Assay Detail
Binding
CHEMBL5628221
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Binding affinity to human 5HT2A receptor expressed in CHO-K1 cells assessed as inhibition constant incubated for 1 hr radioligand binding assay
28
Total Activities
28
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
Synthesis, computational and experimental pharmacological studies for (thio)ether-triazine 5-HT<sub>6</sub>R ligands with noticeable action on AChE/BChE and chalcogen-dependent intrinsic activity in search for new class of drugs against Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 6.42 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 7.68 |
| CHEMBL5632885 | — | — | 1 | 7.21 |
| CHEMBL5631694 | — | — | 1 | 6.94 |
| CHEMBL5632000 | — | — | 1 | 6.93 |
| CHEMBL5633662 | — | — | 1 | 6.75 |
| CHEMBL5632758 | — | — | 1 | 6.75 |
| CHEMBL5632197 | — | — | 1 | 6.75 |
| CHEMBL5632895 | — | — | 1 | 6.73 |
| CHEMBL4873623 | — | — | 1 | 6.68 |
| CHEMBL4869411 | — | — | 1 | 6.51 |
| CHEMBL4846146 | — | — | 1 | 6.45 |
| CHEMBL4858771 | — | — | 1 | 6.42 |
| CHEMBL4860006 | — | — | 1 | 6.38 |
| CHEMBL5499005 | — | — | 1 | 6.37 |
| CHEMBL4873127 | — | — | 1 | 6.33 |
| CHEMBL4876727 | — | — | 1 | 6.33 |
| CHEMBL4860275 | — | — | 1 | 6.32 |
| CHEMBL4864448 | — | — | 1 | 6.31 |
| CHEMBL5631953 | — | — | 1 | 6.30 |
| CHEMBL5631952 | — | — | 1 | 6.26 |
| CHEMBL5633074 | — | — | 1 | 6.26 |
| CHEMBL5632924 | — | — | 1 | 6.24 |
| CHEMBL4861431 | — | — | 1 | 6.24 |
| CHEMBL4857676 | — | — | 1 | 6.16 |
| CHEMBL5632828 | — | — | 1 | 6.05 |
| CHEMBL5633651 | — | — | 1 | 5.67 |
| CHEMBL5632600 | — | — | 1 | 5.32 |
| CHEMBL4847379 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL5632885 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL5631694 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL5632000 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL5633662 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL5632758 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL5632197 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL5632895 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL4873623 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL4869411 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL4846146 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL4858771 | — | Ki | = | 382.0 | nM | 6.42 |
| CHEMBL4860006 | — | Ki | = | 412.0 | nM | 6.38 |
| CHEMBL5499005 | — | Ki | = | 427.0 | nM | 6.37 |
| CHEMBL4873127 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL4876727 | — | Ki | = | 463.0 | nM | 6.33 |
| CHEMBL4860275 | — | Ki | = | 484.0 | nM | 6.32 |
| CHEMBL4864448 | — | Ki | = | 488.0 | nM | 6.31 |
| CHEMBL5631953 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL5631952 | — | Ki | = | 547.0 | nM | 6.26 |
| CHEMBL5633074 | — | Ki | = | 551.0 | nM | 6.26 |
| CHEMBL5632924 | — | Ki | = | 573.0 | nM | 6.24 |
| CHEMBL4861431 | — | Ki | = | 576.0 | nM | 6.24 |
| CHEMBL4857676 | — | Ki | = | 696.0 | nM | 6.16 |
| CHEMBL5632828 | — | Ki | = | 892.0 | nM | 6.05 |
| CHEMBL5633651 | — | Ki | = | 2153.0 | nM | 5.67 |
| CHEMBL5632600 | — | Ki | = | 4817.0 | nM | 5.32 |
| CHEMBL4847379 | — | Ki | = | 5047.0 | nM | 5.30 |