Assay Detail
Binding
CHEMBL617606
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In vitro binding affinity for serotonin 5-hydroxytryptamine 2A receptor of rat cerebral cortex using [3H]ketanserin as radioligand
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.45 | 7.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18786 | CINANSERIN | 2.0 | 1 | 7.83 |
| CHEMBL356993 | — | — | 1 | 7.60 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.39 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.90 |
| CHEMBL358316 | — | — | 1 | 6.88 |
| CHEMBL344084 | — | — | 1 | 6.85 |
| CHEMBL143744 | — | — | 1 | 6.77 |
| CHEMBL143372 | — | — | 1 | 6.59 |
| CHEMBL142147 | — | — | 1 | 6.56 |
| CHEMBL356068 | — | — | 1 | 6.50 |
| CHEMBL141077 | — | — | 1 | 6.30 |
| CHEMBL141824 | — | — | 1 | 6.14 |
| CHEMBL143218 | — | — | 1 | 6.11 |
| CHEMBL142825 | — | — | 1 | 5.82 |
| CHEMBL341743 | — | — | 1 | 5.72 |
| CHEMBL344796 | — | — | 1 | 5.70 |
| CHEMBL342119 | — | — | 1 | 5.67 |
| CHEMBL356116 | — | — | 1 | 5.66 |
| CHEMBL344202 | — | — | 1 | 5.63 |
| CHEMBL142309 | — | — | 1 | - |
| CHEMBL344995 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18786 | CINANSERIN | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL356993 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 40.7 | nM | 7.39 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL358316 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL344084 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL143744 | — | IC50 | = | 171.5 | nM | 6.77 |
| CHEMBL143372 | — | IC50 | = | 259.2 | nM | 6.59 |
| CHEMBL142147 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL356068 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL141077 | — | IC50 | = | 501.0 | nM | 6.30 |
| CHEMBL141824 | — | IC50 | = | 717.0 | nM | 6.14 |
| CHEMBL143218 | — | IC50 | = | 783.0 | nM | 6.11 |
| CHEMBL142825 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL341743 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL344796 | — | IC50 | = | 2016.0 | nM | 5.70 |
| CHEMBL342119 | — | IC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL356116 | — | IC50 | = | 2169.0 | nM | 5.66 |
| CHEMBL344202 | — | IC50 | = | 2341.0 | nM | 5.63 |
| CHEMBL142309 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL344995 | — | IC50 | > | 10000.0 | nM | - |