Assay Detail
Binding
CHEMBL647134
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Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Frontal cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.77 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL304438 | — | — | 1 | 9.30 |
| CHEMBL60885 | — | — | 1 | 9.22 |
| CHEMBL64878 | — | — | 1 | 9.09 |
| CHEMBL292935 | — | — | 1 | 9.00 |
| CHEMBL294730 | — | — | 1 | 8.22 |
| CHEMBL293923 | — | — | 1 | 8.00 |
| CHEMBL59823 | — | — | 1 | 7.70 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.70 |
| CHEMBL64610 | — | — | 1 | 7.52 |
| CHEMBL60318 | — | — | 1 | 7.52 |
| CHEMBL61819 | — | — | 1 | 7.52 |
| CHEMBL64845 | — | — | 1 | 7.35 |
| CHEMBL60047 | — | — | 1 | 7.07 |
| CHEMBL59741 | — | — | 1 | 7.05 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.80 |
| CHEMBL61818 | — | — | 1 | 6.70 |
| CHEMBL418499 | — | — | 1 | 6.40 |
| CHEMBL64167 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL304438 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL60885 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL64878 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL292935 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL294730 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL293923 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL59823 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL64610 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL60318 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL61819 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL64845 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL60047 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL59741 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL61818 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL418499 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL64167 | — | IC50 | > | 100.0 | nM | - |