Assay Detail
Binding
CHEMBL4625523
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
42
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT<sub>7A</sub>R ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.59 | 8.40 |
| Inhibition | 12 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.40 |
| CHEMBL4640588 | — | — | 1 | 7.07 |
| CHEMBL4646172 | — | — | 1 | 6.99 |
| CHEMBL4645997 | — | — | 1 | 6.90 |
| CHEMBL4639400 | — | — | 1 | 6.88 |
| CHEMBL4640150 | — | — | 1 | 6.70 |
| CHEMBL4632872 | — | — | 1 | 6.66 |
| CHEMBL4642034 | — | — | 1 | 6.49 |
| CHEMBL4646861 | — | — | 1 | 6.48 |
| CHEMBL4649697 | — | — | 1 | 6.45 |
| CHEMBL4636165 | — | — | 1 | 6.45 |
| CHEMBL4640332 | — | — | 1 | 6.39 |
| CHEMBL4635229 | — | — | 1 | 6.38 |
| CHEMBL4640281 | — | — | 1 | 6.30 |
| CHEMBL4634426 | — | — | 1 | 6.28 |
| CHEMBL4644833 | — | — | 1 | 6.23 |
| CHEMBL4633765 | — | — | 1 | 5.82 |
| CHEMBL4636329 | — | — | 1 | 5.80 |
| CHEMBL4633042 | — | — | 2 | - |
| CHEMBL4633786 | — | — | 2 | - |
| CHEMBL4649078 | — | — | 2 | - |
| CHEMBL4641502 | — | — | 2 | - |
| CHEMBL4633889 | — | — | 2 | - |
| CHEMBL4639633 | — | — | 2 | - |
| CHEMBL4636148 | — | — | 2 | - |
| CHEMBL4643640 | — | — | 2 | - |
| CHEMBL4647589 | — | — | 2 | - |
| CHEMBL4635676 | — | — | 2 | - |
| CHEMBL4637084 | — | — | 2 | - |
| CHEMBL4649646 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4640588 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL4646172 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL4645997 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL4639400 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL4640150 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL4632872 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL4642034 | — | Ki | = | 322.0 | nM | 6.49 |
| CHEMBL4646861 | — | Ki | = | 329.0 | nM | 6.48 |
| CHEMBL4649697 | — | Ki | = | 356.0 | nM | 6.45 |
| CHEMBL4636165 | — | Ki | = | 354.0 | nM | 6.45 |
| CHEMBL4640332 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL4635229 | — | Ki | = | 415.0 | nM | 6.38 |
| CHEMBL4640281 | — | Ki | = | 505.0 | nM | 6.30 |
| CHEMBL4634426 | — | Ki | = | 527.0 | nM | 6.28 |
| CHEMBL4644833 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL4633765 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL4636329 | — | Ki | = | 1588.0 | nM | 5.80 |
| CHEMBL4649646 | — | Ki | - | — | - | |
| CHEMBL4637084 | — | Ki | - | — | - | |
| CHEMBL4635676 | — | Ki | - | — | - | |
| CHEMBL4647589 | — | Ki | - | — | - | |
| CHEMBL4643640 | — | Ki | - | — | - | |
| CHEMBL4636148 | — | Ki | - | — | - | |
| CHEMBL4639633 | — | Ki | - | — | - | |
| CHEMBL4633889 | — | Ki | - | — | - | |
| CHEMBL4641502 | — | Ki | - | — | - | |
| CHEMBL4649078 | — | Ki | - | — | - | |
| CHEMBL4633786 | — | Ki | - | — | - | |
| CHEMBL4633042 | — | Ki | - | — | - | |
| CHEMBL4633042 | — | Inhibition | < | 50.0 | % | - |
| CHEMBL4633786 | — | Inhibition | < | 50.0 | % | - |
| CHEMBL4649078 | — | Inhibition | < | 50.0 | % | - |
| CHEMBL4641502 | — | Inhibition | < | 50.0 | % | - |
| CHEMBL4633889 | — | Inhibition | < | 50.0 | % | - |
| CHEMBL4639633 | — | Inhibition | < | 50.0 | % | - |
| CHEMBL4636148 | — | Inhibition | < | 50.0 | % | - |
| CHEMBL4643640 | — | Inhibition | < | 50.0 | % | - |
| CHEMBL4647589 | — | Inhibition | < | 50.0 | % | - |
| CHEMBL4635676 | — | Inhibition | < | 50.0 | % | - |
| CHEMBL4637084 | — | Inhibition | < | 50.0 | % | - |
| CHEMBL4649646 | — | Inhibition | < | 50.0 | % | - |