Assay Detail
Binding
CHEMBL617265
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Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 9.05 | 9.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL35085 | — | — | 1 | 9.81 |
| CHEMBL284847 | — | — | 1 | 9.57 |
| CHEMBL35743 | — | — | 1 | 9.52 |
| CHEMBL37633 | — | — | 1 | 9.48 |
| CHEMBL35040 | — | — | 1 | 9.45 |
| CHEMBL708 | ZIPRASIDONE | 4.0 | 1 | 9.38 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 9.27 |
| CHEMBL35057 | TIOSPIRONE | 2.0 | 1 | 9.24 |
| CHEMBL35565 | — | — | 1 | 8.84 |
| CHEMBL287605 | — | — | 1 | 8.84 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.82 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL35085 | — | Ki | = | 0.1549 | nM | 9.81 |
| CHEMBL284847 | — | Ki | = | 0.2692 | nM | 9.57 |
| CHEMBL35743 | — | Ki | = | 0.302 | nM | 9.52 |
| CHEMBL37633 | — | Ki | = | 0.3311 | nM | 9.48 |
| CHEMBL35040 | — | Ki | = | 0.3548 | nM | 9.45 |
| CHEMBL708 | ZIPRASIDONE | Ki | = | 0.4169 | nM | 9.38 |
| CHEMBL85 | RISPERIDONE | Ki | = | 0.537 | nM | 9.27 |
| CHEMBL35057 | TIOSPIRONE | Ki | = | 0.5754 | nM | 9.24 |
| CHEMBL35565 | — | Ki | = | 1.445 | nM | 8.84 |
| CHEMBL287605 | — | Ki | = | 1.445 | nM | 8.84 |
| CHEMBL42 | CLOZAPINE | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 44.67 | nM | 7.35 |