Assay Detail
Binding
CHEMBL643954
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Displacement of [3H]clonidine from alpha-2-adrenergic receptor of calf neocortical membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Piperazinylimidazo[1,2-a]pyrazines with selective affinity for in vitro alpha-adrenergic receptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 14 | 6.26 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 7.72 |
| CHEMBL1204339 | — | — | 1 | 7.72 |
| CHEMBL2448004 | — | — | 1 | 7.06 |
| CHEMBL2447999 | — | — | 1 | 6.84 |
| CHEMBL269521 | MK-212 | — | 1 | 6.82 |
| CHEMBL2447998 | — | — | 1 | 6.60 |
| CHEMBL538788 | — | — | 1 | 6.54 |
| CHEMBL2448003 | — | — | 1 | 6.00 |
| CHEMBL2448001 | — | — | 1 | 5.82 |
| CHEMBL2448000 | — | — | 1 | 5.80 |
| CHEMBL123188 | — | — | 1 | 5.75 |
| CHEMBL1203218 | — | — | 1 | 5.75 |
| CHEMBL2448002 | — | — | 1 | 4.72 |
| CHEMBL120491 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL1204339 | — | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL2448004 | — | Kd | = | 88.0 | nM | 7.06 |
| CHEMBL2447999 | — | Kd | = | 144.0 | nM | 6.84 |
| CHEMBL269521 | MK-212 | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL2447998 | — | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL538788 | — | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL2448003 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL2448001 | — | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL2448000 | — | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL123188 | — | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL1203218 | — | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL2448002 | — | Kd | = | 18900.0 | nM | 4.72 |
| CHEMBL120491 | — | Kd | = | 28100.0 | nM | 4.55 |