Assay Detail
Binding
CHEMBL746567
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Tested in vitro for its ability to displace 3[H] clozapine from Muscarinic acetylcholine receptor in rat brain
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.55 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.92 |
| CHEMBL415300 | ISOCLOZAPINE | — | 1 | 7.55 |
| CHEMBL73538 | — | — | 1 | 7.51 |
| CHEMBL7617 | — | — | 1 | 6.54 |
| CHEMBL7821 | — | — | 1 | 6.21 |
| CHEMBL275696 | — | — | 1 | 6.17 |
| CHEMBL88464 | — | — | 1 | 5.71 |
| CHEMBL90882 | — | — | 1 | 5.69 |
| CHEMBL89970 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL415300 | ISOCLOZAPINE | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL73538 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL7617 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL7821 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL275696 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL88464 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL90882 | — | IC50 | = | 2027.0 | nM | 5.69 |
| CHEMBL89970 | — | IC50 | = | 2290.0 | nM | 5.64 |