Assay Detail
Binding
CHEMBL1909090
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 6.10 | 8.37 |
| Ki | 871 | 6.94 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL157138 | LISURIDE | 3.0 | 2 | 9.20 |
| CHEMBL42 | CLOZAPINE | 4.0 | 2 | 8.94 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | — | 2 | 8.90 |
| CHEMBL85 | RISPERIDONE | 4.0 | 2 | 8.86 |
| CHEMBL1732 | DIHYDROERGOTAMINE | 4.0 | 2 | 8.82 |
| CHEMBL442 | ERGOTAMINE | 4.0 | 2 | 8.74 |
| CHEMBL1385840 | ERGOCORNINE | — | 2 | 8.62 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 2 | 8.29 |
| CHEMBL1403281 | ERGOCRYPTINE | — | 2 | 8.26 |
| CHEMBL1909072 | PIPAMAZINE | 4.0 | 2 | 8.19 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 8.07 |
| CHEMBL728 | PROCHLORPERAZINE | 4.0 | 2 | 7.92 |
| CHEMBL723 | CARVEDILOL | 4.0 | 2 | 7.89 |
| CHEMBL1626 | CLEMASTINE | 4.0 | 2 | 7.85 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 2 | 7.80 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 2 | 7.66 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 7.60 |
| CHEMBL50588 | EMETINE | 4.0 | 2 | 7.58 |
| CHEMBL6437 | MIANSERIN | 4.0 | 2 | 7.58 |
| CHEMBL19215 | METERGOLINE | 2.0 | 2 | 7.57 |
| CHEMBL445 | NORTRIPTYLINE | 4.0 | 2 | 7.52 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 2 | 7.50 |
| CHEMBL564 | PROMAZINE | 4.0 | 2 | 7.43 |
| CHEMBL305660 | EBASTINE | 4.0 | 2 | 7.40 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 7.27 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 2 | 7.24 |
| CHEMBL716 | QUETIAPINE | 4.0 | 2 | 7.21 |
| CHEMBL1714574 | TERCONAZOLE | 4.0 | 2 | 7.21 |
| CHEMBL493 | BROMOCRIPTINE | 4.0 | 2 | 7.12 |
| CHEMBL715 | OLANZAPINE | 4.0 | 2 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL157138 | LISURIDE | Ki | = | 0.626 | nM | 9.20 |
| CHEMBL42 | CLOZAPINE | Ki | = | 1.144 | nM | 8.94 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | Ki | = | 1.257 | nM | 8.90 |
| CHEMBL85 | RISPERIDONE | Ki | = | 1.389 | nM | 8.86 |
| CHEMBL1732 | DIHYDROERGOTAMINE | Ki | = | 1.51 | nM | 8.82 |
| CHEMBL442 | ERGOTAMINE | Ki | = | 1.809 | nM | 8.74 |
| CHEMBL1385840 | ERGOCORNINE | Ki | = | 2.409 | nM | 8.62 |
| CHEMBL157138 | LISURIDE | IC50 | = | 4.308 | nM | 8.37 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 5.162 | nM | 8.29 |
| CHEMBL1403281 | ERGOCRYPTINE | Ki | = | 5.484 | nM | 8.26 |
| CHEMBL1909072 | PIPAMAZINE | Ki | = | 6.468 | nM | 8.19 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 7.875 | nM | 8.10 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 8.599 | nM | 8.07 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | IC50 | = | 8.65 | nM | 8.06 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 9.557 | nM | 8.02 |
| CHEMBL1732 | DIHYDROERGOTAMINE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL728 | PROCHLORPERAZINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL442 | ERGOTAMINE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL723 | CARVEDILOL | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1626 | CLEMASTINE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1385840 | ERGOCORNINE | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL726 | FLUPHENAZINE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL50588 | EMETINE | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL6437 | MIANSERIN | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL19215 | METERGOLINE | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL445 | NORTRIPTYLINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL30008 | FLUNARIZINE | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL15245 | YOHIMBINE | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL564 | PROMAZINE | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL1403281 | ERGOCRYPTINE | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL305660 | EBASTINE | Ki | = | 40.1 | nM | 7.40 |
| CHEMBL1909072 | PIPAMAZINE | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL1201203 | BENZTROPINE | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1714574 | TERCONAZOLE | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL716 | QUETIAPINE | Ki | = | 61.1 | nM | 7.21 |
| CHEMBL493 | BROMOCRIPTINE | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL715 | OLANZAPINE | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL728 | PROCHLORPERAZINE | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2 | PRAZOSIN | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL1626 | CLEMASTINE | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL43064 | CINNARIZINE | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL81 | RALOXIFENE | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL597 | PHENTOLAMINE | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1729 | CISAPRIDE | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL219916 | DOMPERIDONE | Ki | = | 147.0 | nM | 6.83 |