Assay Detail
Binding
CHEMBL1909088
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: 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 | 6.11 | 9.51 |
| Ki | 871 | 6.54 | 9.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL157138 | LISURIDE | 3.0 | 2 | 9.94 |
| CHEMBL1732 | DIHYDROERGOTAMINE | 4.0 | 2 | 9.41 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | — | 2 | 9.13 |
| CHEMBL442 | ERGOTAMINE | 4.0 | 2 | 9.10 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 2 | 8.65 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 2 | 8.64 |
| CHEMBL1385840 | ERGOCORNINE | — | 2 | 8.63 |
| CHEMBL1403281 | ERGOCRYPTINE | — | 2 | 8.53 |
| CHEMBL85 | RISPERIDONE | 4.0 | 2 | 8.44 |
| CHEMBL493 | BROMOCRIPTINE | 4.0 | 2 | 8.26 |
| CHEMBL762 | OXYMETAZOLINE | 4.0 | 2 | 8.06 |
| CHEMBL50588 | EMETINE | 4.0 | 2 | 7.85 |
| CHEMBL420 | GUANABENZ | 4.0 | 2 | 7.82 |
| CHEMBL6437 | MIANSERIN | 4.0 | 2 | 7.80 |
| CHEMBL19215 | METERGOLINE | 2.0 | 2 | 7.66 |
| CHEMBL1909072 | PIPAMAZINE | 4.0 | 2 | 7.60 |
| CHEMBL42 | CLOZAPINE | 4.0 | 2 | 7.47 |
| CHEMBL723 | CARVEDILOL | 4.0 | 2 | 7.40 |
| CHEMBL862 | GUANFACINE | 4.0 | 2 | 7.30 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 7.30 |
| CHEMBL728 | PROCHLORPERAZINE | 4.0 | 2 | 7.20 |
| CHEMBL1909065 | MADURAMICIN ACID | 2.0 | 2 | 7.17 |
| CHEMBL1626 | CLEMASTINE | 4.0 | 2 | 7.16 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 2 | 7.10 |
| CHEMBL334255 | CETYLPYRIDINIUM BROMIDE | — | 2 | 7.04 |
| CHEMBL531 | PERGOLIDE | 4.0 | 2 | 7.00 |
| CHEMBL134 | CLONIDINE | 4.0 | 2 | 6.98 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 2 | 6.97 |
| CHEMBL809 | SERTRALINE | 4.0 | 2 | 6.96 |
| CHEMBL844 | BRIMONIDINE | 4.0 | 2 | 6.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL157138 | LISURIDE | Ki | = | 0.116 | nM | 9.94 |
| CHEMBL157138 | LISURIDE | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL1732 | DIHYDROERGOTAMINE | Ki | = | 0.387 | nM | 9.41 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | Ki | = | 0.747 | nM | 9.13 |
| CHEMBL442 | ERGOTAMINE | Ki | = | 0.796 | nM | 9.10 |
| CHEMBL1732 | DIHYDROERGOTAMINE | IC50 | = | 1.032 | nM | 8.99 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | IC50 | = | 1.993 | nM | 8.70 |
| CHEMBL442 | ERGOTAMINE | IC50 | = | 2.123 | nM | 8.67 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 2.25 | nM | 8.65 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 2.307 | nM | 8.64 |
| CHEMBL1385840 | ERGOCORNINE | Ki | = | 2.361 | nM | 8.63 |
| CHEMBL1403281 | ERGOCRYPTINE | Ki | = | 2.98 | nM | 8.53 |
| CHEMBL85 | RISPERIDONE | Ki | = | 3.628 | nM | 8.44 |
| CHEMBL493 | BROMOCRIPTINE | Ki | = | 5.533 | nM | 8.26 |
| CHEMBL597 | PHENTOLAMINE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL15245 | YOHIMBINE | IC50 | = | 6.151 | nM | 8.21 |
| CHEMBL1385840 | ERGOCORNINE | IC50 | = | 6.296 | nM | 8.20 |
| CHEMBL1403281 | ERGOCRYPTINE | IC50 | = | 7.946 | nM | 8.10 |
| CHEMBL762 | OXYMETAZOLINE | Ki | = | 8.639 | nM | 8.06 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 9.674 | nM | 8.01 |
| CHEMBL50588 | EMETINE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL493 | BROMOCRIPTINE | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL420 | GUANABENZ | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL6437 | MIANSERIN | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL19215 | METERGOLINE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL762 | OXYMETAZOLINE | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1909072 | PIPAMAZINE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL42 | CLOZAPINE | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL50588 | EMETINE | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL723 | CARVEDILOL | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL420 | GUANABENZ | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL6437 | MIANSERIN | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL862 | GUANFACINE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL19215 | METERGOLINE | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL728 | PROCHLORPERAZINE | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL1909072 | PIPAMAZINE | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1909065 | MADURAMICIN ACID | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL1626 | CLEMASTINE | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL726 | FLUPHENAZINE | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL334255 | CETYLPYRIDINIUM BROMIDE | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL531 | PERGOLIDE | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL134 | CLONIDINE | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL516 | CYPROHEPTADINE | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL809 | SERTRALINE | Ki | = | 108.3 | nM | 6.96 |
| CHEMBL844 | BRIMONIDINE | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL633 | AMIODARONE | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL564 | PROMAZINE | Ki | = | 126.0 | nM | 6.90 |