Assay Detail
Binding
CHEMBL643401
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In vitro binding affinity against Alpha-1D adrenergic receptor of human liver microsomes.
30
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Liver |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 7.10 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 8.46 |
| CHEMBL344525 | — | — | 1 | 8.01 |
| CHEMBL145190 | — | — | 2 | 7.92 |
| CHEMBL142251 | — | — | 1 | 7.85 |
| CHEMBL142398 | — | — | 1 | 7.85 |
| CHEMBL342731 | — | — | 1 | 7.68 |
| CHEMBL341849 | — | — | 1 | 7.55 |
| CHEMBL145338 | — | — | 1 | 7.52 |
| CHEMBL146654 | — | — | 1 | 7.51 |
| CHEMBL141821 | — | — | 1 | 7.51 |
| CHEMBL145843 | — | — | 1 | 7.50 |
| CHEMBL145547 | — | — | 1 | 7.47 |
| CHEMBL145443 | — | — | 1 | 7.43 |
| CHEMBL142307 | — | — | 1 | 7.28 |
| CHEMBL445577 | — | — | 1 | 7.04 |
| CHEMBL145525 | — | — | 1 | 6.92 |
| CHEMBL357172 | — | — | 1 | 6.85 |
| CHEMBL142236 | — | — | 1 | 6.85 |
| CHEMBL145072 | — | — | 1 | 6.72 |
| CHEMBL145394 | — | — | 2 | 6.60 |
| CHEMBL145574 | — | — | 1 | 6.54 |
| CHEMBL356584 | — | — | 1 | 6.47 |
| CHEMBL359433 | — | — | 1 | 6.47 |
| CHEMBL358795 | — | — | 1 | 6.41 |
| CHEMBL357439 | — | — | 1 | 6.32 |
| CHEMBL145756 | — | — | 1 | 6.21 |
| CHEMBL142718 | — | — | 1 | 5.96 |
| CHEMBL145122 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL344525 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL145190 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL142251 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL142398 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL145190 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL342731 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL341849 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL145338 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL146654 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL141821 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL145843 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL145547 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL145443 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL142307 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL445577 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL145525 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL357172 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL142236 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL145072 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL145394 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL145574 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL145394 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL356584 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL359433 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL358795 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL357439 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL145756 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL142718 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL145122 | — | Ki | = | 1800.0 | nM | 5.75 |