Assay Detail
Binding
CHEMBL4367999
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr 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 |
| 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 | 6.13 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.75 |
| CHEMBL4471755 | — | — | 1 | 6.26 |
| CHEMBL4476164 | — | — | 1 | 5.96 |
| CHEMBL4582567 | — | — | 1 | 5.95 |
| CHEMBL4455658 | — | — | 1 | 5.87 |
| CHEMBL4469633 | — | — | 1 | 5.86 |
| CHEMBL4469537 | — | — | 1 | 5.77 |
| CHEMBL4470437 | — | — | 1 | 5.61 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | - |
| CHEMBL6437 | MIANSERIN | 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 |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4471755 | — | Ki | = | 546.0 | nM | 6.26 |
| CHEMBL4476164 | — | Ki | = | 1092.0 | nM | 5.96 |
| CHEMBL4582567 | — | Ki | = | 1112.0 | nM | 5.95 |
| CHEMBL4455658 | — | Ki | = | 1361.0 | nM | 5.87 |
| CHEMBL4469633 | — | Ki | = | 1384.0 | nM | 5.86 |
| CHEMBL4469537 | — | Ki | = | 1712.0 | nM | 5.77 |
| CHEMBL4470437 | — | Ki | = | 2431.0 | nM | 5.61 |
| CHEMBL715 | OLANZAPINE | Ki | - | — | - | |
| CHEMBL6437 | MIANSERIN | Ki | - | — | - | |
| CHEMBL54 | HALOPERIDOL | Ki | - | — | - | |
| CHEMBL53 | APOMORPHINE | Ki | - | — | - | |
| CHEMBL71 | CHLORPROMAZINE | Ki | - | — | - |