Assay Detail
Binding
CHEMBL646286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
42
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 8.77 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL40650 | — | — | 1 | 9.57 |
| CHEMBL290519 | — | — | 1 | 9.55 |
| CHEMBL291073 | — | — | 1 | 9.54 |
| CHEMBL287965 | — | — | 1 | 9.48 |
| CHEMBL441032 | — | — | 1 | 9.46 |
| CHEMBL290243 | — | — | 1 | 9.41 |
| CHEMBL40780 | — | — | 1 | 9.40 |
| CHEMBL41444 | — | — | 1 | 9.36 |
| CHEMBL2112073 | — | — | 2 | 9.33 |
| CHEMBL297218 | — | — | 1 | 9.31 |
| CHEMBL291154 | — | — | 1 | 9.29 |
| CHEMBL290388 | — | — | 1 | 9.28 |
| CHEMBL40754 | — | — | 1 | 9.28 |
| CHEMBL291262 | — | — | 1 | 9.23 |
| CHEMBL289361 | — | — | 2 | 9.19 |
| CHEMBL41234 | — | — | 1 | 9.18 |
| CHEMBL288678 | — | — | 1 | 9.17 |
| CHEMBL288530 | — | — | 1 | 9.14 |
| CHEMBL41344 | — | — | 1 | 9.11 |
| CHEMBL287928 | — | — | 1 | 9.10 |
| CHEMBL288809 | — | — | 1 | 9.10 |
| CHEMBL39037 | — | — | 1 | 8.89 |
| CHEMBL40819 | — | — | 1 | 8.89 |
| CHEMBL40896 | — | — | 1 | 8.79 |
| CHEMBL41155 | — | — | 1 | 8.79 |
| CHEMBL40310 | — | — | 1 | 8.67 |
| CHEMBL417890 | — | — | 1 | 8.66 |
| CHEMBL289437 | — | — | 1 | 8.50 |
| CHEMBL289166 | — | — | 1 | 8.48 |
| CHEMBL43909 | — | — | 1 | 8.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL40650 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL290519 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL291073 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL287965 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL441032 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL290243 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL40780 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL41444 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL2112073 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL297218 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL291154 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL40754 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL290388 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL291262 | — | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL289361 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL41234 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL288678 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL288530 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL41344 | — | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL287928 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL288809 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL289361 | — | Ki | = | 1.08 | nM | 8.97 |
| CHEMBL40819 | — | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL39037 | — | Ki | = | 1.29 | nM | 8.89 |
| CHEMBL41155 | — | Ki | = | 1.64 | nM | 8.79 |
| CHEMBL40896 | — | Ki | = | 1.62 | nM | 8.79 |
| CHEMBL40310 | — | Ki | = | 2.16 | nM | 8.67 |
| CHEMBL417890 | — | Ki | = | 2.17 | nM | 8.66 |
| CHEMBL289437 | — | Ki | = | 3.13 | nM | 8.50 |
| CHEMBL289166 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL43909 | — | Ki | = | 3.91 | nM | 8.41 |
| CHEMBL43573 | — | Ki | = | 4.75 | nM | 8.32 |
| CHEMBL434591 | — | Ki | = | 5.27 | nM | 8.28 |
| CHEMBL289627 | — | Ki | = | 6.35 | nM | 8.20 |
| CHEMBL289758 | — | Ki | = | 7.43 | nM | 8.13 |
| CHEMBL2112073 | — | Ki | = | 9.03 | nM | 8.04 |
| CHEMBL43234 | — | Ki | = | 9.27 | nM | 8.03 |
| CHEMBL43921 | — | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL40564 | — | Ki | = | 17.1 | nM | 7.77 |
| CHEMBL41332 | — | Ki | = | 38.1 | nM | 7.42 |
| CHEMBL41396 | — | Ki | = | 98.9 | nM | 7.00 |
| CHEMBL296711 | — | Ki | = | 153.0 | nM | 6.82 |