Assay Detail
Binding
CHEMBL4401065
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-raclopride from recombinant human D2 receptor expressed in HEK293 cells measured after 1 hr 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 | 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 |
| CHEMBL4462139 | — | — | 1 | 6.02 |
| CHEMBL4469813 | — | — | 1 | 5.95 |
| CHEMBL4570209 | — | — | 1 | 4.95 |
| CHEMBL4451231 | — | — | 1 | 4.75 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | - |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | - |
| CHEMBL715 | OLANZAPINE | 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 |
| CHEMBL4462139 | — | Ki | = | 963.0 | nM | 6.02 |
| CHEMBL4469813 | — | Ki | = | 1129.0 | nM | 5.95 |
| CHEMBL4570209 | — | Ki | = | 11160.0 | nM | 4.95 |
| CHEMBL4451231 | — | Ki | = | 17670.0 | nM | 4.75 |
| CHEMBL42 | CLOZAPINE | Ki | - | — | - | |
| CHEMBL6437 | MIANSERIN | Ki | - | — | - | |
| CHEMBL715 | OLANZAPINE | Ki | - | — | - |