Assay Detail
Binding
CHEMBL4316413
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Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
18
Total Activities
18
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
Virtual screening-driven discovery of dual 5-HT<sub>6</sub>/5-HT<sub>2A</sub> receptor ligands with pro-cognitive properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.46 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.46 |
| CHEMBL4435528 | — | — | 1 | 7.19 |
| CHEMBL4464881 | — | — | 1 | 7.04 |
| CHEMBL4583082 | — | — | 1 | 6.92 |
| CHEMBL4462814 | — | — | 1 | 6.90 |
| CHEMBL4591410 | — | — | 1 | 6.84 |
| CHEMBL4584504 | — | — | 1 | 6.70 |
| CHEMBL4593671 | — | — | 1 | 6.66 |
| CHEMBL4465414 | — | — | 1 | 6.54 |
| CHEMBL4519266 | — | — | 1 | 6.48 |
| CHEMBL4438434 | — | — | 1 | 6.40 |
| CHEMBL4442111 | — | — | 1 | 6.37 |
| CHEMBL4474618 | — | — | 1 | 6.13 |
| CHEMBL4552041 | — | — | 1 | 6.11 |
| CHEMBL4437523 | — | — | 1 | 6.00 |
| CHEMBL4448285 | — | — | 1 | 5.98 |
| CHEMBL3286580 | IDALOPIRDINE | 3.0 | 1 | 5.41 |
| CHEMBL4442855 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49 | BUSPIRONE | Ki | = | 34.3 | nM | 7.46 |
| CHEMBL4435528 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL4464881 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL4583082 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4462814 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL4591410 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL4584504 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL4593671 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL4465414 | — | Ki | = | 292.0 | nM | 6.54 |
| CHEMBL4519266 | — | Ki | = | 334.0 | nM | 6.48 |
| CHEMBL4438434 | — | Ki | = | 399.0 | nM | 6.40 |
| CHEMBL4442111 | — | Ki | = | 431.0 | nM | 6.37 |
| CHEMBL4474618 | — | Ki | = | 732.0 | nM | 6.13 |
| CHEMBL4552041 | — | Ki | = | 775.0 | nM | 6.11 |
| CHEMBL4437523 | — | Ki | = | 1010.0 | nM | 6.00 |
| CHEMBL4448285 | — | Ki | = | 1052.0 | nM | 5.98 |
| CHEMBL3286580 | IDALOPIRDINE | Ki | = | 3936.0 | nM | 5.41 |
| CHEMBL4442855 | — | Ki | = | 6204.0 | nM | 5.21 |