Assay Detail
Binding
CHEMBL651991
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In vitro binding affinity against Alpha-1B 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 | 7.30 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 8.72 |
| CHEMBL342731 | — | — | 1 | 8.12 |
| CHEMBL145443 | — | — | 1 | 8.08 |
| CHEMBL142251 | — | — | 1 | 8.06 |
| CHEMBL341849 | — | — | 1 | 7.89 |
| CHEMBL142398 | — | — | 1 | 7.82 |
| CHEMBL145190 | — | — | 2 | 7.82 |
| CHEMBL141821 | — | — | 1 | 7.80 |
| CHEMBL142307 | — | — | 1 | 7.77 |
| CHEMBL344525 | — | — | 1 | 7.77 |
| CHEMBL146654 | — | — | 1 | 7.75 |
| CHEMBL145843 | — | — | 1 | 7.64 |
| CHEMBL145338 | — | — | 1 | 7.60 |
| CHEMBL445577 | — | — | 1 | 7.50 |
| CHEMBL145525 | — | — | 1 | 7.37 |
| CHEMBL145547 | — | — | 1 | 7.31 |
| CHEMBL357172 | — | — | 1 | 7.24 |
| CHEMBL142236 | — | — | 1 | 7.00 |
| CHEMBL145072 | — | — | 1 | 6.89 |
| CHEMBL145394 | — | — | 2 | 6.87 |
| CHEMBL359433 | — | — | 1 | 6.82 |
| CHEMBL145574 | — | — | 1 | 6.77 |
| CHEMBL358795 | — | — | 1 | 6.66 |
| CHEMBL356584 | — | — | 1 | 6.58 |
| CHEMBL357439 | — | — | 1 | 6.39 |
| CHEMBL145756 | — | — | 1 | 6.29 |
| CHEMBL142718 | — | — | 1 | 6.14 |
| CHEMBL145122 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL342731 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL145443 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL142251 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL341849 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL145190 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL145190 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL142398 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL141821 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL344525 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL142307 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL146654 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL145843 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL145338 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL445577 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL145525 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL145547 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL357172 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL142236 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL145072 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL145394 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL359433 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL145574 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL145394 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL358795 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL356584 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL357439 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL145756 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL142718 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL145122 | — | Ki | = | 1300.0 | nM | 5.89 |