Assay Detail
Binding
CHEMBL748594
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Binding affinity against muscarinic (M) receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.44 | 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 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 7.22 |
| CHEMBL304902 | CLOTHIAPINE | 2.0 | 1 | 6.87 |
| CHEMBL151263 | — | — | 1 | 6.68 |
| CHEMBL435441 | — | — | 1 | 6.13 |
| CHEMBL149108 | — | — | 1 | 6.07 |
| CHEMBL149240 | — | — | 1 | 5.86 |
| CHEMBL433744 | — | — | 1 | 5.75 |
| CHEMBL147463 | — | — | 1 | 5.65 |
| CHEMBL356076 | — | — | 1 | 5.61 |
| CHEMBL146741 | — | — | 1 | 5.47 |
| CHEMBL151809 | — | — | 1 | 5.42 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL67284 | ISOCLOTHIAPINE | Ki | = | 5.623 | nM | 8.25 |
| CHEMBL415300 | ISOCLOZAPINE | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL42 | CLOZAPINE | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL63756 | FLUPERLAPINE | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 60.26 | nM | 7.22 |
| CHEMBL304902 | CLOTHIAPINE | Ki | = | 134.9 | nM | 6.87 |
| CHEMBL151263 | — | Ki | = | 208.93 | nM | 6.68 |
| CHEMBL435441 | — | Ki | = | 741.31 | nM | 6.13 |
| CHEMBL149108 | — | Ki | = | 851.14 | nM | 6.07 |
| CHEMBL149240 | — | Ki | = | 1380.38 | nM | 5.86 |
| CHEMBL433744 | — | Ki | = | 1778.28 | nM | 5.75 |
| CHEMBL147463 | — | Ki | = | 2238.72 | nM | 5.65 |
| CHEMBL356076 | — | Ki | = | 2454.71 | nM | 5.61 |
| CHEMBL146741 | — | Ki | = | 3388.44 | nM | 5.47 |
| CHEMBL151809 | — | Ki | = | 3801.89 | nM | 5.42 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 7413.1 | nM | 5.13 |