Assay Detail
Binding
CHEMBL1948477
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Displacement of [3H]-OH-DPAT from human recombinant 5HT1A receptor expressed in HeLa cells after 30 mins by liquid scintillation counting
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.65 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1946786 | — | — | 1 | 9.49 |
| CHEMBL514874 | — | — | 1 | 9.48 |
| CHEMBL1946787 | — | — | 1 | 9.25 |
| CHEMBL286003 | — | — | 1 | 9.22 |
| CHEMBL1946788 | — | — | 1 | 9.10 |
| CHEMBL1946779 | — | — | 1 | 9.08 |
| CHEMBL13647 | BMY-7378 | — | 1 | 8.90 |
| CHEMBL1946778 | — | — | 1 | 8.70 |
| CHEMBL1946782 | — | — | 1 | 8.46 |
| CHEMBL1946783 | — | — | 1 | 8.46 |
| CHEMBL37883 | — | — | 1 | 8.45 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 8.43 |
| CHEMBL1946780 | — | — | 1 | 8.36 |
| CHEMBL1946784 | — | — | 1 | 8.03 |
| CHEMBL1946785 | — | — | 1 | 8.02 |
| CHEMBL1946781 | — | — | 1 | 7.98 |
| CHEMBL1946777 | — | — | 1 | 7.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1946786 | — | Ki | = | 0.3236 | nM | 9.49 |
| CHEMBL514874 | — | Ki | = | 0.3311 | nM | 9.48 |
| CHEMBL1946787 | — | Ki | = | 0.5623 | nM | 9.25 |
| CHEMBL286003 | — | Ki | = | 0.6026 | nM | 9.22 |
| CHEMBL1946788 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL1946779 | — | Ki | = | 0.8318 | nM | 9.08 |
| CHEMBL13647 | BMY-7378 | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL1946778 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL1946782 | — | Ki | = | 3.467 | nM | 8.46 |
| CHEMBL1946783 | — | Ki | = | 3.467 | nM | 8.46 |
| CHEMBL37883 | — | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL56 | 8-OH-DPAT | Ki | = | 3.715 | nM | 8.43 |
| CHEMBL1946780 | — | Ki | = | 4.365 | nM | 8.36 |
| CHEMBL1946784 | — | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL1946785 | — | Ki | = | 9.55 | nM | 8.02 |
| CHEMBL1946781 | — | Ki | = | 10.47 | nM | 7.98 |
| CHEMBL1946777 | — | Ki | = | 22.91 | nM | 7.64 |