Assay Detail
Binding
CHEMBL644948
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The concentration required to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat brain membranes was measured (in vitro)
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.09 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440134 | — | — | 1 | 8.11 |
| CHEMBL84087 | — | — | 1 | 8.10 |
| CHEMBL83664 | — | — | 1 | 8.00 |
| CHEMBL418929 | — | — | 1 | 7.57 |
| CHEMBL309660 | — | — | 1 | 7.46 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 7.43 |
| CHEMBL84346 | — | — | 1 | 7.30 |
| CHEMBL83975 | — | — | 1 | 7.28 |
| CHEMBL82229 | — | — | 1 | 7.19 |
| CHEMBL79927 | — | — | 1 | 7.12 |
| CHEMBL79598 | — | — | 1 | 7.12 |
| CHEMBL310105 | — | — | 1 | 7.01 |
| CHEMBL83894 | FANANSERIN | 2.0 | 1 | 6.99 |
| CHEMBL79375 | — | — | 1 | 6.96 |
| CHEMBL82651 | — | — | 1 | 6.85 |
| CHEMBL418911 | — | — | 1 | 6.84 |
| CHEMBL309408 | — | — | 1 | 6.74 |
| CHEMBL83787 | — | — | 1 | 6.72 |
| CHEMBL316227 | — | — | 1 | 6.57 |
| CHEMBL442185 | — | — | 1 | 6.24 |
| CHEMBL415272 | — | — | 1 | 6.16 |
| CHEMBL84465 | — | — | 1 | 6.16 |
| CHEMBL311550 | — | — | 1 | - |
| CHEMBL82167 | — | — | 1 | - |
| CHEMBL83035 | — | — | 1 | - |
| CHEMBL83780 | — | — | 1 | - |
| CHEMBL84077 | — | — | 1 | - |
| CHEMBL81813 | — | — | 1 | - |
| CHEMBL312043 | — | — | 1 | - |
| CHEMBL79420 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440134 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL84087 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL83664 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL418929 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL309660 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL267777 | RITANSERIN | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL84346 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL83975 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL82229 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL79927 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL79598 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL310105 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL83894 | FANANSERIN | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL79375 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL82651 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL418911 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL309408 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL83787 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL316227 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL442185 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL415272 | — | IC50 | = | 688.0 | nM | 6.16 |
| CHEMBL84465 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL311550 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL82167 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL83035 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL83780 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL84077 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL81813 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL312043 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL79420 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL83391 | — | IC50 | > | 1000.0 | nM | - |