Assay Detail
Binding
CHEMBL4041725
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]8-OH-DPAT from recombinant human 5HT1A receptor expressed in human HeLa cell membranes after 30 mins by liquid scintillation counting method
32
Total Activities
32
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
The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT1A receptor over α1-adrenoceptor and D2-like receptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 8.28 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2312536 | — | — | 1 | 9.51 |
| CHEMBL13647 | BMY-7378 | — | 1 | 9.43 |
| CHEMBL2312538 | — | — | 1 | 9.40 |
| CHEMBL2312226 | — | — | 1 | 9.26 |
| CHEMBL4067083 | — | — | 1 | 9.25 |
| CHEMBL2312537 | — | — | 1 | 9.23 |
| CHEMBL493486 | — | — | 1 | 9.22 |
| CHEMBL4071929 | — | — | 1 | 9.20 |
| CHEMBL2312227 | — | — | 1 | 9.18 |
| CHEMBL4082195 | — | — | 1 | 9.16 |
| CHEMBL4075507 | — | — | 1 | 9.10 |
| CHEMBL4091168 | — | — | 1 | 9.05 |
| CHEMBL4070363 | — | — | 1 | 8.95 |
| CHEMBL2312225 | — | — | 1 | 8.85 |
| CHEMBL493285 | — | — | 1 | 8.83 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 8.47 |
| CHEMBL521665 | — | — | 1 | 8.46 |
| CHEMBL452437 | — | — | 1 | 8.38 |
| CHEMBL493041 | — | — | 1 | 8.22 |
| CHEMBL4076339 | — | — | 1 | 8.12 |
| CHEMBL449057 | — | — | 1 | 7.59 |
| CHEMBL4079031 | — | — | 1 | 7.43 |
| CHEMBL494908 | — | — | 1 | 7.41 |
| CHEMBL493697 | — | — | 1 | 7.35 |
| CHEMBL492785 | — | — | 1 | 7.28 |
| CHEMBL492835 | — | — | 1 | 7.27 |
| CHEMBL521694 | — | — | 1 | 6.83 |
| CHEMBL4083434 | — | — | 1 | 6.64 |
| CHEMBL493661 | — | — | 1 | 6.63 |
| CHEMBL492834 | — | — | 1 | 6.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2312536 | — | Ki | = | 0.309 | nM | 9.51 |
| CHEMBL13647 | BMY-7378 | Ki | = | 0.3715 | nM | 9.43 |
| CHEMBL2312538 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL2312226 | — | Ki | = | 0.5495 | nM | 9.26 |
| CHEMBL4067083 | — | Ki | = | 0.5623 | nM | 9.25 |
| CHEMBL2312537 | — | Ki | = | 0.5888 | nM | 9.23 |
| CHEMBL493486 | — | Ki | = | 0.6026 | nM | 9.22 |
| CHEMBL4071929 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL2312227 | — | Ki | = | 0.6607 | nM | 9.18 |
| CHEMBL4082195 | — | Ki | = | 0.6918 | nM | 9.16 |
| CHEMBL4075507 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL4091168 | — | Ki | = | 0.8913 | nM | 9.05 |
| CHEMBL4070363 | — | Ki | = | 1.122 | nM | 8.95 |
| CHEMBL2312225 | — | Ki | = | 1.413 | nM | 8.85 |
| CHEMBL493285 | — | Ki | = | 1.479 | nM | 8.83 |
| CHEMBL56 | 8-OH-DPAT | Ki | = | 3.388 | nM | 8.47 |
| CHEMBL521665 | — | Ki | = | 3.467 | nM | 8.46 |
| CHEMBL452437 | — | Ki | = | 4.169 | nM | 8.38 |
| CHEMBL493041 | — | Ki | = | 6.026 | nM | 8.22 |
| CHEMBL4076339 | — | Ki | = | 7.586 | nM | 8.12 |
| CHEMBL449057 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL4079031 | — | Ki | = | 37.15 | nM | 7.43 |
| CHEMBL494908 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL493697 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL492785 | — | Ki | = | 52.48 | nM | 7.28 |
| CHEMBL492835 | — | Ki | = | 53.7 | nM | 7.27 |
| CHEMBL521694 | — | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL4083434 | — | Ki | = | 229.09 | nM | 6.64 |
| CHEMBL493661 | — | Ki | = | 234.42 | nM | 6.63 |
| CHEMBL492834 | — | Ki | = | 257.04 | nM | 6.59 |
| CHEMBL493042 | — | Ki | = | 416.87 | nM | 6.38 |
| CHEMBL493043 | — | Ki | > | 1000.0 | nM | - |