Assay Detail
Binding
CHEMBL1909159
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DRUGMATRIX: Imidazoline I2, Central radioligand binding (ligand: [3H] Idazoxan)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 6.27 | 8.79 |
| Ki | 871 | 6.44 | 8.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL157138 | LISURIDE | 3.0 | 2 | 8.97 |
| CHEMBL1732 | DIHYDROERGOTAMINE | 4.0 | 2 | 8.78 |
| CHEMBL1403281 | ERGOCRYPTINE | — | 2 | 8.66 |
| CHEMBL442 | ERGOTAMINE | 4.0 | 2 | 8.61 |
| CHEMBL1385840 | ERGOCORNINE | — | 2 | 8.52 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | — | 2 | 8.44 |
| CHEMBL420 | GUANABENZ | 4.0 | 2 | 7.92 |
| CHEMBL85 | RISPERIDONE | 4.0 | 2 | 7.89 |
| CHEMBL762 | OXYMETAZOLINE | 4.0 | 2 | 7.75 |
| CHEMBL862 | GUANFACINE | 4.0 | 2 | 7.52 |
| CHEMBL1365675 | AMITRAZ | 2.0 | 2 | 7.50 |
| CHEMBL493 | BROMOCRIPTINE | 4.0 | 2 | 7.46 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 2 | 7.41 |
| CHEMBL134 | CLONIDINE | 4.0 | 2 | 7.37 |
| CHEMBL844 | BRIMONIDINE | 4.0 | 2 | 7.31 |
| CHEMBL6437 | MIANSERIN | 4.0 | 2 | 7.08 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 2 | 6.98 |
| CHEMBL679 | EPINEPHRINE | 4.0 | 2 | 6.81 |
| CHEMBL42 | CLOZAPINE | 4.0 | 2 | 6.59 |
| CHEMBL1535 | HYDROXYCHLOROQUINE | 4.0 | 2 | 6.50 |
| CHEMBL1909065 | MADURAMICIN ACID | 2.0 | 2 | 6.39 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 2 | 6.33 |
| CHEMBL1909072 | PIPAMAZINE | 4.0 | 2 | 6.29 |
| CHEMBL2 | PRAZOSIN | 4.0 | 2 | 6.20 |
| CHEMBL564 | PROMAZINE | 4.0 | 2 | 6.13 |
| CHEMBL715 | OLANZAPINE | 4.0 | 2 | 6.11 |
| CHEMBL12089 | BERBERINE CHLORIDE | 1.0 | 2 | 6.07 |
| CHEMBL611 | TERAZOSIN | 4.0 | 2 | 6.07 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 2 | 6.06 |
| CHEMBL19236 | MOXONIDINE | 4.0 | 2 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL157138 | LISURIDE | Ki | = | 1.071 | nM | 8.97 |
| CHEMBL157138 | LISURIDE | IC50 | = | 1.606 | nM | 8.79 |
| CHEMBL1732 | DIHYDROERGOTAMINE | Ki | = | 1.669 | nM | 8.78 |
| CHEMBL1403281 | ERGOCRYPTINE | Ki | = | 2.186 | nM | 8.66 |
| CHEMBL442 | ERGOTAMINE | Ki | = | 2.43 | nM | 8.61 |
| CHEMBL1732 | DIHYDROERGOTAMINE | IC50 | = | 2.503 | nM | 8.60 |
| CHEMBL1385840 | ERGOCORNINE | Ki | = | 2.991 | nM | 8.52 |
| CHEMBL1403281 | ERGOCRYPTINE | IC50 | = | 3.279 | nM | 8.48 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | Ki | = | 3.619 | nM | 8.44 |
| CHEMBL442 | ERGOTAMINE | IC50 | = | 3.645 | nM | 8.44 |
| CHEMBL1385840 | ERGOCORNINE | IC50 | = | 4.487 | nM | 8.35 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | IC50 | = | 5.428 | nM | 8.27 |
| CHEMBL420 | GUANABENZ | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL85 | RISPERIDONE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL420 | GUANABENZ | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL762 | OXYMETAZOLINE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL762 | OXYMETAZOLINE | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL862 | GUANFACINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1365675 | AMITRAZ | Ki | = | 31.8 | nM | 7.50 |
| CHEMBL493 | BROMOCRIPTINE | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL134 | CLONIDINE | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL862 | GUANFACINE | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1365675 | AMITRAZ | IC50 | = | 47.7 | nM | 7.32 |
| CHEMBL844 | BRIMONIDINE | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL493 | BROMOCRIPTINE | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL597 | PHENTOLAMINE | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL134 | CLONIDINE | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL844 | BRIMONIDINE | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL6437 | MIANSERIN | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL6437 | MIANSERIN | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL679 | EPINEPHRINE | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL15245 | YOHIMBINE | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL679 | EPINEPHRINE | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL42 | CLOZAPINE | Ki | = | 256.0 | nM | 6.59 |
| CHEMBL1535 | HYDROXYCHLOROQUINE | Ki | = | 319.0 | nM | 6.50 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL1909065 | MADURAMICIN ACID | Ki | = | 405.0 | nM | 6.39 |
| CHEMBL86 | METOCLOPRAMIDE | Ki | = | 472.0 | nM | 6.33 |
| CHEMBL1535 | HYDROXYCHLOROQUINE | IC50 | = | 479.0 | nM | 6.32 |
| CHEMBL1909072 | PIPAMAZINE | Ki | = | 512.0 | nM | 6.29 |
| CHEMBL1909065 | MADURAMICIN ACID | IC50 | = | 607.0 | nM | 6.22 |
| CHEMBL2 | PRAZOSIN | Ki | = | 633.0 | nM | 6.20 |
| CHEMBL86 | METOCLOPRAMIDE | IC50 | = | 708.0 | nM | 6.15 |
| CHEMBL564 | PROMAZINE | Ki | = | 732.0 | nM | 6.13 |
| CHEMBL1909072 | PIPAMAZINE | IC50 | = | 768.0 | nM | 6.12 |
| CHEMBL715 | OLANZAPINE | Ki | = | 772.0 | nM | 6.11 |
| CHEMBL12089 | BERBERINE CHLORIDE | Ki | = | 852.0 | nM | 6.07 |