Assay Detail
Binding
CHEMBL1030598
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Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 6.71 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL908 | CHLORPROTHIXENE | 4.0 | 1 | 7.75 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 7.05 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.05 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 7.02 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 1 | 6.75 |
| CHEMBL517244 | — | — | 1 | 6.69 |
| CHEMBL455288 | — | — | 1 | 6.69 |
| CHEMBL459373 | — | — | 1 | 6.63 |
| CHEMBL517407 | — | — | 1 | 6.61 |
| CHEMBL459350 | — | — | 1 | 6.52 |
| CHEMBL21731 | MAPROTILINE | 4.0 | 1 | 6.40 |
| CHEMBL457957 | — | — | 1 | 6.06 |
| CHEMBL464811 | — | — | 1 | 6.06 |
| CHEMBL460402 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL908 | CHLORPROTHIXENE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL42 | CLOZAPINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL726 | FLUPHENAZINE | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL517244 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL455288 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL459373 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL517407 | — | Ki | = | 248.0 | nM | 6.61 |
| CHEMBL459350 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL21731 | MAPROTILINE | Ki | = | 402.0 | nM | 6.40 |
| CHEMBL457957 | — | Ki | = | 879.0 | nM | 6.06 |
| CHEMBL464811 | — | Ki | = | 866.0 | nM | 6.06 |
| CHEMBL460402 | — | Ki | > | 1000.0 | nM | - |