Assay Detail
Binding
CHEMBL1030596
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Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in CHO/HEK293 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 | 9.05 | 10.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL455288 | — | — | 1 | 10.38 |
| CHEMBL459350 | — | — | 1 | 9.60 |
| CHEMBL517244 | — | — | 1 | 9.45 |
| CHEMBL459373 | — | — | 1 | 8.92 |
| CHEMBL517407 | — | — | 1 | 8.81 |
| CHEMBL464811 | — | — | 1 | 8.48 |
| CHEMBL460402 | — | — | 1 | 8.46 |
| CHEMBL457957 | — | — | 1 | 8.31 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | - |
| CHEMBL21731 | MAPROTILINE | 4.0 | 1 | - |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | - |
| CHEMBL908 | CHLORPROTHIXENE | 4.0 | 1 | - |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | - |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL455288 | — | Ki | = | 0.042 | nM | 10.38 |
| CHEMBL459350 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL517244 | — | Ki | = | 0.358 | nM | 9.45 |
| CHEMBL459373 | — | Ki | = | 1.21 | nM | 8.92 |
| CHEMBL517407 | — | Ki | = | 1.54 | nM | 8.81 |
| CHEMBL464811 | — | Ki | = | 3.27 | nM | 8.48 |
| CHEMBL460402 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL457957 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL629 | AMITRIPTYLINE | Ki | > | 1000.0 | nM | - |
| CHEMBL21731 | MAPROTILINE | Ki | > | 1000.0 | nM | - |
| CHEMBL71 | CHLORPROMAZINE | Ki | > | 1000.0 | nM | - |
| CHEMBL908 | CHLORPROTHIXENE | Ki | > | 1000.0 | nM | - |
| CHEMBL42 | CLOZAPINE | Ki | > | 1000.0 | nM | - |
| CHEMBL726 | FLUPHENAZINE | Ki | > | 1000.0 | nM | - |