Assay Detail
Binding
CHEMBL645242
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In vitro affinity for cortical alpha-1 adrenergic receptor labelled with [3H]WB-4101
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.73 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1203220 | — | — | 1 | 9.05 |
| CHEMBL332241 | — | — | 1 | 9.00 |
| CHEMBL123338 | — | — | 1 | 8.70 |
| CHEMBL331227 | — | — | 1 | 8.70 |
| CHEMBL123133 | — | — | 1 | 8.52 |
| CHEMBL332147 | — | — | 1 | 8.40 |
| CHEMBL420164 | — | — | 1 | 8.30 |
| CHEMBL121774 | — | — | 1 | 8.30 |
| CHEMBL123653 | — | — | 1 | 8.15 |
| CHEMBL124291 | — | — | 1 | 8.10 |
| CHEMBL1203224 | — | — | 1 | 8.05 |
| CHEMBL1203226 | — | — | 1 | 8.05 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 7.51 |
| CHEMBL124047 | — | — | 1 | 7.48 |
| CHEMBL124119 | — | — | 1 | 7.48 |
| CHEMBL333257 | — | — | 1 | 7.34 |
| CHEMBL1204189 | TIOSPIRONE HYDROCHLORIDE | -1.0 | 1 | 7.33 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.21 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 1 | 7.19 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.89 |
| CHEMBL1203222 | — | — | 1 | 6.78 |
| CHEMBL422 | TRIFLUOPERAZINE | 4.0 | 1 | 6.46 |
| CHEMBL122100 | — | — | 1 | 6.34 |
| CHEMBL1204336 | — | — | 1 | 6.29 |
| CHEMBL1203223 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1203220 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL332241 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL123338 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL331227 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL123133 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL332147 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL420164 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL121774 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL123653 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL124291 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1203224 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1203226 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL124047 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL124119 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL333257 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL1204189 | TIOSPIRONE HYDROCHLORIDE | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1203222 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL422 | TRIFLUOPERAZINE | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL122100 | — | IC50 | = | 454.0 | nM | 6.34 |
| CHEMBL1204336 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1203223 | — | IC50 | > | 1000.0 | nM | - |