Assay Detail
Binding
CHEMBL617444
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Binding affinity to rat cortical membranes at 5-hydroxytryptamine 2 (5-HT2) receptor using [3H]KET as a radioligand
43
Total Activities
42
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
Central serotonin receptors as targets for drug research.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 6.53 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19215 | METERGOLINE | 2.0 | 1 | 9.52 |
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 9.30 |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 8.85 |
| CHEMBL12314 | MESULERGINE | 2.0 | 1 | 8.70 |
| CHEMBL18786 | CINANSERIN | 2.0 | 1 | 8.40 |
| CHEMBL134519 | — | — | 2 | 8.00 |
| CHEMBL69700 | — | — | 1 | 7.62 |
| CHEMBL1434583 | — | — | 1 | 7.46 |
| CHEMBL6607 | BROLAMFETAMINE | 2.0 | 1 | 7.39 |
| CHEMBL317634 | — | — | 1 | 7.22 |
| CHEMBL8569 | — | — | 1 | 7.16 |
| CHEMBL8600 | DOM | — | 1 | 7.00 |
| CHEMBL8224 | — | — | 1 | 7.00 |
| CHEMBL275854 | — | — | 1 | 6.90 |
| CHEMBL468880 | — | — | 1 | 6.84 |
| CHEMBL277362 | — | — | 1 | 6.75 |
| CHEMBL1788278 | — | — | 1 | 6.68 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 6.64 |
| CHEMBL1788248 | — | — | 1 | 6.58 |
| CHEMBL8301 | — | — | 1 | 6.52 |
| CHEMBL416526 | BUFOTENINE | — | 1 | 6.42 |
| CHEMBL7257 | MEBUFOTENIN | 2.0 | 1 | 6.41 |
| CHEMBL19044 | — | — | 1 | 6.38 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 6.25 |
| CHEMBL18855 | — | — | 1 | 6.14 |
| CHEMBL18785 | RU-24969 | — | 1 | 6.11 |
| CHEMBL267526 | — | — | 1 | 5.96 |
| CHEMBL8389 | — | — | 1 | 5.78 |
| CHEMBL18762 | — | — | 1 | 5.71 |
| CHEMBL8165 | 5-METHOXYTRYPTAMINE | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19215 | METERGOLINE | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL267930 | SPIPERONE | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL6437 | MIANSERIN | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL12314 | MESULERGINE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL18786 | CINANSERIN | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL134519 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL134519 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL69700 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL1434583 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL6607 | BROLAMFETAMINE | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL317634 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL8569 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL8600 | DOM | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL8224 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL275854 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL468880 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL277362 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL1788278 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL18772 | QUIPAZINE | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL1788248 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL8301 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL416526 | BUFOTENINE | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL7257 | MEBUFOTENIN | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL19044 | — | Ki | = | 415.0 | nM | 6.38 |
| CHEMBL39 | SEROTONIN | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL18855 | — | Ki | = | 725.0 | nM | 6.14 |
| CHEMBL18785 | RU-24969 | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL267526 | — | Ki | = | 1110.0 | nM | 5.96 |
| CHEMBL8389 | — | Ki | = | 1650.0 | nM | 5.78 |
| CHEMBL18762 | — | Ki | = | 1930.0 | nM | 5.71 |
| CHEMBL8165 | 5-METHOXYTRYPTAMINE | Ki | = | 2570.0 | nM | 5.59 |
| CHEMBL6640 | TRYPTAMINE | Ki | = | 2895.0 | nM | 5.54 |
| CHEMBL1927025 | — | Ki | = | 3420.0 | nM | 5.47 |
| CHEMBL8642 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL56 | 8-OH-DPAT | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL452861 | LEVOPROPRANOLOL | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL16247 | — | Ki | = | 7850.0 | nM | 5.11 |
| CHEMBL16451 | — | Ki | = | 8130.0 | nM | 5.09 |
| CHEMBL19264 | — | Ki | = | 11500.0 | nM | 4.94 |
| CHEMBL278663 | PARA-METHOXYAMPHETAMINE | Ki | = | 33600.0 | nM | 4.47 |
| CHEMBL405 | AMPHETAMINE | Ki | = | 43000.0 | nM | 4.37 |
| CHEMBL277540 | — | Ki | = | 43300.0 | nM | 4.36 |
| CHEMBL500 | PINDOLOL | Ki | = | 200000.0 | nM | - |