Assay Detail
Binding
CHEMBL748274
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Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M5 in transfected CHO cells.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M5 (CHEMBL2035) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 5.56 | 6.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL106219 | — | — | 1 | 6.32 |
| CHEMBL104332 | — | — | 1 | 6.30 |
| CHEMBL104804 | — | — | 1 | 5.95 |
| CHEMBL104574 | — | — | 1 | 5.95 |
| CHEMBL318995 | — | — | 1 | 5.83 |
| CHEMBL280220 | — | — | 1 | 5.77 |
| CHEMBL105122 | — | — | 1 | 5.71 |
| CHEMBL420662 | — | — | 1 | 5.65 |
| CHEMBL320465 | — | — | 1 | 5.65 |
| CHEMBL104693 | — | — | 1 | 5.62 |
| CHEMBL107679 | — | — | 1 | 5.60 |
| CHEMBL106505 | — | — | 1 | 5.60 |
| CHEMBL106218 | — | — | 1 | 5.51 |
| CHEMBL105148 | — | — | 1 | 5.51 |
| CHEMBL59898 | — | — | 1 | 5.47 |
| CHEMBL106224 | — | — | 1 | 5.47 |
| CHEMBL105945 | — | — | 1 | 5.44 |
| CHEMBL107444 | — | — | 1 | 5.43 |
| CHEMBL105593 | — | — | 1 | 5.32 |
| CHEMBL104210 | — | — | 1 | 5.27 |
| CHEMBL105674 | — | — | 1 | 5.27 |
| CHEMBL104803 | — | — | 1 | 5.21 |
| CHEMBL326450 | — | — | 1 | 4.95 |
| CHEMBL106259 | — | — | 1 | 4.71 |
| CHEMBL105160 | — | — | 1 | - |
| CHEMBL107680 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL106219 | — | Ki | = | 478.63 | nM | 6.32 |
| CHEMBL104332 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL104804 | — | Ki | = | 1122.02 | nM | 5.95 |
| CHEMBL104574 | — | Ki | = | 1122.02 | nM | 5.95 |
| CHEMBL318995 | — | Ki | = | 1479.11 | nM | 5.83 |
| CHEMBL280220 | — | Ki | = | 1698.24 | nM | 5.77 |
| CHEMBL105122 | — | Ki | = | 1949.84 | nM | 5.71 |
| CHEMBL420662 | — | Ki | = | 2238.72 | nM | 5.65 |
| CHEMBL320465 | — | Ki | = | 2238.72 | nM | 5.65 |
| CHEMBL104693 | — | Ki | = | 2398.83 | nM | 5.62 |
| CHEMBL107679 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL106505 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL106218 | — | Ki | = | 3090.3 | nM | 5.51 |
| CHEMBL105148 | — | Ki | = | 3090.3 | nM | 5.51 |
| CHEMBL59898 | — | Ki | = | 3388.44 | nM | 5.47 |
| CHEMBL106224 | — | Ki | = | 3388.44 | nM | 5.47 |
| CHEMBL105945 | — | Ki | = | 3630.78 | nM | 5.44 |
| CHEMBL107444 | — | Ki | = | 3715.35 | nM | 5.43 |
| CHEMBL105593 | — | Ki | = | 4786.3 | nM | 5.32 |
| CHEMBL104210 | — | Ki | = | 5370.32 | nM | 5.27 |
| CHEMBL105674 | — | Ki | = | 5370.32 | nM | 5.27 |
| CHEMBL104803 | — | Ki | = | 6165.95 | nM | 5.21 |
| CHEMBL326450 | — | Ki | = | 11220.18 | nM | 4.95 |
| CHEMBL106259 | — | Ki | = | 19498.45 | nM | 4.71 |
| CHEMBL105160 | — | Ki | > | 28183.83 | nM | - |
| CHEMBL107680 | — | Ki | > | 28183.83 | nM | - |