Assay Detail
Binding
CHEMBL617155
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Binding affinity against 5-hydroxytryptamine 2 receptor in rat brain using [3H]ketanserin as radioligand
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Serotonin 2 (5-HT2) receptor (CHEMBL2093870) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.09 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 8.47 |
| CHEMBL108942 | — | — | 1 | 6.87 |
| CHEMBL322275 | — | — | 1 | 6.64 |
| CHEMBL444590 | — | — | 1 | 6.60 |
| CHEMBL26929 | — | — | 1 | 6.48 |
| CHEMBL111760 | — | — | 1 | 6.46 |
| CHEMBL324637 | — | — | 1 | 6.37 |
| CHEMBL323242 | — | — | 1 | 6.14 |
| CHEMBL28063 | — | — | 1 | 6.08 |
| CHEMBL325565 | — | — | 1 | 6.07 |
| CHEMBL321184 | — | — | 1 | 5.97 |
| CHEMBL108858 | — | — | 1 | 5.92 |
| CHEMBL107503 | — | — | 1 | 5.90 |
| CHEMBL320587 | — | — | 1 | 5.81 |
| CHEMBL26426 | — | — | 1 | 5.77 |
| CHEMBL326017 | — | — | 1 | 5.76 |
| CHEMBL107921 | — | — | 1 | 5.72 |
| CHEMBL110968 | — | — | 1 | 5.69 |
| CHEMBL108241 | — | — | 1 | 5.59 |
| CHEMBL325079 | — | — | 1 | 5.57 |
| CHEMBL325092 | — | — | 1 | 5.57 |
| CHEMBL107486 | — | — | 1 | 5.48 |
| CHEMBL108245 | — | — | 1 | 5.04 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | - |
| CHEMBL109263 | — | — | 1 | - |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL51 | KETANSERIN | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL108942 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL322275 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL444590 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL26929 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL111760 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL324637 | — | IC50 | = | 428.0 | nM | 6.37 |
| CHEMBL323242 | — | IC50 | = | 726.0 | nM | 6.14 |
| CHEMBL28063 | — | IC50 | = | 841.0 | nM | 6.08 |
| CHEMBL325565 | — | IC50 | = | 848.0 | nM | 6.07 |
| CHEMBL321184 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL108858 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL107503 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL320587 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL26426 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL326017 | — | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL107921 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL110968 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL108241 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL325079 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL325092 | — | IC50 | = | 2720.0 | nM | 5.57 |
| CHEMBL107486 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL108245 | — | IC50 | = | 9140.0 | nM | 5.04 |
| CHEMBL56 | 8-OH-DPAT | IC50 | > | 10000.0 | nM | - |
| CHEMBL109263 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL49 | BUSPIRONE | IC50 | > | 10000.0 | nM | - |