Assay Detail
Binding
CHEMBL744323
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Inhibitory binding of [3H]pirenzepine to human Muscarinic acetylcholine receptor M1 in membranes from CHO-K1 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.22 | 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 |
| CHEMBL72794 | — | — | 1 | 7.41 |
| CHEMBL72292 | — | — | 1 | 5.92 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 5.26 |
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 |
| CHEMBL72794 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL72292 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 5500.0 | nM | 5.26 |