Assay Detail
Binding
CHEMBL4394033
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Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Fluorinated indole-imidazole conjugates: Selective orally bioavailable 5-HT7 receptor low-basicity agonists, potential neuropathic painkillers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 5.76 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.06 |
| CHEMBL4526012 | — | — | 1 | 6.61 |
| CHEMBL4541526 | — | — | 1 | 6.39 |
| CHEMBL4438349 | — | — | 1 | 6.26 |
| CHEMBL4516621 | — | — | 1 | 6.22 |
| CHEMBL4585956 | — | — | 1 | 6.10 |
| CHEMBL4555115 | — | — | 1 | 6.10 |
| CHEMBL4559312 | — | — | 1 | 5.87 |
| CHEMBL4592256 | — | — | 1 | 5.86 |
| CHEMBL4476372 | — | — | 1 | 5.79 |
| CHEMBL4216263 | — | — | 1 | 5.78 |
| CHEMBL4555349 | — | — | 1 | 5.61 |
| CHEMBL4452569 | — | — | 1 | 5.54 |
| CHEMBL4462820 | — | — | 1 | 5.53 |
| CHEMBL4464377 | — | — | 1 | 5.52 |
| CHEMBL4476520 | — | — | 1 | 5.46 |
| CHEMBL4583507 | — | — | 1 | 5.46 |
| CHEMBL4558202 | — | — | 1 | 5.42 |
| CHEMBL4452121 | — | — | 1 | 5.38 |
| CHEMBL4565881 | — | — | 1 | 5.31 |
| CHEMBL4573883 | — | — | 1 | 5.23 |
| CHEMBL4442337 | — | — | 1 | 5.19 |
| CHEMBL4204595 | — | — | 1 | 5.16 |
| CHEMBL4529615 | — | — | 1 | 5.15 |
| CHEMBL4469847 | — | — | 1 | 5.11 |
| CHEMBL4531898 | — | — | 1 | - |
| CHEMBL4455588 | — | — | 1 | - |
| CHEMBL4444268 | — | — | 1 | - |
| CHEMBL4435235 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL4526012 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL4541526 | — | Ki | = | 407.0 | nM | 6.39 |
| CHEMBL4438349 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL4516621 | — | Ki | = | 603.0 | nM | 6.22 |
| CHEMBL4585956 | — | Ki | = | 794.0 | nM | 6.10 |
| CHEMBL4555115 | — | Ki | = | 794.0 | nM | 6.10 |
| CHEMBL4559312 | — | Ki | = | 1349.0 | nM | 5.87 |
| CHEMBL4592256 | — | Ki | = | 1380.0 | nM | 5.86 |
| CHEMBL4476372 | — | Ki | = | 1622.0 | nM | 5.79 |
| CHEMBL4216263 | — | Ki | = | 1660.0 | nM | 5.78 |
| CHEMBL4555349 | — | Ki | = | 2455.0 | nM | 5.61 |
| CHEMBL4452569 | — | Ki | = | 2884.0 | nM | 5.54 |
| CHEMBL4462820 | — | Ki | = | 2951.0 | nM | 5.53 |
| CHEMBL4464377 | — | Ki | = | 3020.0 | nM | 5.52 |
| CHEMBL4476520 | — | Ki | = | 3467.0 | nM | 5.46 |
| CHEMBL4583507 | — | Ki | = | 3467.0 | nM | 5.46 |
| CHEMBL4558202 | — | Ki | = | 3802.0 | nM | 5.42 |
| CHEMBL4452121 | — | Ki | = | 4169.0 | nM | 5.38 |
| CHEMBL4565881 | — | Ki | = | 4898.0 | nM | 5.31 |
| CHEMBL4573883 | — | Ki | = | 5888.0 | nM | 5.23 |
| CHEMBL4442337 | — | Ki | = | 6457.0 | nM | 5.19 |
| CHEMBL4204595 | — | Ki | = | 6918.0 | nM | 5.16 |
| CHEMBL4529615 | — | Ki | = | 7079.0 | nM | 5.15 |
| CHEMBL4469847 | — | Ki | = | 7762.0 | nM | 5.11 |
| CHEMBL4531898 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4455588 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4444268 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4435235 | — | Ki | > | 10000.0 | nM | - |