Assay Detail
Binding
CHEMBL747850
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Binding affinity was determined against Muscarinic acetylcholine receptor using [3H]QNB as radioligand in rat brain.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.73 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL73538 | — | — | 1 | 7.41 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.29 |
| CHEMBL415300 | ISOCLOZAPINE | — | 1 | 7.26 |
| CHEMBL91310 | — | — | 1 | 6.82 |
| CHEMBL355107 | — | — | 1 | 6.61 |
| CHEMBL73082 | — | — | 1 | 6.53 |
| CHEMBL72162 | — | — | 1 | 6.48 |
| CHEMBL88870 | — | — | 1 | 6.38 |
| CHEMBL328246 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL73538 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL415300 | ISOCLOZAPINE | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL91310 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL355107 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL73082 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL72162 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL88870 | — | IC50 | = | 415.0 | nM | 6.38 |
| CHEMBL328246 | — | IC50 | = | 1750.0 | nM | 5.76 |