Assay Detail
Binding
CHEMBL873186
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In vitro binding affinity against Alpha-1A 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 | 9.03 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL142743 | — | — | 1 | 10.00 |
| CHEMBL298713 | — | — | 1 | 10.00 |
| CHEMBL141444 | — | — | 1 | 9.70 |
| CHEMBL358595 | — | — | 3 | 9.70 |
| CHEMBL356584 | — | — | 1 | 9.70 |
| CHEMBL144925 | — | — | 1 | 9.70 |
| CHEMBL142957 | — | — | 1 | 9.52 |
| CHEMBL142383 | — | — | 3 | 9.40 |
| CHEMBL5483012 | — | — | 1 | 9.40 |
| CHEMBL145562 | — | — | 1 | 9.15 |
| CHEMBL123012 | — | — | 1 | 9.10 |
| CHEMBL143066 | — | — | 1 | 8.96 |
| CHEMBL145752 | — | — | 1 | 8.92 |
| CHEMBL145610 | — | — | 1 | 8.92 |
| CHEMBL356978 | — | — | 1 | 8.82 |
| CHEMBL358489 | — | — | 1 | 8.74 |
| CHEMBL145334 | — | — | 1 | 8.68 |
| CHEMBL356829 | — | — | 1 | 8.62 |
| CHEMBL146163 | — | — | 1 | 8.35 |
| CHEMBL143940 | — | — | 1 | 8.30 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 8.16 |
| CHEMBL359173 | — | — | 1 | 8.10 |
| CHEMBL145267 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL142743 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL298713 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL141444 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL358595 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL356584 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL144925 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL142957 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL142383 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL5483012 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL142383 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL358595 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL145562 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL123012 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL143066 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL145752 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL145610 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL356978 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL358489 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL358595 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL145334 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL142383 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL356829 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL146163 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL143940 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL611 | TERAZOSIN | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL359173 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL145267 | — | Ki | = | 10.0 | nM | 8.00 |