Assay Detail
Binding
CHEMBL749865
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Binding affinity against Muscarinic acetylcholine receptor M4
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.46 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL71124 | — | — | 1 | 10.15 |
| CHEMBL2114068 | — | — | 1 | 10.05 |
| CHEMBL2115128 | — | — | 1 | 9.49 |
| CHEMBL71147 | — | — | 1 | 9.48 |
| CHEMBL307810 | — | — | 1 | 8.66 |
| CHEMBL71531 | — | — | 1 | 8.04 |
| CHEMBL2114064 | — | — | 1 | 7.89 |
| CHEMBL2111540 | — | — | 1 | 7.83 |
| CHEMBL2115127 | — | — | 1 | 7.82 |
| CHEMBL2114067 | — | — | 1 | 7.75 |
| CHEMBL2114066 | — | — | 1 | 7.74 |
| CHEMBL71971 | — | — | 1 | 7.73 |
| CHEMBL2115126 | — | — | 1 | 7.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL71124 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL2114068 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL2115128 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL71147 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL307810 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL71531 | — | Ki | = | 9.05 | nM | 8.04 |
| CHEMBL2114064 | — | Ki | = | 12.74 | nM | 7.89 |
| CHEMBL2111540 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL2115127 | — | Ki | = | 15.2 | nM | 7.82 |
| CHEMBL2114067 | — | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL2114066 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL71971 | — | Ki | = | 18.6 | nM | 7.73 |
| CHEMBL2115126 | — | Ki | = | 45.05 | nM | 7.35 |