Assay Detail
Binding
CHEMBL617536
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Binding affinity at rat 5-hydroxytryptamine 2 receptor by [3H]ketanserin displacement.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Serotonin 2 (5-HT2) receptor (CHEMBL2093870) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.62 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | 2.0 | 1 | 7.40 |
| CHEMBL9467 | — | — | 1 | 6.91 |
| CHEMBL276156 | — | — | 1 | 6.72 |
| CHEMBL9921 | — | — | 1 | 6.69 |
| CHEMBL9669 | — | — | 1 | 6.63 |
| CHEMBL9870 | — | — | 1 | 6.63 |
| CHEMBL9452 | — | — | 1 | 6.56 |
| CHEMBL267153 | — | — | 1 | 6.38 |
| CHEMBL9434 | PHENYLPIPERAZINE | — | 1 | 6.17 |
| CHEMBL273923 | — | — | 1 | 6.11 |
| CHEMBL9841 | — | — | 1 | - |
| CHEMBL9429 | — | — | 1 | - |
| CHEMBL275943 | — | — | 1 | - |
| CHEMBL269784 | — | — | 1 | - |
| CHEMBL9666 | — | — | 1 | - |
| CHEMBL269521 | MK-212 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL9467 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL276156 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL9921 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL9669 | — | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL9870 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL9452 | — | Ki | = | 277.0 | nM | 6.56 |
| CHEMBL267153 | — | Ki | = | 419.0 | nM | 6.38 |
| CHEMBL9434 | PHENYLPIPERAZINE | Ki | = | 668.0 | nM | 6.17 |
| CHEMBL273923 | — | Ki | = | 774.0 | nM | 6.11 |
| CHEMBL9841 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL9429 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL275943 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL269784 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL9666 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL269521 | MK-212 | Ki | > | 1000.0 | nM | - |