Assay Detail
Binding
CHEMBL749896
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Displacement of [3H]- QNB binding at the muscarinic-cholinergic binding site of rat brain S1
15
Total Activities
15
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
Synthesis and receptor binding studies relevant to the neuroleptic activities of some 1-methyl-4-piperidylidene-9-substituted-pyrrolo[2,1-b][3]benzazepine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.86 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 1 | 8.40 |
| CHEMBL175154 | — | — | 1 | 7.84 |
| CHEMBL368578 | — | — | 1 | 7.75 |
| CHEMBL415761 | — | — | 1 | 7.70 |
| CHEMBL178376 | — | — | 1 | 7.68 |
| CHEMBL368357 | — | — | 1 | 7.32 |
| CHEMBL368413 | — | — | 1 | 7.31 |
| CHEMBL175508 | — | — | 1 | 7.22 |
| CHEMBL424967 | — | — | 1 | 7.06 |
| CHEMBL368475 | — | — | 1 | 6.60 |
| CHEMBL176365 | — | — | 1 | 6.57 |
| CHEMBL1255588 | — | — | 1 | 5.28 |
| CHEMBL174649 | — | — | 1 | 5.01 |
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 4.30 |
| CHEMBL442783 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL516 | CYPROHEPTADINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL175154 | — | Ki | = | 14.5 | nM | 7.84 |
| CHEMBL368578 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL415761 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL178376 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL368357 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL368413 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL175508 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL424967 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL368475 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL176365 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL1255588 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL174649 | — | Ki | = | 9800.0 | nM | 5.01 |
| CHEMBL267930 | SPIPERONE | Ki | = | 49600.0 | nM | 4.30 |
| CHEMBL442783 | — | Ki | > | 50000.0 | nM | - |