 | nM | 10.60 |
| CHEMBL523299 | UMECLIDINIUM BROMIDE | Kd | = | 0.03162 | nM | 10.50 |
| CHEMBL490237 | — | Kd | = | 0.03981 | nM | 10.40 |
| CHEMBL523957 | — | Kd | = | 0.03981 | nM | 10.40 |
| CHEMBL489211 | — | Kd | = | 0.03981 | nM | 10.40 |
| CHEMBL522081 | — | Kd | = | 0.0631 | nM | 10.20 |
| CHEMBL523474 | — | Kd | = | 0.0631 | nM | 10.20 |
| CHEMBL521781 | — | Kd | = | 0.07943 | nM | 10.10 |
| CHEMBL476434 | — | Kd | = | 0.1 | nM | 10.00 |
| CHEMBL524119 | — | Kd | = | 0.1259 | nM | 9.90 |
| CHEMBL489625 | — | Kd | = | 0.2512 | nM | 9.60 |
| CHEMBL489032 | — | Kd | = | 0.3981 | nM | 9.40 |
| CHEMBL523598 | — | Kd | = | 0.3981 | nM | 9.40 |
| CHEMBL490243 | — | Kd | = | 0.3981 | nM | 9.40 |
| CHEMBL484475 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL490244 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL522418 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL519652 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL490236 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL490242 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL491246 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL490651 | — | Kd | = | 10.0 | nM | 8.00 |