Assay Detail
Binding
CHEMBL617842
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]mesulergine (0.5 nM) from rat 5-hydroxytryptamine 2C receptor expressed in SR-3T3 cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | SR-3T3 |
| 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 | 21 | 6.81 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12314 | MESULERGINE | 2.0 | 1 | 9.43 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.29 |
| CHEMBL330171 | — | — | 1 | 7.43 |
| CHEMBL328048 | — | — | 1 | 7.35 |
| CHEMBL94612 | — | — | 1 | 7.30 |
| CHEMBL328940 | — | — | 1 | 7.14 |
| CHEMBL97650 | — | — | 1 | 6.92 |
| CHEMBL318735 | — | — | 1 | 6.89 |
| CHEMBL97184 | — | — | 1 | 6.85 |
| CHEMBL97422 | — | — | 1 | 6.82 |
| CHEMBL330603 | — | — | 1 | 6.75 |
| CHEMBL98299 | — | — | 1 | 6.72 |
| CHEMBL319352 | — | — | 1 | 6.48 |
| CHEMBL93923 | — | — | 1 | 6.48 |
| CHEMBL318249 | — | — | 1 | 6.30 |
| CHEMBL329280 | — | — | 1 | 6.00 |
| CHEMBL327662 | — | — | 1 | 5.96 |
| CHEMBL421573 | — | — | 1 | 5.92 |
| CHEMBL328187 | — | — | 1 | 5.82 |
| CHEMBL98241 | — | — | 1 | 5.58 |
| CHEMBL327527 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12314 | MESULERGINE | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL330171 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL328048 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL94612 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL328940 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL97650 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL318735 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL97184 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL97422 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL330603 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL98299 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL319352 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL93923 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL318249 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL329280 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL327662 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL421573 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL328187 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL98241 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL327527 | — | Ki | = | 2900.0 | nM | 5.54 |