Assay Detail
Binding
CHEMBL744322
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Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.98 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415300 | ISOCLOZAPINE | — | 1 | 8.22 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.03 |
| CHEMBL73074 | — | — | 1 | 7.72 |
| CHEMBL70377 | — | — | 1 | 7.57 |
| CHEMBL310712 | — | — | 1 | 7.46 |
| CHEMBL308090 | — | — | 1 | 7.43 |
| CHEMBL70609 | — | — | 1 | 7.42 |
| CHEMBL72794 | — | — | 1 | 7.41 |
| CHEMBL70319 | — | — | 1 | 7.27 |
| CHEMBL73589 | — | — | 1 | 6.34 |
| CHEMBL430798 | — | — | 1 | 6.31 |
| CHEMBL307163 | — | — | 1 | 6.00 |
| CHEMBL831 | LOXAPINE | 4.0 | 1 | 5.26 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 5.26 |
| CHEMBL72292 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415300 | ISOCLOZAPINE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL73074 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL70377 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL310712 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL308090 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL70609 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL72794 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL70319 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL73589 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL430798 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL307163 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL831 | LOXAPINE | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL72292 | — | IC50 | > | 1000.0 | nM | - |