Assay Detail
Binding
CHEMBL1030600
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Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.24 | 8.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL726 | FLUPHENAZINE | 4.0 | 1 | 8.84 |
| CHEMBL908 | CHLORPROTHIXENE | 4.0 | 1 | 8.53 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 8.39 |
| CHEMBL459373 | — | — | 1 | 7.39 |
| CHEMBL455288 | — | — | 1 | 7.33 |
| CHEMBL517407 | — | — | 1 | 7.28 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.08 |
| CHEMBL459350 | — | — | 1 | 7.00 |
| CHEMBL517244 | — | — | 1 | 6.84 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 6.71 |
| CHEMBL464811 | — | — | 1 | 6.54 |
| CHEMBL21731 | MAPROTILINE | 4.0 | 1 | 6.18 |
| CHEMBL457957 | — | — | 1 | 6.04 |
| CHEMBL460402 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL726 | FLUPHENAZINE | Ki | = | 1.44 | nM | 8.84 |
| CHEMBL908 | CHLORPROTHIXENE | Ki | = | 2.96 | nM | 8.53 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 4.06 | nM | 8.39 |
| CHEMBL459373 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL455288 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL517407 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL42 | CLOZAPINE | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL459350 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL517244 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 196.0 | nM | 6.71 |
| CHEMBL464811 | — | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL21731 | MAPROTILINE | Ki | = | 665.0 | nM | 6.18 |
| CHEMBL457957 | — | Ki | = | 904.0 | nM | 6.04 |
| CHEMBL460402 | — | Ki | > | 1000.0 | nM | - |