Assay Detail
Functional
CHEMBL858335
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Compound was evaluated for its activity at membrane-bound receptor (M+L+P fraction) from rat frontal cortex
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Frontal cortex |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.96 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18331 | PIRENPERONE | 2.0 | 1 | 8.74 |
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 8.62 |
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 8.58 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 8.46 |
| CHEMBL440294 | PIPAMPERONE | 3.0 | 1 | 8.27 |
| CHEMBL1065 | METHYSERGIDE | 4.0 | 1 | 8.13 |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 7.93 |
| CHEMBL1255588 | — | — | 1 | 7.88 |
| CHEMBL219916 | DOMPERIDONE | 3.0 | 1 | 6.23 |
| CHEMBL416526 | BUFOTENINE | — | 1 | 5.88 |
| CHEMBL25554 | — | — | 1 | 5.57 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 5.45 |
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | 5.40 |
| CHEMBL6066837 | (-)-BUTACLAMOL | — | 1 | 4.90 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 4.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18331 | PIRENPERONE | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL267930 | SPIPERONE | IC50 | = | 2.399 | nM | 8.62 |
| CHEMBL51 | KETANSERIN | IC50 | = | 2.63 | nM | 8.58 |
| CHEMBL267777 | RITANSERIN | IC50 | = | 3.467 | nM | 8.46 |
| CHEMBL440294 | PIPAMPERONE | IC50 | = | 5.37 | nM | 8.27 |
| CHEMBL1065 | METHYSERGIDE | IC50 | = | 7.413 | nM | 8.13 |
| CHEMBL6437 | MIANSERIN | IC50 | = | 11.75 | nM | 7.93 |
| CHEMBL1255588 | — | IC50 | = | 13.18 | nM | 7.88 |
| CHEMBL219916 | DOMPERIDONE | IC50 | = | 588.84 | nM | 6.23 |
| CHEMBL416526 | BUFOTENINE | IC50 | = | 1318.26 | nM | 5.88 |
| CHEMBL25554 | — | IC50 | = | 2691.53 | nM | 5.57 |
| CHEMBL39 | SEROTONIN | IC50 | = | 3548.13 | nM | 5.45 |
| CHEMBL511 | PYRILAMINE | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL6066837 | (-)-BUTACLAMOL | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL2 | PRAZOSIN | IC50 | = | 44668.36 | nM | 4.35 |