Assay Detail
Binding
CHEMBL4401062
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ketanserin from recombinant human 5HT2A receptor expressed in HEK293 cells measured after 1.5 hrs by microbeta scintillation counting analysis
10
Total Activities
10
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 novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT1A receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.30 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 8.55 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.34 |
| CHEMBL4469813 | — | — | 1 | 7.68 |
| CHEMBL4570209 | — | — | 1 | 6.50 |
| CHEMBL4462139 | — | — | 1 | 6.36 |
| CHEMBL4451231 | — | — | 1 | 6.36 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | - |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | - |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | - |
| CHEMBL42 | CLOZAPINE | 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 |
| CHEMBL4469813 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4570209 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL4462139 | — | Ki | = | 435.0 | nM | 6.36 |
| CHEMBL4451231 | — | Ki | = | 433.0 | nM | 6.36 |
| CHEMBL71 | CHLORPROMAZINE | Ki | - | — | - | |
| CHEMBL53 | APOMORPHINE | Ki | - | — | - | |
| CHEMBL54 | HALOPERIDOL | Ki | - | — | - | |
| CHEMBL42 | CLOZAPINE | Ki | - | — | - |