Assay Detail
Binding
CHEMBL866126
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Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Submaxillary gland |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of selective alpha1B adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.04 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.64 |
| CHEMBL541129 | — | — | 1 | 7.68 |
| CHEMBL557584 | — | — | 1 | 7.25 |
| CHEMBL537651 | — | — | 1 | 7.24 |
| CHEMBL534943 | — | — | 1 | 7.24 |
| CHEMBL534944 | — | — | 1 | 7.22 |
| CHEMBL537428 | — | — | 1 | 6.92 |
| CHEMBL537650 | — | — | 1 | 6.32 |
| CHEMBL539601 | — | — | 1 | 6.16 |
| CHEMBL535838 | — | — | 1 | 6.05 |
| CHEMBL535837 | — | — | 1 | 5.72 |
| CHEMBL539600 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL541129 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL557584 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL537651 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL534943 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL534944 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL537428 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL537650 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL539601 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL535838 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL535837 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL539600 | — | Ki | - | — | - |