Assay Detail
Binding
CHEMBL645101
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 11 | 7.27 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL424967 | — | — | 1 | 7.89 |
| CHEMBL368578 | — | — | 1 | 7.72 |
| CHEMBL415761 | — | — | 1 | 7.70 |
| CHEMBL175154 | — | — | 1 | 7.54 |
| CHEMBL178376 | — | — | 1 | 7.52 |
| CHEMBL368475 | — | — | 1 | 7.44 |
| CHEMBL175508 | — | — | 1 | 7.36 |
| CHEMBL368357 | — | — | 1 | 7.10 |
| CHEMBL368413 | — | — | 1 | 6.89 |
| CHEMBL176365 | — | — | 1 | 6.85 |
| CHEMBL174649 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL424967 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL368578 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL415761 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL175154 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL178376 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL368475 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL175508 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL368357 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL368413 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL176365 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL174649 | — | Ki | = | 1200.0 | nM | 5.92 |