Assay Detail
Binding
CHEMBL652742
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to displace [3H]prazosin (0.25 nM) from whole brain of rat alpha-1 adrenergic receptor
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 8.34 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.54 |
| CHEMBL98299 | — | — | 1 | 9.35 |
| CHEMBL97422 | — | — | 1 | 9.00 |
| CHEMBL97184 | — | — | 1 | 8.92 |
| CHEMBL97698 | — | — | 1 | 8.92 |
| CHEMBL318735 | — | — | 1 | 8.92 |
| CHEMBL330603 | — | — | 1 | 8.89 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 8.85 |
| CHEMBL328940 | — | — | 1 | 8.77 |
| CHEMBL319352 | — | — | 1 | 8.74 |
| CHEMBL421573 | — | — | 1 | 8.70 |
| CHEMBL327527 | — | — | 1 | 8.60 |
| CHEMBL97242 | — | — | 1 | 8.59 |
| CHEMBL328048 | — | — | 1 | 8.54 |
| CHEMBL97650 | — | — | 1 | 8.49 |
| CHEMBL93923 | — | — | 1 | 8.43 |
| CHEMBL330171 | — | — | 1 | 8.36 |
| CHEMBL94612 | — | — | 1 | 8.28 |
| CHEMBL313424 | — | — | 1 | 8.28 |
| CHEMBL317333 | — | — | 1 | 8.24 |
| CHEMBL97333 | — | — | 1 | 8.20 |
| CHEMBL420997 | — | — | 1 | 8.20 |
| CHEMBL327662 | — | — | 1 | 8.17 |
| CHEMBL328187 | — | — | 1 | 8.02 |
| CHEMBL318249 | — | — | 1 | 7.96 |
| CHEMBL318901 | — | — | 1 | 7.89 |
| CHEMBL95175 | — | — | 1 | 7.85 |
| CHEMBL329280 | — | — | 1 | 7.66 |
| CHEMBL95169 | — | — | 1 | 7.20 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL98299 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL97422 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL97184 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL97698 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL318735 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL330603 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL12713 | SERTINDOLE | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL328940 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL319352 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL421573 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL327527 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL97242 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL328048 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL97650 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL93923 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL330171 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL94612 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL313424 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL317333 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL97333 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL420997 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL327662 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL328187 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL318249 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL318901 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL95175 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL329280 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL95169 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL98241 | — | Ki | = | 840.0 | nM | 6.08 |