Assay Detail
Binding
CHEMBL643399
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In vitro binding affinity against Alpha-1D adrenergic receptor of human liver microsomes.
27
Total Activities
23
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. 1. Structure-activity relationship in dihydropyrimidinones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 6.68 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 8.46 |
| CHEMBL142383 | — | — | 3 | 7.10 |
| CHEMBL123012 | — | — | 1 | 7.06 |
| CHEMBL142957 | — | — | 1 | 7.04 |
| CHEMBL142743 | — | — | 1 | 7.03 |
| CHEMBL143940 | — | — | 1 | 6.92 |
| CHEMBL145562 | — | — | 1 | 6.85 |
| CHEMBL298713 | — | — | 1 | 6.85 |
| CHEMBL356978 | — | — | 1 | 6.82 |
| CHEMBL5483012 | — | — | 1 | 6.80 |
| CHEMBL146163 | — | — | 1 | 6.77 |
| CHEMBL141444 | — | — | 1 | 6.75 |
| CHEMBL145610 | — | — | 1 | 6.75 |
| CHEMBL143066 | — | — | 1 | 6.75 |
| CHEMBL359173 | — | — | 1 | 6.66 |
| CHEMBL145334 | — | — | 1 | 6.57 |
| CHEMBL358595 | — | — | 3 | 6.54 |
| CHEMBL358489 | — | — | 1 | 6.50 |
| CHEMBL356584 | — | — | 1 | 6.46 |
| CHEMBL145752 | — | — | 1 | 6.40 |
| CHEMBL144925 | — | — | 1 | 6.36 |
| CHEMBL145267 | — | — | 1 | 5.58 |
| CHEMBL356829 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL142383 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL123012 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL142957 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL142743 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL142383 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL143940 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL298713 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL145562 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL356978 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL5483012 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL146163 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL145610 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL142383 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL141444 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL143066 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL359173 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL145334 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL358595 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL358489 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL356584 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL145752 | — | Ki | = | 398.0 | nM | 6.40 |
| CHEMBL358595 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL144925 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL358595 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL145267 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL356829 | — | Ki | = | 8800.0 | nM | 5.06 |