Assay Detail
Binding
CHEMBL1030597
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Displacement of [3H]pyrilamine from human histamine H1 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 | 7.42 | 8.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 8.95 |
| CHEMBL21731 | MAPROTILINE | 4.0 | 1 | 8.78 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.62 |
| CHEMBL908 | CHLORPROTHIXENE | 4.0 | 1 | 8.43 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 8.37 |
| CHEMBL517244 | — | — | 1 | 7.40 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 1 | 7.40 |
| CHEMBL459350 | — | — | 1 | 7.10 |
| CHEMBL464811 | — | — | 1 | 6.72 |
| CHEMBL459373 | — | — | 1 | 6.69 |
| CHEMBL517407 | — | — | 1 | 6.53 |
| CHEMBL455288 | — | — | 1 | 6.41 |
| CHEMBL457957 | — | — | 1 | 6.25 |
| CHEMBL460402 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 1.12 | nM | 8.95 |
| CHEMBL21731 | MAPROTILINE | Ki | = | 1.67 | nM | 8.78 |
| CHEMBL42 | CLOZAPINE | Ki | = | 2.38 | nM | 8.62 |
| CHEMBL908 | CHLORPROTHIXENE | Ki | = | 3.75 | nM | 8.43 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 4.25 | nM | 8.37 |
| CHEMBL517244 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL726 | FLUPHENAZINE | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL459350 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL464811 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL459373 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL517407 | — | Ki | = | 295.0 | nM | 6.53 |
| CHEMBL455288 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL457957 | — | Ki | = | 559.0 | nM | 6.25 |
| CHEMBL460402 | — | Ki | = | 686.0 | nM | 6.16 |