Assay Detail
Binding
CHEMBL4367997
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEK293 cells incubated for 1.5 hrs by Cheng-Prusoff analysis based microbeta scintillation counting method
13
Total Activities
13
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
Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT<sub>1A</sub> receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.63 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 8.55 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.34 |
| CHEMBL4470437 | — | — | 1 | 6.49 |
| CHEMBL4582567 | — | — | 1 | 6.32 |
| CHEMBL4455658 | — | — | 1 | 6.21 |
| CHEMBL4476164 | — | — | 1 | 6.14 |
| CHEMBL4471755 | — | — | 1 | 5.92 |
| CHEMBL4469537 | — | — | 1 | 5.89 |
| CHEMBL4469633 | — | — | 1 | 5.83 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | - |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | - |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | - |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL715 | OLANZAPINE | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL4470437 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL4582567 | — | Ki | = | 484.0 | nM | 6.32 |
| CHEMBL4455658 | — | Ki | = | 609.0 | nM | 6.21 |
| CHEMBL4476164 | — | Ki | = | 725.0 | nM | 6.14 |
| CHEMBL4471755 | — | Ki | = | 1191.0 | nM | 5.92 |
| CHEMBL4469537 | — | Ki | = | 1277.0 | nM | 5.89 |
| CHEMBL4469633 | — | Ki | = | 1488.0 | nM | 5.83 |
| CHEMBL42 | CLOZAPINE | Ki | - | — | - | |
| CHEMBL54 | HALOPERIDOL | Ki | - | — | - | |
| CHEMBL53 | APOMORPHINE | Ki | - | — | - | |
| CHEMBL71 | CHLORPROMAZINE | Ki | - | — | - |