Assay Detail
Binding
CHEMBL884529
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ketanserin from 5-hydroxytryptamine 2 receptor from rat cortical membranes.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Serotonin 2 (5-HT2) receptor (CHEMBL2093870) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 8.51 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.41 |
| CHEMBL423024 | — | — | 1 | 9.23 |
| CHEMBL344276 | — | — | 1 | 9.14 |
| CHEMBL12780 | — | — | 1 | 9.14 |
| CHEMBL144086 | — | — | 1 | 9.09 |
| CHEMBL422840 | — | — | 1 | 8.96 |
| CHEMBL422480 | — | — | 1 | 8.89 |
| CHEMBL359046 | — | — | 1 | 8.89 |
| CHEMBL423009 | — | — | 1 | 8.85 |
| CHEMBL331545 | — | — | 1 | 8.82 |
| CHEMBL144457 | — | — | 1 | 8.80 |
| CHEMBL144325 | — | — | 1 | 8.80 |
| CHEMBL341669 | — | — | 1 | 8.77 |
| CHEMBL144951 | — | — | 1 | 8.74 |
| CHEMBL343899 | — | — | 1 | 8.70 |
| CHEMBL144252 | — | — | 1 | 8.66 |
| CHEMBL357186 | — | — | 1 | 8.60 |
| CHEMBL342104 | — | — | 1 | 8.59 |
| CHEMBL144184 | — | — | 1 | 8.54 |
| CHEMBL145706 | — | — | 1 | 8.43 |
| CHEMBL145763 | — | — | 1 | 8.35 |
| CHEMBL144165 | — | — | 1 | 8.22 |
| CHEMBL358994 | — | — | 1 | 7.96 |
| CHEMBL142908 | — | — | 1 | 7.80 |
| CHEMBL143782 | — | — | 1 | 7.75 |
| CHEMBL145460 | — | — | 1 | 7.22 |
| CHEMBL357178 | — | — | 1 | 7.18 |
| CHEMBL356320 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL423024 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL344276 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL12780 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL144086 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL422840 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL422480 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL359046 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL423009 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL331545 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL144457 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL144325 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL341669 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL144951 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL343899 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL144252 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL357186 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL342104 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL144184 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL145706 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL145763 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL144165 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL358994 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL142908 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL143782 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL145460 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL357178 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL356320 | — | IC50 | = | 150.0 | nM | 6.82 |