Assay Detail
Binding
CHEMBL4394034
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Displacement of [3H]-5-CT from human recombinant 5-HT7B 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 | 7.29 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4452569 | — | — | 1 | 8.40 |
| CHEMBL4469847 | — | — | 1 | 8.30 |
| CHEMBL4216263 | — | — | 1 | 8.22 |
| CHEMBL4541526 | — | — | 1 | 8.10 |
| CHEMBL4585956 | — | — | 1 | 7.85 |
| CHEMBL4462820 | — | — | 1 | 7.80 |
| CHEMBL4444268 | — | — | 1 | 7.75 |
| CHEMBL4559312 | — | — | 1 | 7.70 |
| CHEMBL4558202 | — | — | 1 | 7.68 |
| CHEMBL4435235 | — | — | 1 | 7.66 |
| CHEMBL4526012 | — | — | 1 | 7.54 |
| CHEMBL4204595 | — | — | 1 | 7.52 |
| CHEMBL4555349 | — | — | 1 | 7.44 |
| CHEMBL4452121 | — | — | 1 | 7.38 |
| CHEMBL4455588 | — | — | 1 | 7.36 |
| CHEMBL4583507 | — | — | 1 | 7.34 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.32 |
| CHEMBL4438349 | — | — | 1 | 7.31 |
| CHEMBL4476372 | — | — | 1 | 7.28 |
| CHEMBL4529615 | — | — | 1 | 7.16 |
| CHEMBL4592256 | — | — | 1 | 6.86 |
| CHEMBL4476520 | — | — | 1 | 6.56 |
| CHEMBL4565881 | — | — | 1 | 6.52 |
| CHEMBL4442337 | — | — | 1 | 6.41 |
| CHEMBL4464377 | — | — | 1 | 6.28 |
| CHEMBL4531898 | — | — | 1 | 5.84 |
| CHEMBL4555115 | — | — | 1 | 5.23 |
| CHEMBL4516621 | — | — | 1 | - |
| CHEMBL4573883 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4452569 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4469847 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4216263 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4541526 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4585956 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4462820 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4444268 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4559312 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4558202 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4435235 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4526012 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4204595 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4555349 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL4452121 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4455588 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL4583507 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL42 | CLOZAPINE | Ki | = | 47.4 | nM | 7.32 |
| CHEMBL4438349 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL4476372 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL4529615 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4592256 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL4476520 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL4565881 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL4442337 | — | Ki | = | 386.0 | nM | 6.41 |
| CHEMBL4464377 | — | Ki | = | 531.0 | nM | 6.28 |
| CHEMBL4531898 | — | Ki | = | 1445.0 | nM | 5.84 |
| CHEMBL4555115 | — | Ki | = | 5888.0 | nM | 5.23 |
| CHEMBL4516621 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4573883 | — | Ki | > | 10000.0 | nM | - |