Assay Detail
Binding
CHEMBL617247
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Tested for 5-hydroxytryptamine 2 receptor binding ability by displacement of [3H]spiperone from rat brain frontal cortex synaptosomes
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Serotonin 2 (5-HT2) receptor (CHEMBL2093870) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Synthesis and 5-hydroxytryptamine antagonist activity of 2-[[2-(dimethylamino)ethyl]thio]-3-phenylquinoline and its analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 61 | 6.52 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 8.30 |
| CHEMBL1065 | METHYSERGIDE | 4.0 | 1 | 8.30 |
| CHEMBL542644 | — | — | 1 | 7.50 |
| CHEMBL419628 | — | — | 1 | 7.40 |
| CHEMBL544062 | — | — | 1 | 7.30 |
| CHEMBL545701 | — | — | 1 | 7.20 |
| CHEMBL419444 | — | — | 1 | 7.20 |
| CHEMBL544061 | — | — | 1 | 7.20 |
| CHEMBL555008 | — | — | 1 | 7.20 |
| CHEMBL542151 | — | — | 1 | 7.10 |
| CHEMBL543825 | — | — | 1 | 7.10 |
| CHEMBL305907 | — | — | 1 | 7.00 |
| CHEMBL553289 | — | — | 1 | 6.90 |
| CHEMBL544998 | — | — | 1 | 6.90 |
| CHEMBL543112 | — | — | 1 | 6.90 |
| CHEMBL543824 | — | — | 1 | 6.90 |
| CHEMBL545696 | — | — | 1 | 6.80 |
| CHEMBL76109 | — | — | 1 | 6.80 |
| CHEMBL553501 | — | — | 1 | 6.80 |
| CHEMBL552901 | — | — | 1 | 6.80 |
| CHEMBL73165 | — | — | 1 | 6.80 |
| CHEMBL73124 | — | — | 1 | 6.80 |
| CHEMBL544531 | — | — | 1 | 6.80 |
| CHEMBL544060 | — | — | 1 | 6.70 |
| CHEMBL544999 | — | — | 1 | 6.70 |
| CHEMBL305663 | — | — | 1 | 6.70 |
| CHEMBL72420 | — | — | 1 | 6.70 |
| CHEMBL543831 | — | — | 1 | 6.70 |
| CHEMBL306411 | — | — | 1 | 6.60 |
| CHEMBL539014 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL51 | KETANSERIN | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL1065 | METHYSERGIDE | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL542644 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL419628 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL544062 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL545701 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL419444 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL544061 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL555008 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL542151 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL543825 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL305907 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL544998 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL553289 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL543112 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL543824 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL545696 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL76109 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL553501 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL552901 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL73165 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL73124 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL544531 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL543831 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL72420 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL305663 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL544060 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL544999 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL306411 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL539014 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL73081 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL309181 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL544293 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL73166 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL544294 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL543350 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL542401 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL73659 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL75931 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL541554 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL75999 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL543114 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL543347 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL76227 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL310155 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL311130 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL420930 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL72656 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL73422 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL307590 | — | IC50 | = | 1258.93 | nM | 5.90 |