Assay Detail
Binding
CHEMBL617199
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Affinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserin
21
Total Activities
21
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 | 21 | 6.57 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.52 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.52 |
| CHEMBL59637 | — | — | 1 | 7.40 |
| CHEMBL64167 | — | — | 1 | 7.16 |
| CHEMBL64878 | — | — | 1 | 6.82 |
| CHEMBL60318 | — | — | 1 | 6.70 |
| CHEMBL59741 | — | — | 1 | 6.70 |
| CHEMBL292935 | — | — | 1 | 6.54 |
| CHEMBL60885 | — | — | 1 | 6.52 |
| CHEMBL61818 | — | — | 1 | 6.40 |
| CHEMBL293923 | — | — | 1 | 6.30 |
| CHEMBL61869 | — | — | 1 | 6.28 |
| CHEMBL64845 | — | — | 1 | 6.24 |
| CHEMBL418499 | — | — | 1 | 6.22 |
| CHEMBL304438 | — | — | 1 | 6.22 |
| CHEMBL64610 | — | — | 1 | 6.21 |
| CHEMBL60047 | — | — | 1 | 6.21 |
| CHEMBL59823 | — | — | 1 | 6.08 |
| CHEMBL294730 | — | — | 1 | 6.04 |
| CHEMBL61819 | — | — | 1 | 6.00 |
| CHEMBL60447 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL59637 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL64167 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL64878 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL60318 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL59741 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL292935 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL60885 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL61818 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL293923 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL61869 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL64845 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL418499 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL304438 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL64610 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL60047 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL59823 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL294730 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL61819 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL60447 | — | IC50 | = | 1100.0 | nM | 5.96 |