Assay Detail
Binding
CHEMBL617468
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ketanserin (0.5 nM) from rat cerebral cortex 5-hydroxytryptamine 2A receptors
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 30 | 7.23 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.70 |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 8.60 |
| CHEMBL328048 | — | — | 1 | 8.22 |
| CHEMBL98299 | — | — | 1 | 8.05 |
| CHEMBL330603 | — | — | 1 | 7.96 |
| CHEMBL97184 | — | — | 1 | 7.92 |
| CHEMBL330171 | — | — | 1 | 7.68 |
| CHEMBL318735 | — | — | 1 | 7.66 |
| CHEMBL97422 | — | — | 1 | 7.52 |
| CHEMBL421573 | — | — | 1 | 7.43 |
| CHEMBL94612 | — | — | 1 | 7.39 |
| CHEMBL328940 | — | — | 1 | 7.37 |
| CHEMBL97650 | — | — | 1 | 7.26 |
| CHEMBL319352 | — | — | 1 | 7.22 |
| CHEMBL318249 | — | — | 1 | 7.22 |
| CHEMBL318901 | — | — | 1 | 7.22 |
| CHEMBL97242 | — | — | 1 | 7.19 |
| CHEMBL328187 | — | — | 1 | 6.96 |
| CHEMBL98241 | — | — | 1 | 6.92 |
| CHEMBL329280 | — | — | 1 | 6.89 |
| CHEMBL93923 | — | — | 1 | 6.85 |
| CHEMBL327527 | — | — | 1 | 6.85 |
| CHEMBL327662 | — | — | 1 | 6.80 |
| CHEMBL95169 | — | — | 1 | 6.68 |
| CHEMBL95175 | — | — | 1 | 6.58 |
| CHEMBL97333 | — | — | 1 | 6.50 |
| CHEMBL317333 | — | — | 1 | 6.30 |
| CHEMBL313424 | — | — | 1 | 6.30 |
| CHEMBL420997 | — | — | 1 | 5.92 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL6437 | MIANSERIN | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL328048 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL98299 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL330603 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL97184 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL330171 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL318735 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL97422 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL421573 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL94612 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL328940 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL97650 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL319352 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL318249 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL318901 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL97242 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL328187 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL98241 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL329280 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL93923 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL327527 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL327662 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL95169 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL95175 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL97333 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL317333 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL313424 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL420997 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2 | PRAZOSIN | Ki | = | 1500.0 | nM | 5.82 |