Assay Detail
Binding
CHEMBL4368000
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-raclopride from human D2 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 | 6.59 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 8.74 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.35 |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | 7.38 |
| CHEMBL4455658 | — | — | 1 | 6.05 |
| CHEMBL4582567 | — | — | 1 | 5.98 |
| CHEMBL4469633 | — | — | 1 | 5.78 |
| CHEMBL4471755 | — | — | 1 | 5.74 |
| CHEMBL4469537 | — | — | 1 | 5.70 |
| CHEMBL4476164 | — | — | 1 | 5.63 |
| CHEMBL4470437 | — | — | 1 | - |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | - |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | - |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL53 | APOMORPHINE | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4455658 | — | Ki | = | 896.0 | nM | 6.05 |
| CHEMBL4582567 | — | Ki | = | 1047.0 | nM | 5.98 |
| CHEMBL4469633 | — | Ki | = | 1651.0 | nM | 5.78 |
| CHEMBL4471755 | — | Ki | = | 1802.0 | nM | 5.74 |
| CHEMBL4469537 | — | Ki | = | 1977.0 | nM | 5.70 |
| CHEMBL4476164 | — | Ki | = | 2349.0 | nM | 5.63 |
| CHEMBL4470437 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL715 | OLANZAPINE | Ki | - | — | - | |
| CHEMBL6437 | MIANSERIN | Ki | - | — | - | |
| CHEMBL42 | CLOZAPINE | Ki | - | — | - |