Assay Detail
Binding
CHEMBL649225
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against alpha-2 adrenergic receptor was determined by the displacement of [3H]clonidine from rat brain cortical membranes
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 8.08 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38829 | — | — | 1 | 9.35 |
| CHEMBL416072 | — | — | 1 | 9.33 |
| CHEMBL41224 | — | — | 1 | 9.14 |
| CHEMBL41720 | — | — | 1 | 9.04 |
| CHEMBL36616 | — | — | 1 | 9.04 |
| CHEMBL38406 | — | — | 1 | 8.82 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 8.74 |
| CHEMBL39254 | — | — | 1 | 8.72 |
| CHEMBL38788 | — | — | 1 | 8.71 |
| CHEMBL41111 | — | — | 1 | 8.68 |
| CHEMBL289153 | — | — | 1 | 8.64 |
| CHEMBL41171 | — | — | 1 | 8.47 |
| CHEMBL290853 | — | — | 1 | 8.46 |
| CHEMBL38660 | — | — | 1 | 8.41 |
| CHEMBL41064 | — | — | 1 | 8.38 |
| CHEMBL41456 | — | — | 1 | 8.22 |
| CHEMBL39286 | — | — | 1 | 8.16 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 8.00 |
| CHEMBL41861 | — | — | 1 | 7.91 |
| CHEMBL290324 | — | — | 1 | 7.88 |
| CHEMBL37352 | — | — | 1 | 7.86 |
| CHEMBL288398 | — | — | 1 | 7.60 |
| CHEMBL43401 | — | — | 1 | 7.58 |
| CHEMBL38579 | — | — | 1 | 7.42 |
| CHEMBL41756 | — | — | 1 | 7.33 |
| CHEMBL289098 | — | — | 1 | 7.27 |
| CHEMBL41803 | — | — | 1 | 7.14 |
| CHEMBL41223 | — | — | 1 | 7.11 |
| CHEMBL288337 | — | — | 1 | 6.58 |
| CHEMBL43138 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38829 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL416072 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL41224 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL41720 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL36616 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL38406 | — | Ki | = | 1.52 | nM | 8.82 |
| CHEMBL134 | CLONIDINE | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL39254 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL38788 | — | Ki | = | 1.93 | nM | 8.71 |
| CHEMBL41111 | — | Ki | = | 2.11 | nM | 8.68 |
| CHEMBL289153 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL41171 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL290853 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL38660 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL41064 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL41456 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL39286 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL41861 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL290324 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL37352 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL288398 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL43401 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL38579 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL41756 | — | Ki | = | 46.7 | nM | 7.33 |
| CHEMBL289098 | — | Ki | = | 53.6 | nM | 7.27 |
| CHEMBL41803 | — | Ki | = | 72.3 | nM | 7.14 |
| CHEMBL41223 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL288337 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL43138 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL38790 | — | Ki | = | 719.0 | nM | 6.14 |
| CHEMBL41549 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL41305 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL41103 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2 | PRAZOSIN | Ki | > | 1000.0 | nM | - |