Assay Detail
Binding
CHEMBL616981
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]spiperone binding to 5-hydroxytryptamine 2 receptor from rat cortical membranes
45
Total Activities
44
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
Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 7.51 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 8.77 |
| CHEMBL1237320 | — | — | 1 | 8.66 |
| CHEMBL1237325 | — | — | 1 | 8.54 |
| CHEMBL1237327 | — | — | 1 | 8.48 |
| CHEMBL1237321 | — | — | 1 | 8.48 |
| CHEMBL73461 | IRINDALONE | 2.0 | 2 | 8.47 |
| CHEMBL1237330 | — | — | 1 | 8.47 |
| CHEMBL267795 | — | — | 1 | 8.38 |
| CHEMBL1237338 | — | — | 1 | 8.37 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 8.36 |
| CHEMBL1237324 | — | — | 1 | 8.32 |
| CHEMBL1237323 | — | — | 1 | 8.32 |
| CHEMBL308157 | — | — | 1 | 8.31 |
| CHEMBL70887 | — | — | 1 | 8.31 |
| CHEMBL1237339 | — | — | 1 | 8.25 |
| CHEMBL431786 | — | — | 1 | 8.19 |
| CHEMBL1237332 | — | — | 1 | 8.12 |
| CHEMBL307717 | — | — | 1 | 8.11 |
| CHEMBL95636 | TEFLUDAZINE | 2.0 | 1 | 8.08 |
| CHEMBL1237331 | — | — | 1 | 8.03 |
| CHEMBL306960 | — | — | 1 | 8.00 |
| CHEMBL1237334 | — | — | 1 | 7.96 |
| CHEMBL1237343 | — | — | 1 | 7.92 |
| CHEMBL1237335 | — | — | 1 | 7.92 |
| CHEMBL1237319 | — | — | 1 | 7.89 |
| CHEMBL1237326 | — | — | 1 | 7.75 |
| CHEMBL1237333 | — | — | 1 | 7.66 |
| CHEMBL76004 | — | — | 1 | 7.52 |
| CHEMBL1237341 | — | — | 1 | 7.43 |
| CHEMBL305905 | — | — | 1 | 7.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL51 | KETANSERIN | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1237320 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1237325 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1237327 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL1237321 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL73461 | IRINDALONE | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL1237330 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL267795 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL1237338 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL267777 | RITANSERIN | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL1237324 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL1237323 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL308157 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL70887 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL1237339 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL431786 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1237332 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL307717 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL95636 | TEFLUDAZINE | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL1237331 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL306960 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1237334 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1237343 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1237335 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1237319 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1237326 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1237333 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL76004 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1237341 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL305905 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1237322 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL308123 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1237329 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1237336 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL306939 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1237337 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1237328 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL308076 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL73461 | IRINDALONE | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL1237344 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL307465 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL312285 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL2 | PRAZOSIN | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL72644 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL74759 | — | IC50 | > | 1000.0 | nM | - |