Assay Detail
Binding
CHEMBL616977
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In vitro binding affinity measured on serotonin 5-hydroxytryptamine 2 receptor using [3H]ketanserin as radioligand.
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Serotonin 2 (5-HT2) receptor (CHEMBL2093870) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.59 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 8.92 |
| CHEMBL172556 | — | — | 1 | 6.96 |
| CHEMBL143110 | — | — | 1 | 6.92 |
| CHEMBL277302 | — | — | 1 | 6.84 |
| CHEMBL174300 | — | — | 1 | 6.83 |
| CHEMBL174083 | — | — | 1 | 6.83 |
| CHEMBL368477 | — | — | 1 | 6.81 |
| CHEMBL322275 | — | — | 1 | 6.77 |
| CHEMBL175300 | — | — | 1 | 6.69 |
| CHEMBL148055 | — | — | 1 | 6.69 |
| CHEMBL366459 | — | — | 1 | 6.68 |
| CHEMBL424125 | — | — | 1 | 6.66 |
| CHEMBL171181 | — | — | 1 | 6.54 |
| CHEMBL444590 | — | — | 1 | 6.48 |
| CHEMBL172363 | — | — | 1 | 6.48 |
| CHEMBL26929 | — | — | 1 | 6.45 |
| CHEMBL367723 | — | — | 1 | 6.41 |
| CHEMBL367435 | — | — | 1 | 6.41 |
| CHEMBL140406 | — | — | 1 | 6.38 |
| CHEMBL173190 | — | — | 1 | 6.18 |
| CHEMBL172161 | — | — | 1 | 6.11 |
| CHEMBL433972 | — | — | 1 | 5.93 |
| CHEMBL171974 | — | — | 1 | 5.62 |
| CHEMBL108241 | — | — | 1 | 5.48 |
| CHEMBL176819 | — | — | 1 | - |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | - |
| CHEMBL174703 | — | — | 1 | - |
| CHEMBL174554 | — | — | 1 | - |
| CHEMBL28209 | — | — | 1 | - |
| CHEMBL172601 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL51 | KETANSERIN | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL172556 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL143110 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL277302 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL174300 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL174083 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL368477 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL322275 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL175300 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL148055 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL366459 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL424125 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL171181 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL444590 | — | IC50 | = | 331.0 | nM | 6.48 |
| CHEMBL172363 | — | IC50 | = | 329.0 | nM | 6.48 |
| CHEMBL26929 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL367723 | — | IC50 | = | 391.0 | nM | 6.41 |
| CHEMBL367435 | — | IC50 | = | 391.0 | nM | 6.41 |
| CHEMBL140406 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL173190 | — | IC50 | = | 667.0 | nM | 6.18 |
| CHEMBL172161 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL433972 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL171974 | — | IC50 | = | 2370.0 | nM | 5.62 |
| CHEMBL108241 | — | IC50 | = | 3340.0 | nM | 5.48 |
| CHEMBL176819 | — | IC50 | - | — | - | |
| CHEMBL49 | BUSPIRONE | IC50 | > | 10.0 | nM | - |
| CHEMBL174703 | — | IC50 | - | — | - | |
| CHEMBL174554 | — | IC50 | - | — | - | |
| CHEMBL28209 | — | IC50 | - | — | - | |
| CHEMBL172601 | — | IC50 | - | — | - | |
| CHEMBL425134 | — | IC50 | - | — | - |