Assay Detail
Binding
CHEMBL651989
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In vitro binding affinity against Alpha-1B 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 | 7.08 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 8.72 |
| CHEMBL142957 | — | — | 1 | 7.82 |
| CHEMBL142383 | — | — | 3 | 7.72 |
| CHEMBL143940 | — | — | 1 | 7.57 |
| CHEMBL142743 | — | — | 1 | 7.57 |
| CHEMBL123012 | — | — | 1 | 7.43 |
| CHEMBL298713 | — | — | 1 | 7.35 |
| CHEMBL146163 | — | — | 1 | 7.32 |
| CHEMBL143066 | — | — | 1 | 7.30 |
| CHEMBL356978 | — | — | 1 | 7.17 |
| CHEMBL5483012 | — | — | 1 | 7.13 |
| CHEMBL359173 | — | — | 1 | 7.11 |
| CHEMBL145610 | — | — | 1 | 7.11 |
| CHEMBL141444 | — | — | 1 | 7.06 |
| CHEMBL145562 | — | — | 1 | 7.00 |
| CHEMBL145334 | — | — | 1 | 7.00 |
| CHEMBL358489 | — | — | 1 | 6.96 |
| CHEMBL358595 | — | — | 3 | 6.89 |
| CHEMBL145752 | — | — | 1 | 6.86 |
| CHEMBL356584 | — | — | 1 | 6.58 |
| CHEMBL144925 | — | — | 1 | 6.47 |
| CHEMBL145267 | — | — | 1 | 5.80 |
| CHEMBL356829 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL142957 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL142383 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL143940 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL142743 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL142383 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL123012 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL298713 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL146163 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL143066 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL356978 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL5483012 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL145610 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL359173 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL142383 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL141444 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL145562 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL145334 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL358489 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL358595 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL145752 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL358595 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL356584 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL144925 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL358595 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL145267 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL356829 | — | Ki | = | 3700.0 | nM | 5.43 |