Assay Detail
Binding
CHEMBL643582
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Displacement of [3H]prazosin from alpha-1-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 | 6.02 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 7.37 |
| CHEMBL2447998 | — | — | 1 | 6.80 |
| CHEMBL2448001 | — | — | 1 | 6.70 |
| CHEMBL2448004 | — | — | 1 | 6.60 |
| CHEMBL123188 | — | — | 1 | 6.44 |
| CHEMBL2447999 | — | — | 1 | 6.42 |
| CHEMBL2448003 | — | — | 1 | 6.39 |
| CHEMBL1203218 | — | — | 1 | 5.89 |
| CHEMBL269521 | MK-212 | — | 1 | 5.62 |
| CHEMBL538788 | — | — | 1 | 5.56 |
| CHEMBL2448000 | — | — | 1 | 5.52 |
| CHEMBL1204339 | — | — | 1 | 5.51 |
| CHEMBL2448002 | — | — | 1 | 5.17 |
| CHEMBL120491 | — | — | 1 | 4.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL2447998 | — | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL2448001 | — | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL2448004 | — | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL123188 | — | Kd | = | 360.0 | nM | 6.44 |
| CHEMBL2447999 | — | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL2448003 | — | Kd | = | 410.0 | nM | 6.39 |
| CHEMBL1203218 | — | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL269521 | MK-212 | Kd | = | 2400.0 | nM | 5.62 |
| CHEMBL538788 | — | Kd | = | 2780.0 | nM | 5.56 |
| CHEMBL2448000 | — | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL1204339 | — | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL2448002 | — | Kd | = | 6800.0 | nM | 5.17 |
| CHEMBL120491 | — | Kd | = | 51000.0 | nM | 4.29 |