Assay Detail
Binding
CHEMBL752969
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Binding affinity towards human muscarinic M2 receptor in CHO-KI cells using [3H]- QNB as radioligand
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-KI |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 6.75 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL354636 | — | — | 1 | 7.89 |
| CHEMBL353311 | — | — | 1 | 7.58 |
| CHEMBL355854 | — | — | 1 | 7.49 |
| CHEMBL277642 | HIMBACINE | — | 1 | 7.32 |
| CHEMBL352618 | — | — | 1 | 7.29 |
| CHEMBL172646 | — | — | 1 | 6.83 |
| CHEMBL352756 | — | — | 1 | 6.74 |
| CHEMBL170977 | — | — | 1 | 6.72 |
| CHEMBL426032 | — | — | 1 | 6.68 |
| CHEMBL352596 | — | — | 1 | 6.65 |
| CHEMBL366819 | — | — | 1 | 6.56 |
| CHEMBL172969 | — | — | 1 | 6.55 |
| CHEMBL355475 | — | — | 1 | 6.51 |
| CHEMBL170205 | — | — | 1 | 6.45 |
| CHEMBL354934 | — | — | 1 | 6.42 |
| CHEMBL366640 | — | — | 1 | 6.31 |
| CHEMBL171520 | — | — | 1 | 6.28 |
| CHEMBL355193 | — | — | 1 | 6.24 |
| CHEMBL170922 | — | — | 1 | 6.22 |
| CHEMBL172272 | — | — | 1 | 6.19 |
| CHEMBL445134 | — | — | 1 | - |
| CHEMBL173950 | — | — | 1 | - |
| CHEMBL423438 | — | — | 1 | - |
| CHEMBL368990 | — | — | 1 | - |
| CHEMBL173155 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL354636 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL353311 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL355854 | — | Ki | = | 32.2 | nM | 7.49 |
| CHEMBL277642 | HIMBACINE | Ki | = | 48.4 | nM | 7.32 |
| CHEMBL352618 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL172646 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL352756 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL170977 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL426032 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL352596 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL366819 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL172969 | — | Ki | = | 283.0 | nM | 6.55 |
| CHEMBL355475 | — | Ki | = | 312.0 | nM | 6.51 |
| CHEMBL170205 | — | Ki | = | 352.0 | nM | 6.45 |
| CHEMBL354934 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL366640 | — | Ki | = | 485.0 | nM | 6.31 |
| CHEMBL171520 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL355193 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL170922 | — | Ki | = | 595.0 | nM | 6.22 |
| CHEMBL172272 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL445134 | — | Ki | > | 280.0 | nM | - |
| CHEMBL173950 | — | Ki | > | 500.0 | nM | - |
| CHEMBL423438 | — | Ki | > | 500.0 | nM | - |
| CHEMBL368990 | — | Ki | > | 500.0 | nM | - |
| CHEMBL173155 | — | Ki | > | 42.0 | nM | - |