Assay Detail
Binding
CHEMBL1030601
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Displacement of [3H]spiperone from human dopamine D3 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 | 7.19 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL726 | FLUPHENAZINE | 4.0 | 1 | 8.49 |
| CHEMBL908 | CHLORPROTHIXENE | 4.0 | 1 | 8.34 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 8.16 |
| CHEMBL455288 | — | — | 1 | 7.82 |
| CHEMBL459373 | — | — | 1 | 7.30 |
| CHEMBL517407 | — | — | 1 | 7.30 |
| CHEMBL459350 | — | — | 1 | 7.17 |
| CHEMBL517244 | — | — | 1 | 6.83 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 6.69 |
| CHEMBL464811 | — | — | 1 | 6.65 |
| CHEMBL460402 | — | — | 1 | 6.61 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.53 |
| CHEMBL457957 | — | — | 1 | 6.49 |
| CHEMBL21731 | MAPROTILINE | 4.0 | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL726 | FLUPHENAZINE | Ki | = | 3.21 | nM | 8.49 |
| CHEMBL908 | CHLORPROTHIXENE | Ki | = | 4.56 | nM | 8.34 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL455288 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL459373 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL517407 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL459350 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL517244 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL464811 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL460402 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL42 | CLOZAPINE | Ki | = | 295.0 | nM | 6.53 |
| CHEMBL457957 | — | Ki | = | 326.0 | nM | 6.49 |
| CHEMBL21731 | MAPROTILINE | Ki | = | 504.0 | nM | 6.30 |