Assay Detail
Binding
CHEMBL617246
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Displacement of [3H]ketanserin from 5-hydroxytryptamine 2 receptor in rat cortical membranes
48
Total Activities
39
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
Stereospecific and selective 5-HT2 antagonism in a series of 5-substituted trans-1-piperazino-3-phenylindans.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 8.11 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 9.40 |
| CHEMBL2112372 | — | — | 2 | 9.12 |
| CHEMBL1204307 | — | — | 2 | 9.02 |
| CHEMBL1744121 | — | — | 3 | 8.96 |
| CHEMBL1744113 | — | — | 2 | 8.96 |
| CHEMBL1744114 | — | — | 2 | 8.89 |
| CHEMBL1744112 | — | — | 1 | 8.82 |
| CHEMBL1788128 | — | — | 1 | 8.82 |
| CHEMBL1744107 | — | — | 1 | 8.82 |
| CHEMBL1744111 | — | — | 1 | 8.77 |
| CHEMBL422067 | — | — | 1 | 8.59 |
| CHEMBL1744120 | — | — | 1 | 8.59 |
| CHEMBL1744109 | — | — | 1 | 8.55 |
| CHEMBL96571 | — | — | 1 | 8.54 |
| CHEMBL1744115 | — | — | 1 | 8.52 |
| CHEMBL73461 | IRINDALONE | 2.0 | 1 | 8.47 |
| CHEMBL1744110 | — | — | 1 | 8.46 |
| CHEMBL1744117 | — | — | 1 | 8.43 |
| CHEMBL1744126 | — | — | 1 | 8.42 |
| CHEMBL92408 | — | — | 1 | 8.40 |
| CHEMBL1744124 | — | — | 1 | 8.25 |
| CHEMBL1744128 | — | — | 1 | 8.21 |
| CHEMBL1744122 | — | — | 1 | 8.19 |
| CHEMBL1744116 | — | — | 1 | 8.05 |
| CHEMBL1744125 | — | — | 1 | 8.00 |
| CHEMBL2447982 | — | — | 1 | 8.00 |
| CHEMBL1744119 | — | — | 1 | 8.00 |
| CHEMBL2111567 | — | — | 3 | 7.96 |
| CHEMBL1744108 | — | — | 1 | 7.96 |
| CHEMBL1204306 | — | — | 2 | 7.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267777 | RITANSERIN | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL2112372 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL1204307 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL1744113 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1744121 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1744114 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1744112 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1744107 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1788128 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1744111 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL422067 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1744120 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1744109 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL96571 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1744115 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL73461 | IRINDALONE | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL1744110 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1744117 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1744126 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL1744121 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL92408 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1744124 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL1744128 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL1744122 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL1744116 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL1744119 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL1744125 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2447982 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2111567 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1744108 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1744118 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1204306 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1788129 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1744105 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1744123 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL320684 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2112372 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2447981 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2111567 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1744106 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL92896 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1204307 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1744127 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1744113 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL1744121 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1744114 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2111567 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1204306 | — | IC50 | = | 500.0 | nM | 6.30 |