Assay Detail
Binding
CHEMBL3877019
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-8-OH-DPAT from recombinant human 5-HT1A receptor expressed in CHOK1 cell membranes after 1 hr by liquid scintillation counting method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New N- and O-arylpiperazinylalkyl pyrimidines and 2-methylquinazolines derivatives as 5-HT7 and 5-HT1A receptor ligands: Synthesis, structure-activity relationships, and molecular modeling studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.30 | 8.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56 | 8-OH-DPAT | — | 1 | 8.58 |
| CHEMBL3884095 | — | — | 1 | 8.52 |
| CHEMBL3883640 | — | — | 1 | 8.16 |
| CHEMBL3883542 | — | — | 1 | 8.09 |
| CHEMBL3884714 | — | — | 1 | 7.76 |
| CHEMBL3884584 | — | — | 1 | 7.75 |
| CHEMBL3885389 | — | — | 1 | 7.73 |
| CHEMBL3883517 | — | — | 1 | 7.61 |
| CHEMBL3884778 | — | — | 1 | 7.59 |
| CHEMBL3885319 | — | — | 1 | 7.47 |
| CHEMBL3883995 | — | — | 1 | 7.28 |
| CHEMBL3885282 | — | — | 1 | 7.04 |
| CHEMBL3885178 | — | — | 1 | 7.00 |
| CHEMBL3884137 | — | — | 1 | 6.96 |
| CHEMBL3884728 | — | — | 1 | 6.78 |
| CHEMBL3884634 | — | — | 1 | 6.11 |
| CHEMBL3884743 | — | — | 1 | 5.99 |
| CHEMBL282199 | — | — | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56 | 8-OH-DPAT | Ki | = | 2.65 | nM | 8.58 |
| CHEMBL3884095 | — | Ki | = | 2.99 | nM | 8.52 |
| CHEMBL3883640 | — | Ki | = | 6.96 | nM | 8.16 |
| CHEMBL3883542 | — | Ki | = | 8.21 | nM | 8.09 |
| CHEMBL3884714 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL3884584 | — | Ki | = | 17.8 | nM | 7.75 |
| CHEMBL3885389 | — | Ki | = | 18.6 | nM | 7.73 |
| CHEMBL3883517 | — | Ki | = | 24.7 | nM | 7.61 |
| CHEMBL3884778 | — | Ki | = | 25.9 | nM | 7.59 |
| CHEMBL3885319 | — | Ki | = | 33.5 | nM | 7.47 |
| CHEMBL3883995 | — | Ki | = | 52.1 | nM | 7.28 |
| CHEMBL3885282 | — | Ki | = | 90.3 | nM | 7.04 |
| CHEMBL3885178 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3884137 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL3884728 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL3884634 | — | Ki | = | 772.0 | nM | 6.11 |
| CHEMBL3884743 | — | Ki | = | 1032.0 | nM | 5.99 |
| CHEMBL282199 | — | Ki | = | 9024.0 | nM | 5.04 |