Assay Detail
Binding
CHEMBL615805
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Ability to displace [3H]5-CT (2.0 nM) from HeLa cells of human 5-hydroxytryptamine 1A receptor
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HeLa |
| 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 | 29 | 7.41 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL93240 | METITEPINE | 2.0 | 1 | 8.66 |
| CHEMBL318735 | — | — | 1 | 8.48 |
| CHEMBL328048 | — | — | 1 | 8.24 |
| CHEMBL98299 | — | — | 1 | 7.96 |
| CHEMBL421573 | — | — | 1 | 7.92 |
| CHEMBL94612 | — | — | 1 | 7.89 |
| CHEMBL97184 | — | — | 1 | 7.75 |
| CHEMBL327527 | — | — | 1 | 7.62 |
| CHEMBL313424 | — | — | 1 | 7.60 |
| CHEMBL328187 | — | — | 1 | 7.54 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 7.48 |
| CHEMBL93923 | — | — | 1 | 7.48 |
| CHEMBL97650 | — | — | 1 | 7.46 |
| CHEMBL327662 | — | — | 1 | 7.40 |
| CHEMBL97422 | — | — | 1 | 7.35 |
| CHEMBL95175 | — | — | 1 | 7.33 |
| CHEMBL329280 | — | — | 1 | 7.31 |
| CHEMBL97242 | — | — | 1 | 7.31 |
| CHEMBL330603 | — | — | 1 | 7.29 |
| CHEMBL318901 | — | — | 1 | 7.26 |
| CHEMBL97333 | — | — | 1 | 7.19 |
| CHEMBL317333 | — | — | 1 | 7.17 |
| CHEMBL319352 | — | — | 1 | 6.89 |
| CHEMBL420997 | — | — | 1 | 6.80 |
| CHEMBL318249 | — | — | 1 | 6.63 |
| CHEMBL330171 | — | — | 1 | 6.56 |
| CHEMBL328940 | — | — | 1 | 6.54 |
| CHEMBL98241 | — | — | 1 | 6.31 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL93240 | METITEPINE | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL318735 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL328048 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL98299 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL421573 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL94612 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL97184 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL327527 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL313424 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL328187 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL12713 | SERTINDOLE | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL93923 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL97650 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL327662 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL97422 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL95175 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL329280 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL97242 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL330603 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL318901 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL97333 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL317333 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL319352 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL420997 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL318249 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL330171 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL328940 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL98241 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL2 | PRAZOSIN | Ki | > | 1800.0 | nM | - |