Assay Detail
Binding
CHEMBL651990
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In vitro binding affinity against Alpha-1B adrenergic receptor of human liver microsomes.
35
Total Activities
34
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. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 6.52 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.22 |
| CHEMBL342126 | — | — | 1 | 7.70 |
| CHEMBL144933 | — | — | 1 | 7.52 |
| CHEMBL145459 | — | — | 1 | 7.44 |
| CHEMBL144989 | — | — | 1 | 7.44 |
| CHEMBL298713 | — | — | 1 | 7.35 |
| CHEMBL145894 | — | — | 1 | 7.10 |
| CHEMBL356571 | — | — | 1 | 7.08 |
| CHEMBL142929 | — | — | 1 | 6.89 |
| CHEMBL142981 | — | — | 1 | 6.85 |
| CHEMBL262217 | — | — | 1 | 6.82 |
| CHEMBL144925 | — | — | 1 | 6.66 |
| CHEMBL144965 | — | — | 1 | 6.60 |
| CHEMBL358785 | — | — | 1 | 6.60 |
| CHEMBL356584 | — | — | 1 | 6.60 |
| CHEMBL146109 | — | — | 1 | 6.57 |
| CHEMBL344339 | — | — | 1 | 6.51 |
| CHEMBL145332 | — | — | 1 | 6.47 |
| CHEMBL145170 | — | — | 1 | 6.40 |
| CHEMBL424494 | — | — | 1 | 6.39 |
| CHEMBL142243 | — | — | 1 | 6.36 |
| CHEMBL359012 | — | — | 1 | 6.31 |
| CHEMBL357628 | — | — | 1 | 6.21 |
| CHEMBL342543 | — | — | 1 | 6.16 |
| CHEMBL145134 | — | — | 1 | 6.14 |
| CHEMBL145719 | — | — | 1 | 6.07 |
| CHEMBL144938 | — | — | 1 | 5.98 |
| CHEMBL358590 | — | — | 2 | 5.84 |
| CHEMBL342111 | — | — | 1 | 5.83 |
| CHEMBL239806 | — | — | 1 | 5.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL342126 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL144933 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL145459 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL144989 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL298713 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL145894 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL356571 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL142929 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL142981 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL262217 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL144925 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL358785 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL356584 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL144965 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL146109 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL344339 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL145332 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL145170 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL424494 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL142243 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL359012 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL357628 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL342543 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL145134 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL145719 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL144938 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL358590 | — | Ki | = | 1450.0 | nM | 5.84 |
| CHEMBL342111 | — | Ki | = | 1490.0 | nM | 5.83 |
| CHEMBL358590 | — | Ki | = | 1480.0 | nM | 5.83 |
| CHEMBL239806 | — | Ki | = | 1940.0 | nM | 5.71 |
| CHEMBL341838 | — | Ki | = | 2630.0 | nM | 5.58 |
| CHEMBL145571 | — | Ki | = | 2820.0 | nM | 5.55 |
| CHEMBL145553 | — | Ki | = | 3130.0 | nM | 5.50 |
| CHEMBL342064 | — | Ki | = | 15500.0 | nM | 4.81 |