Assay Detail
Binding
CHEMBL643400
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In vitro binding affinity against alpha-1D 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 | 6.33 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.52 |
| CHEMBL144933 | — | — | 1 | 6.96 |
| CHEMBL342126 | — | — | 1 | 6.92 |
| CHEMBL298713 | — | — | 1 | 6.85 |
| CHEMBL145459 | — | — | 1 | 6.82 |
| CHEMBL142981 | — | — | 1 | 6.82 |
| CHEMBL262217 | — | — | 1 | 6.75 |
| CHEMBL144989 | — | — | 1 | 6.72 |
| CHEMBL145170 | — | — | 1 | 6.68 |
| CHEMBL145332 | — | — | 1 | 6.64 |
| CHEMBL424494 | — | — | 1 | 6.64 |
| CHEMBL145894 | — | — | 1 | 6.60 |
| CHEMBL142929 | — | — | 1 | 6.58 |
| CHEMBL358785 | — | — | 1 | 6.48 |
| CHEMBL356584 | — | — | 1 | 6.47 |
| CHEMBL144925 | — | — | 1 | 6.47 |
| CHEMBL144965 | — | — | 1 | 6.43 |
| CHEMBL146109 | — | — | 1 | 6.32 |
| CHEMBL356571 | — | — | 1 | 6.25 |
| CHEMBL359012 | — | — | 1 | 6.21 |
| CHEMBL144938 | — | — | 1 | 6.21 |
| CHEMBL142243 | — | — | 1 | 6.19 |
| CHEMBL145719 | — | — | 1 | 6.12 |
| CHEMBL342543 | — | — | 1 | 6.11 |
| CHEMBL344339 | — | — | 1 | 6.04 |
| CHEMBL145134 | — | — | 1 | 6.03 |
| CHEMBL357628 | — | — | 1 | 5.89 |
| CHEMBL342111 | — | — | 1 | 5.81 |
| CHEMBL145571 | — | — | 1 | 5.71 |
| CHEMBL358590 | — | — | 2 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL144933 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL342126 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL298713 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL145459 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL142981 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL262217 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL144989 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL145170 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL424494 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL145332 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL145894 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL142929 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL358785 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL356584 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL144925 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL144965 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL146109 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL356571 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL359012 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL144938 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL142243 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL145719 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL342543 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL344339 | — | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL145134 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL357628 | — | Ki | = | 1280.0 | nM | 5.89 |
| CHEMBL342111 | — | Ki | = | 1560.0 | nM | 5.81 |
| CHEMBL145571 | — | Ki | = | 1940.0 | nM | 5.71 |
| CHEMBL358590 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL358590 | — | Ki | = | 2260.0 | nM | 5.65 |
| CHEMBL239806 | — | Ki | = | 2260.0 | nM | 5.65 |
| CHEMBL341838 | — | Ki | = | 5280.0 | nM | 5.28 |
| CHEMBL145553 | — | Ki | = | 5370.0 | nM | 5.27 |
| CHEMBL342064 | — | Ki | = | 14700.0 | nM | 4.83 |