Assay Detail
Binding
CHEMBL4831101
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT<sub>6</sub>R antagonists with β-amyloid anti-aggregation properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 54 | 7.86 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL93240 | METITEPINE | 2.0 | 1 | 9.52 |
| CHEMBL4855991 | — | — | 1 | 9.52 |
| CHEMBL4850738 | — | — | 1 | 9.40 |
| CHEMBL4871652 | — | — | 1 | 9.30 |
| CHEMBL4866390 | — | — | 1 | 9.30 |
| CHEMBL4864854 | — | — | 1 | 8.85 |
| CHEMBL178254 | — | — | 1 | 8.80 |
| CHEMBL368698 | — | — | 1 | 8.59 |
| CHEMBL4873700 | — | — | 1 | 8.57 |
| CHEMBL4860124 | — | — | 1 | 8.52 |
| CHEMBL4862752 | — | — | 1 | 8.52 |
| CHEMBL4862289 | — | — | 1 | 8.52 |
| CHEMBL4863037 | — | — | 1 | 8.52 |
| CHEMBL4871678 | — | — | 1 | 8.46 |
| CHEMBL4871357 | — | — | 1 | 8.44 |
| CHEMBL4849702 | — | — | 1 | 8.40 |
| CHEMBL4854460 | — | — | 1 | 8.32 |
| CHEMBL4849917 | — | — | 1 | 8.30 |
| CHEMBL4863101 | — | — | 1 | 8.22 |
| CHEMBL4850764 | — | — | 1 | 8.22 |
| CHEMBL4861756 | — | — | 1 | 8.22 |
| CHEMBL4867606 | — | — | 1 | 8.19 |
| CHEMBL4854568 | — | — | 1 | 8.15 |
| CHEMBL4853545 | — | — | 1 | 8.07 |
| CHEMBL4872486 | — | — | 1 | 8.05 |
| CHEMBL4846931 | — | — | 1 | 7.96 |
| CHEMBL4845762 | — | — | 1 | 7.96 |
| CHEMBL4872078 | — | — | 1 | 7.92 |
| CHEMBL4874512 | — | — | 1 | 7.92 |
| CHEMBL4849680 | — | — | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL93240 | METITEPINE | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4855991 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4850738 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4871652 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4866390 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4864854 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL178254 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL368698 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL4873700 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4860124 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4862752 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4862289 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4863037 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4871678 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL4871357 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL4849702 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4854460 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL4849917 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4863101 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4850764 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4861756 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4867606 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4854568 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4853545 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL4872486 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4846931 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4845762 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4872078 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4874512 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4849680 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4879036 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4849477 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4862131 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4850275 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4874372 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4852840 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4872905 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL4863079 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4873096 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL4874675 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL4851655 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL4863967 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4845699 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4865076 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL4870158 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL4849430 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL4858014 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL4866962 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL4862516 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL4857018 | — | Ki | = | 293.0 | nM | 6.53 |