Assay Detail
Binding
CHEMBL617600
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Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Serotonin 5-HT2 receptor, dopamine D2 receptor, and alpha 1 adrenoceptor antagonists. Conformationally flexible analogues of the atypical antipsychotic sertindole.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 8.03 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.41 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 9.40 |
| CHEMBL421244 | — | — | 1 | 9.06 |
| CHEMBL122269 | — | — | 1 | 9.02 |
| CHEMBL341229 | — | — | 1 | 9.00 |
| CHEMBL331545 | — | — | 1 | 8.82 |
| CHEMBL332425 | — | — | 1 | 8.72 |
| CHEMBL333774 | — | — | 1 | 8.70 |
| CHEMBL125483 | — | — | 1 | 8.38 |
| CHEMBL122113 | — | — | 1 | 8.28 |
| CHEMBL123640 | — | — | 1 | 8.26 |
| CHEMBL331193 | — | — | 1 | 8.24 |
| CHEMBL125291 | — | — | 1 | 8.23 |
| CHEMBL122047 | — | — | 1 | 8.20 |
| CHEMBL122042 | — | — | 1 | 8.11 |
| CHEMBL332365 | — | — | 1 | 8.05 |
| CHEMBL301956 | — | — | 1 | 7.92 |
| CHEMBL339919 | — | — | 1 | 7.77 |
| CHEMBL421239 | — | — | 1 | 7.75 |
| CHEMBL123094 | — | — | 1 | 7.72 |
| CHEMBL122018 | — | — | 1 | 7.70 |
| CHEMBL332077 | — | — | 1 | 7.57 |
| CHEMBL123027 | — | — | 1 | 7.38 |
| CHEMBL332913 | — | — | 1 | 7.32 |
| CHEMBL20734 | NEMONAPRIDE | 2.0 | 1 | 7.31 |
| CHEMBL125072 | — | — | 1 | 7.07 |
| CHEMBL122384 | — | — | 1 | 7.00 |
| CHEMBL123584 | — | — | 1 | 7.00 |
| CHEMBL332385 | — | — | 1 | 6.96 |
| CHEMBL338022 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL267777 | RITANSERIN | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL421244 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL122269 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL341229 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL331545 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL332425 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL333774 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL125483 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL122113 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL123640 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL331193 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL125291 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL122047 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL122042 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL332365 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL301956 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL339919 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL421239 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL123094 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL122018 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL332077 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL123027 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL332913 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL20734 | NEMONAPRIDE | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL125072 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL122384 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL123584 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL332385 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL338022 | — | IC50 | = | 220.0 | nM | 6.66 |