Assay Detail
Binding
CHEMBL652741
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Ability to displace [3H]-prazosin binding to rat cortical membranes expressing Alpha-1 adrenergic receptors
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.78 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296512 | — | — | 1 | 8.96 |
| CHEMBL496860 | — | — | 1 | 8.68 |
| CHEMBL497054 | — | — | 1 | 8.55 |
| CHEMBL523245 | — | — | 1 | 8.54 |
| CHEMBL2368734 | — | — | 1 | 8.44 |
| CHEMBL504699 | — | — | 1 | 8.42 |
| CHEMBL497064 | — | — | 1 | 8.41 |
| CHEMBL523585 | — | — | 1 | 8.17 |
| CHEMBL507727 | — | — | 1 | 8.14 |
| CHEMBL523760 | — | — | 1 | 8.14 |
| CHEMBL496687 | — | — | 1 | 8.07 |
| CHEMBL498048 | — | — | 1 | 7.80 |
| CHEMBL507898 | — | — | 1 | 7.68 |
| CHEMBL42557 | — | — | 1 | 7.68 |
| CHEMBL497877 | — | — | 1 | 7.60 |
| CHEMBL40584 | — | — | 1 | 7.60 |
| CHEMBL498729 | — | — | 1 | 7.57 |
| CHEMBL43819 | — | — | 1 | 7.52 |
| CHEMBL496852 | — | — | 1 | 7.40 |
| CHEMBL46523 | — | — | 1 | 7.33 |
| CHEMBL43697 | — | — | 1 | 7.00 |
| CHEMBL497878 | — | — | 1 | 6.68 |
| CHEMBL2113667 | — | — | 1 | 6.60 |
| CHEMBL295559 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296512 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL496860 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL497054 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL523245 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL2368734 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL504699 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL497064 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL523585 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL507727 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL523760 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL496687 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL498048 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL507898 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL42557 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL497877 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL40584 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL498729 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL43819 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL496852 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL46523 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL43697 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL497878 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL2113667 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL295559 | — | Ki | = | 2100.0 | nM | 5.68 |