Assay Detail
Binding
CHEMBL748440
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In vitro binding affinity against Muscarinic acetylcholine receptors in rat brain.
20
Total Activities
20
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
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.64 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL67284 | ISOCLOTHIAPINE | — | 1 | 8.25 |
| CHEMBL415300 | ISOCLOZAPINE | — | 1 | 7.68 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.60 |
| CHEMBL63756 | FLUPERLAPINE | 2.0 | 1 | 7.60 |
| CHEMBL63329 | — | — | 1 | 7.32 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 7.22 |
| CHEMBL63576 | — | — | 1 | 7.19 |
| CHEMBL304902 | CLOTHIAPINE | 2.0 | 1 | 6.87 |
| CHEMBL63390 | — | — | 1 | 6.76 |
| CHEMBL67355 | — | — | 1 | 6.52 |
| CHEMBL303435 | — | — | 1 | 6.51 |
| CHEMBL304493 | — | — | 1 | 6.44 |
| CHEMBL63347 | — | — | 1 | 6.38 |
| CHEMBL66730 | — | — | 1 | 6.37 |
| CHEMBL63590 | — | — | 1 | 6.28 |
| CHEMBL303173 | — | — | 1 | 6.18 |
| CHEMBL67298 | — | — | 1 | 5.49 |
| CHEMBL292738 | — | — | 1 | 5.47 |
| CHEMBL65768 | — | — | 1 | 5.46 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL67284 | ISOCLOTHIAPINE | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL415300 | ISOCLOZAPINE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL42 | CLOZAPINE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL63756 | FLUPERLAPINE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL63329 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 60.7 | nM | 7.22 |
| CHEMBL63576 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL304902 | CLOTHIAPINE | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL63390 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL67355 | — | Ki | = | 303.0 | nM | 6.52 |
| CHEMBL303435 | — | Ki | = | 311.0 | nM | 6.51 |
| CHEMBL304493 | — | Ki | = | 366.0 | nM | 6.44 |
| CHEMBL63347 | — | Ki | = | 415.0 | nM | 6.38 |
| CHEMBL66730 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL63590 | — | Ki | = | 523.0 | nM | 6.28 |
| CHEMBL303173 | — | Ki | = | 665.0 | nM | 6.18 |
| CHEMBL67298 | — | Ki | = | 3260.0 | nM | 5.49 |
| CHEMBL292738 | — | Ki | = | 3415.0 | nM | 5.47 |
| CHEMBL65768 | — | Ki | = | 3450.0 | nM | 5.46 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 7466.0 | nM | 5.13 |