Assay Detail
Binding
CHEMBL3241203
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr by beta-counting
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Solid-supported synthesis, molecular modeling, and biological activity of long-chain arylpiperazine derivatives with cyclic amino acid amide fragments as 5-HT(7) and 5-HT(1A) receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 6.95 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3235745 | — | — | 1 | 8.70 |
| CHEMBL3235739 | — | — | 1 | 8.40 |
| CHEMBL3235748 | — | — | 1 | 7.92 |
| CHEMBL3235727 | — | — | 1 | 7.85 |
| CHEMBL3235756 | — | — | 1 | 7.80 |
| CHEMBL3235743 | — | — | 1 | 7.75 |
| CHEMBL3235728 | — | — | 1 | 7.64 |
| CHEMBL3235736 | — | — | 1 | 7.42 |
| CHEMBL3235731 | — | — | 1 | 7.36 |
| CHEMBL3235726 | — | — | 1 | 7.33 |
| CHEMBL225284 | — | — | 1 | 7.28 |
| CHEMBL3235733 | — | — | 1 | 7.28 |
| CHEMBL3235750 | — | — | 1 | 7.14 |
| CHEMBL3235749 | — | — | 1 | 7.11 |
| CHEMBL3235738 | — | — | 1 | 7.08 |
| CHEMBL3235760 | — | — | 1 | 7.05 |
| CHEMBL3235747 | — | — | 1 | 6.97 |
| CHEMBL3235742 | — | — | 1 | 6.91 |
| CHEMBL3235746 | — | — | 1 | 6.91 |
| CHEMBL3235735 | — | — | 1 | 6.85 |
| CHEMBL522691 | — | — | 1 | 6.73 |
| CHEMBL3235753 | — | — | 1 | 6.68 |
| CHEMBL3235730 | — | — | 1 | 6.67 |
| CHEMBL3235757 | — | — | 1 | 6.67 |
| CHEMBL3235741 | — | — | 1 | 6.67 |
| CHEMBL3235759 | — | — | 1 | 6.64 |
| CHEMBL3235734 | — | — | 1 | 6.63 |
| CHEMBL3235751 | — | — | 1 | 6.63 |
| CHEMBL3235729 | — | — | 1 | 6.50 |
| CHEMBL3235758 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3235745 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3235739 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3235748 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3235727 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3235756 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3235743 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3235728 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3235736 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL3235731 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL3235726 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL225284 | — | Ki | = | 52.7 | nM | 7.28 |
| CHEMBL3235733 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL3235750 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL3235749 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL3235738 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL3235760 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL3235747 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL3235746 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL3235742 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL3235735 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL522691 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL3235753 | — | Ki | = | 211.0 | nM | 6.68 |
| CHEMBL3235730 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL3235757 | — | Ki | = | 212.0 | nM | 6.67 |
| CHEMBL3235741 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL3235759 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL3235751 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL3235734 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL3235729 | — | Ki | = | 313.0 | nM | 6.50 |
| CHEMBL3235758 | — | Ki | = | 377.0 | nM | 6.42 |
| CHEMBL3235752 | — | Ki | = | 499.0 | nM | 6.30 |
| CHEMBL3235737 | — | Ki | = | 573.0 | nM | 6.24 |
| CHEMBL3235755 | — | Ki | = | 643.0 | nM | 6.19 |
| CHEMBL3235754 | — | Ki | = | 1914.0 | nM | 5.72 |
| CHEMBL3235740 | — | Ki | = | 2908.0 | nM | 5.54 |
| CHEMBL3235732 | — | Ki | = | 6307.0 | nM | 5.20 |
| CHEMBL3235744 | — | Ki | < | 1.0 | nM | - |