Assay Detail
Binding
CHEMBL1909085
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Submaxillary gland |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 6.77 | 9.66 |
| Ki | 871 | 7.16 | 10.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 2 | 10.06 |
| CHEMBL85 | RISPERIDONE | 4.0 | 2 | 9.40 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 2 | 9.20 |
| CHEMBL1108 | DROPERIDOL | 4.0 | 2 | 9.18 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | — | 2 | 9.18 |
| CHEMBL1732 | DIHYDROERGOTAMINE | 4.0 | 2 | 8.69 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 8.69 |
| CHEMBL1909072 | PIPAMAZINE | 4.0 | 2 | 8.68 |
| CHEMBL493 | BROMOCRIPTINE | 4.0 | 2 | 8.55 |
| CHEMBL723 | CARVEDILOL | 4.0 | 2 | 8.50 |
| CHEMBL442 | ERGOTAMINE | 4.0 | 2 | 8.49 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 8.46 |
| CHEMBL564 | PROMAZINE | 4.0 | 2 | 8.43 |
| CHEMBL1403281 | ERGOCRYPTINE | — | 2 | 8.37 |
| CHEMBL1385840 | ERGOCORNINE | — | 2 | 8.35 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 2 | 8.33 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 8.25 |
| CHEMBL157138 | LISURIDE | 3.0 | 2 | 8.04 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 2 | 8.02 |
| CHEMBL611 | TERAZOSIN | 4.0 | 2 | 8.02 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 2 | 8.00 |
| CHEMBL728 | PROCHLORPERAZINE | 4.0 | 2 | 7.89 |
| CHEMBL42 | CLOZAPINE | 4.0 | 2 | 7.82 |
| CHEMBL762 | OXYMETAZOLINE | 4.0 | 2 | 7.80 |
| CHEMBL1626 | CLEMASTINE | 4.0 | 2 | 7.68 |
| CHEMBL429 | LABETALOL | 4.0 | 2 | 7.64 |
| CHEMBL715 | OLANZAPINE | 4.0 | 2 | 7.58 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 2 | 7.55 |
| CHEMBL643 | PROMETHAZINE | 4.0 | 2 | 7.50 |
| CHEMBL716 | QUETIAPINE | 4.0 | 2 | 7.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.088 | nM | 10.06 |
| CHEMBL2 | PRAZOSIN | IC50 | = | 0.218 | nM | 9.66 |
| CHEMBL85 | RISPERIDONE | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL707 | DOXAZOSIN | Ki | = | 0.628 | nM | 9.20 |
| CHEMBL1108 | DROPERIDOL | Ki | = | 0.669 | nM | 9.18 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | Ki | = | 0.656 | nM | 9.18 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 0.989 | nM | 9.01 |
| CHEMBL707 | DOXAZOSIN | IC50 | = | 1.551 | nM | 8.81 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL1108 | DROPERIDOL | IC50 | = | 1.653 | nM | 8.78 |
| CHEMBL1732 | DIHYDROERGOTAMINE | Ki | = | 2.035 | nM | 8.69 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 2.062 | nM | 8.69 |
| CHEMBL1909072 | PIPAMAZINE | Ki | = | 2.081 | nM | 8.68 |
| CHEMBL493 | BROMOCRIPTINE | Ki | = | 2.817 | nM | 8.55 |
| CHEMBL723 | CARVEDILOL | Ki | = | 3.153 | nM | 8.50 |
| CHEMBL442 | ERGOTAMINE | Ki | = | 3.262 | nM | 8.49 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 3.456 | nM | 8.46 |
| CHEMBL564 | PROMAZINE | Ki | = | 3.739 | nM | 8.43 |
| CHEMBL1403281 | ERGOCRYPTINE | Ki | = | 4.279 | nM | 8.37 |
| CHEMBL1385840 | ERGOCORNINE | Ki | = | 4.472 | nM | 8.35 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 4.655 | nM | 8.33 |
| CHEMBL1732 | DIHYDROERGOTAMINE | IC50 | = | 5.028 | nM | 8.30 |
| CHEMBL1909072 | PIPAMAZINE | IC50 | = | 5.142 | nM | 8.29 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 5.093 | nM | 8.29 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 5.599 | nM | 8.25 |
| CHEMBL493 | BROMOCRIPTINE | IC50 | = | 6.96 | nM | 8.16 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 7.789 | nM | 8.11 |
| CHEMBL442 | ERGOTAMINE | IC50 | = | 8.06 | nM | 8.09 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 8.538 | nM | 8.07 |
| CHEMBL157138 | LISURIDE | Ki | = | 9.188 | nM | 8.04 |
| CHEMBL564 | PROMAZINE | IC50 | = | 9.238 | nM | 8.03 |
| CHEMBL726 | FLUPHENAZINE | Ki | = | 9.578 | nM | 8.02 |
| CHEMBL611 | TERAZOSIN | Ki | = | 9.592 | nM | 8.02 |
| CHEMBL296419 | ASTEMIZOLE | Ki | = | 9.901 | nM | 8.00 |
| CHEMBL1385840 | ERGOCORNINE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL597 | PHENTOLAMINE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1403281 | ERGOCRYPTINE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL728 | PROCHLORPERAZINE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL42 | CLOZAPINE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL762 | OXYMETAZOLINE | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1626 | CLEMASTINE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL429 | LABETALOL | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL157138 | LISURIDE | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL726 | FLUPHENAZINE | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL611 | TERAZOSIN | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL715 | OLANZAPINE | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL643 | PROMETHAZINE | Ki | = | 32.0 | nM | 7.50 |