Assay Detail
Binding
CHEMBL746610
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Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 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 M4 (CHEMBL1821) ↗| 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 | 7.59 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL326450 | — | — | 1 | 9.00 |
| CHEMBL104693 | — | — | 1 | 9.00 |
| CHEMBL320465 | — | — | 1 | 8.70 |
| CHEMBL280220 | — | — | 1 | 8.70 |
| CHEMBL106224 | — | — | 1 | 8.70 |
| CHEMBL318995 | — | — | 1 | 8.52 |
| CHEMBL106218 | — | — | 1 | 8.52 |
| CHEMBL105148 | — | — | 1 | 8.40 |
| CHEMBL105122 | — | — | 1 | 8.15 |
| CHEMBL59898 | — | — | 1 | 8.15 |
| CHEMBL104210 | — | — | 1 | 7.96 |
| CHEMBL105160 | — | — | 1 | 7.85 |
| CHEMBL107444 | — | — | 1 | 7.82 |
| CHEMBL420662 | — | — | 1 | 7.82 |
| CHEMBL104803 | — | — | 1 | 7.21 |
| CHEMBL106505 | — | — | 1 | 7.17 |
| CHEMBL104574 | — | — | 1 | 7.14 |
| CHEMBL104332 | — | — | 1 | 7.14 |
| CHEMBL106219 | — | — | 1 | 7.01 |
| CHEMBL107679 | — | — | 1 | 6.96 |
| CHEMBL105945 | — | — | 1 | 6.72 |
| CHEMBL105674 | — | — | 1 | 6.44 |
| CHEMBL104804 | — | — | 1 | 5.87 |
| CHEMBL105593 | — | — | 1 | 5.71 |
| CHEMBL106259 | — | — | 1 | 5.01 |
| CHEMBL107680 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL326450 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL104693 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL320465 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL280220 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL106224 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL318995 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL106218 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL105148 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL105122 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL59898 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL104210 | — | Ki | = | 10.96 | nM | 7.96 |
| CHEMBL105160 | — | Ki | = | 14.13 | nM | 7.85 |
| CHEMBL107444 | — | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL420662 | — | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL104803 | — | Ki | = | 61.66 | nM | 7.21 |
| CHEMBL106505 | — | Ki | = | 67.61 | nM | 7.17 |
| CHEMBL104574 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL104332 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL106219 | — | Ki | = | 97.72 | nM | 7.01 |
| CHEMBL107679 | — | Ki | = | 109.65 | nM | 6.96 |
| CHEMBL105945 | — | Ki | = | 190.55 | nM | 6.72 |
| CHEMBL105674 | — | Ki | = | 363.08 | nM | 6.44 |
| CHEMBL104804 | — | Ki | = | 1348.96 | nM | 5.87 |
| CHEMBL105593 | — | Ki | = | 1949.84 | nM | 5.71 |
| CHEMBL106259 | — | Ki | = | 9772.37 | nM | 5.01 |
| CHEMBL107680 | — | Ki | > | 12302.69 | nM | - |