Assay Detail
Binding
CHEMBL643628
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Inhibition of [3H]prazosin binding to alpha-1 adrenergic receptor from rat cortical membranes
33
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
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 | 33 | 7.35 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.44 |
| CHEMBL1237325 | — | — | 1 | 8.28 |
| CHEMBL1237330 | — | — | 1 | 8.26 |
| CHEMBL70887 | — | — | 1 | 8.03 |
| CHEMBL1237338 | — | — | 1 | 8.00 |
| CHEMBL1237327 | — | — | 1 | 7.96 |
| CHEMBL306960 | — | — | 1 | 7.96 |
| CHEMBL1237339 | — | — | 1 | 7.92 |
| CHEMBL1237320 | — | — | 1 | 7.89 |
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 7.82 |
| CHEMBL95636 | TEFLUDAZINE | 2.0 | 1 | 7.77 |
| CHEMBL307717 | — | — | 1 | 7.66 |
| CHEMBL431786 | — | — | 1 | 7.62 |
| CHEMBL73461 | IRINDALONE | 2.0 | 2 | 7.58 |
| CHEMBL1237324 | — | — | 1 | 7.55 |
| CHEMBL267795 | — | — | 1 | 7.48 |
| CHEMBL1237323 | — | — | 1 | 7.47 |
| CHEMBL1237343 | — | — | 1 | 7.44 |
| CHEMBL1237326 | — | — | 1 | 7.43 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 7.33 |
| CHEMBL308123 | — | — | 1 | 7.21 |
| CHEMBL305905 | — | — | 1 | 7.07 |
| CHEMBL76004 | — | — | 1 | 7.00 |
| CHEMBL1237331 | — | — | 1 | 6.80 |
| CHEMBL1237344 | — | — | 1 | 6.27 |
| CHEMBL1237336 | — | — | 1 | 6.27 |
| CHEMBL1237337 | — | — | 1 | 6.25 |
| CHEMBL1237328 | — | — | 1 | 6.05 |
| CHEMBL308076 | — | — | 1 | 5.89 |
| CHEMBL306939 | — | — | 1 | 5.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL1237325 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL1237330 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL70887 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL1237338 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1237327 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL306960 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1237339 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1237320 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL51 | KETANSERIN | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL95636 | TEFLUDAZINE | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL307717 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL431786 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL73461 | IRINDALONE | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1237324 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL267795 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1237323 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1237343 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1237326 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL267777 | RITANSERIN | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL308123 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL305905 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL76004 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1237331 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1237344 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL1237336 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL1237337 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL73461 | IRINDALONE | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL1237328 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL308076 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL306939 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL74759 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1237332 | — | IC50 | - | nM | - |