Assay Detail
Binding
CHEMBL4316412
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human 5-HT2AR expressed in HEK293 cells by competitive binding assay
19
Total Activities
19
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 | 19 | 7.10 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.21 |
| CHEMBL4437523 | — | — | 1 | 7.96 |
| CHEMBL4438434 | — | — | 1 | 7.66 |
| CHEMBL4591410 | — | — | 1 | 7.55 |
| CHEMBL4435528 | — | — | 1 | 7.54 |
| CHEMBL4442855 | — | — | 1 | 7.50 |
| CHEMBL4442111 | — | — | 1 | 7.48 |
| CHEMBL4519266 | — | — | 1 | 7.46 |
| CHEMBL4583082 | — | — | 1 | 7.39 |
| CHEMBL4536315 | — | — | 1 | 7.38 |
| CHEMBL4584504 | — | — | 1 | 7.02 |
| CHEMBL4474618 | — | — | 1 | 6.88 |
| CHEMBL4465414 | — | — | 1 | 6.76 |
| CHEMBL4552041 | — | — | 1 | 6.70 |
| CHEMBL4464881 | — | — | 1 | 6.67 |
| CHEMBL4462814 | — | — | 1 | 6.34 |
| CHEMBL4593671 | — | — | 1 | 6.22 |
| CHEMBL3286580 | IDALOPIRDINE | 3.0 | 1 | 6.10 |
| CHEMBL4448285 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL4437523 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4438434 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4591410 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4435528 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4442855 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4442111 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4519266 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL4583082 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL4536315 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4584504 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL4474618 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL4465414 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL4552041 | — | Ki | = | 199.0 | nM | 6.70 |
| CHEMBL4464881 | — | Ki | = | 216.0 | nM | 6.67 |
| CHEMBL4462814 | — | Ki | = | 461.0 | nM | 6.34 |
| CHEMBL4593671 | — | Ki | = | 607.0 | nM | 6.22 |
| CHEMBL3286580 | IDALOPIRDINE | Ki | = | 791.0 | nM | 6.10 |
| CHEMBL4448285 | — | Ki | = | 843.0 | nM | 6.07 |