Assay Detail
Binding
CHEMBL4815613
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-NMS from human muscarinic M5 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M5 (CHEMBL2035) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dibenzodiazepinone-type muscarinic receptor antagonists conjugated to basic peptides: Impact of the linker moiety and unnatural amino acids on M<sub>2</sub>R selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 5.96 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448933 | — | — | 1 | 7.14 |
| CHEMBL4596899 | — | — | 1 | 6.90 |
| CHEMBL4059733 | — | — | 1 | 6.80 |
| CHEMBL4876453 | — | — | 1 | 6.65 |
| CHEMBL4596065 | — | — | 1 | 6.50 |
| CHEMBL4597498 | — | — | 1 | 6.40 |
| CHEMBL4862996 | — | — | 1 | 6.28 |
| CHEMBL4854886 | — | — | 1 | 6.22 |
| CHEMBL4852868 | — | — | 1 | 6.21 |
| CHEMBL4850130 | — | — | 1 | 6.17 |
| CHEMBL4856659 | — | — | 1 | 6.06 |
| CHEMBL4872608 | — | — | 1 | 5.95 |
| CHEMBL4870729 | — | — | 1 | 5.58 |
| CHEMBL4854179 | — | — | 1 | 5.32 |
| CHEMBL4865939 | — | — | 1 | 5.31 |
| CHEMBL4869723 | — | — | 1 | 5.29 |
| CHEMBL4862098 | — | — | 1 | 5.24 |
| CHEMBL4850553 | — | — | 1 | 5.10 |
| CHEMBL4862221 | — | — | 1 | 5.06 |
| CHEMBL4871563 | — | — | 1 | 5.04 |
| CHEMBL4865137 | — | — | 1 | - |
| CHEMBL4847458 | — | — | 1 | - |
| CHEMBL4863723 | — | — | 1 | - |
| CHEMBL4852079 | — | — | 1 | - |
| CHEMBL4858774 | — | — | 1 | - |
| CHEMBL4872632 | — | — | 1 | - |
| CHEMBL4875268 | — | — | 1 | - |
| CHEMBL4877107 | — | — | 1 | - |
| CHEMBL4856090 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448933 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL4596899 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL4059733 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL4876453 | — | Ki | = | 223.87 | nM | 6.65 |
| CHEMBL4596065 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL4597498 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL4862996 | — | Ki | = | 524.81 | nM | 6.28 |
| CHEMBL4854886 | — | Ki | = | 602.56 | nM | 6.22 |
| CHEMBL4852868 | — | Ki | = | 616.6 | nM | 6.21 |
| CHEMBL4850130 | — | Ki | = | 676.08 | nM | 6.17 |
| CHEMBL4856659 | — | Ki | = | 870.96 | nM | 6.06 |
| CHEMBL4872608 | — | Ki | = | 1122.02 | nM | 5.95 |
| CHEMBL4870729 | — | Ki | = | 2630.27 | nM | 5.58 |
| CHEMBL4854179 | — | Ki | = | 4786.3 | nM | 5.32 |
| CHEMBL4865939 | — | Ki | = | 4897.79 | nM | 5.31 |
| CHEMBL4869723 | — | Ki | = | 5128.61 | nM | 5.29 |
| CHEMBL4862098 | — | Ki | = | 5754.4 | nM | 5.24 |
| CHEMBL4850553 | — | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL4862221 | — | Ki | = | 8709.64 | nM | 5.06 |
| CHEMBL4871563 | — | Ki | = | 9120.11 | nM | 5.04 |
| CHEMBL4865137 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4847458 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4863723 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4852079 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4858774 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4872632 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4875268 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4877107 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4856090 | — | Ki | > | 10000.0 | nM | - |