Assay Detail
Binding
CHEMBL617601
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Binding affinity towards rat 5-hydroxytryptamine 2A receptor was evaluated using [3H]- ketanserin as radioligand
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.86 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 8.47 |
| CHEMBL144417 | — | — | 1 | 7.92 |
| CHEMBL357176 | — | — | 1 | 7.25 |
| CHEMBL143728 | — | — | 1 | 7.07 |
| CHEMBL342518 | — | — | 1 | 6.97 |
| CHEMBL143110 | — | — | 1 | 6.92 |
| CHEMBL343432 | — | — | 1 | 6.80 |
| CHEMBL147678 | — | — | 1 | 6.80 |
| CHEMBL148055 | — | — | 1 | 6.69 |
| CHEMBL144445 | — | — | 1 | 6.64 |
| CHEMBL322275 | — | — | 1 | 6.64 |
| CHEMBL147387 | — | — | 1 | 6.62 |
| CHEMBL444590 | — | — | 1 | 6.60 |
| CHEMBL26929 | — | — | 1 | 6.48 |
| CHEMBL341893 | — | — | 1 | 6.38 |
| CHEMBL147440 | — | — | 1 | 6.24 |
| CHEMBL145432 | — | — | 1 | 6.21 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | - |
| CHEMBL56 | 8-OH-DPAT | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL51 | KETANSERIN | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL144417 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL357176 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL143728 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL342518 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL143110 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL343432 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL147678 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL148055 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL144445 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL322275 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL147387 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL444590 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL26929 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL341893 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL147440 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL145432 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL49 | BUSPIRONE | IC50 | > | 10000.0 | nM | - |
| CHEMBL56 | 8-OH-DPAT | IC50 | > | 10000.0 | nM | - |