Assay Detail
Binding
CHEMBL4394031
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells 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 | 6.01 | 7.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.49 |
| CHEMBL4469847 | — | — | 1 | 6.91 |
| CHEMBL4558202 | — | — | 1 | 6.70 |
| CHEMBL4583507 | — | — | 1 | 6.58 |
| CHEMBL4462820 | — | — | 1 | 6.50 |
| CHEMBL4452569 | — | — | 1 | 6.23 |
| CHEMBL4204595 | — | — | 1 | 6.18 |
| CHEMBL4555349 | — | — | 1 | 6.17 |
| CHEMBL4541526 | — | — | 1 | 6.08 |
| CHEMBL4435235 | — | — | 1 | 6.03 |
| CHEMBL4216263 | — | — | 1 | 5.98 |
| CHEMBL4585956 | — | — | 1 | 5.97 |
| CHEMBL4559312 | — | — | 1 | 5.91 |
| CHEMBL4526012 | — | — | 1 | 5.91 |
| CHEMBL4476372 | — | — | 1 | 5.77 |
| CHEMBL4444268 | — | — | 1 | 5.76 |
| CHEMBL4455588 | — | — | 1 | 5.67 |
| CHEMBL4565881 | — | — | 1 | 5.63 |
| CHEMBL4438349 | — | — | 1 | 5.63 |
| CHEMBL4476520 | — | — | 1 | 5.48 |
| CHEMBL4592256 | — | — | 1 | 5.36 |
| CHEMBL4442337 | — | — | 1 | 5.25 |
| CHEMBL4452121 | — | — | 1 | 5.04 |
| CHEMBL4529615 | — | — | 1 | - |
| CHEMBL4555115 | — | — | 1 | - |
| CHEMBL4516621 | — | — | 1 | - |
| CHEMBL4531898 | — | — | 1 | - |
| CHEMBL4464377 | — | — | 1 | - |
| CHEMBL4573883 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49 | BUSPIRONE | Ki | = | 32.2 | nM | 7.49 |
| CHEMBL4469847 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL4558202 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL4583507 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL4462820 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL4452569 | — | Ki | = | 589.0 | nM | 6.23 |
| CHEMBL4204595 | — | Ki | = | 661.0 | nM | 6.18 |
| CHEMBL4555349 | — | Ki | = | 676.0 | nM | 6.17 |
| CHEMBL4541526 | — | Ki | = | 832.0 | nM | 6.08 |
| CHEMBL4435235 | — | Ki | = | 933.0 | nM | 6.03 |
| CHEMBL4216263 | — | Ki | = | 1047.0 | nM | 5.98 |
| CHEMBL4585956 | — | Ki | = | 1072.0 | nM | 5.97 |
| CHEMBL4559312 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL4526012 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL4476372 | — | Ki | = | 1698.0 | nM | 5.77 |
| CHEMBL4444268 | — | Ki | = | 1738.0 | nM | 5.76 |
| CHEMBL4455588 | — | Ki | = | 2138.0 | nM | 5.67 |
| CHEMBL4565881 | — | Ki | = | 2344.0 | nM | 5.63 |
| CHEMBL4438349 | — | Ki | = | 2344.0 | nM | 5.63 |
| CHEMBL4476520 | — | Ki | = | 3311.0 | nM | 5.48 |
| CHEMBL4592256 | — | Ki | = | 4365.0 | nM | 5.36 |
| CHEMBL4442337 | — | Ki | = | 5623.0 | nM | 5.25 |
| CHEMBL4452121 | — | Ki | = | 9120.0 | nM | 5.04 |
| CHEMBL4529615 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4555115 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4516621 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4531898 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4464377 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4573883 | — | Ki | > | 10000.0 | nM | - |