Assay Detail
Binding
CHEMBL4401060
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-8-OH-DPAT from recombinant human 5HT1A receptor expressed in CHO cell membranes measured after 60 mins by microbeta scintillation counting analysis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 | 28 | 6.94 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 8.52 |
| CHEMBL4451231 | — | — | 1 | 7.66 |
| CHEMBL4469813 | — | — | 1 | 7.38 |
| CHEMBL4462139 | — | — | 1 | 7.34 |
| CHEMBL4587833 | — | — | 1 | 7.30 |
| CHEMBL4576769 | — | — | 1 | 7.28 |
| CHEMBL4570209 | — | — | 1 | 7.21 |
| CHEMBL4441125 | — | — | 1 | 7.20 |
| CHEMBL4470492 | — | — | 1 | 7.16 |
| CHEMBL4572860 | — | — | 1 | 7.10 |
| CHEMBL4459776 | — | — | 1 | 6.99 |
| CHEMBL4441004 | — | — | 1 | 6.89 |
| CHEMBL4473888 | — | — | 1 | 6.88 |
| CHEMBL4473005 | — | — | 1 | 6.87 |
| CHEMBL4438147 | — | — | 1 | 6.85 |
| CHEMBL4556098 | — | — | 1 | 6.83 |
| CHEMBL4457041 | — | — | 1 | 6.81 |
| CHEMBL4563197 | — | — | 1 | 6.75 |
| CHEMBL4515193 | — | — | 1 | 6.68 |
| CHEMBL4439370 | — | — | 1 | 6.66 |
| CHEMBL4580595 | — | — | 1 | 6.59 |
| CHEMBL4475065 | — | — | 1 | 6.58 |
| CHEMBL4570910 | — | — | 1 | 6.55 |
| CHEMBL4567376 | — | — | 1 | 6.53 |
| CHEMBL4518119 | — | — | 1 | 6.48 |
| CHEMBL4451382 | — | — | 1 | 6.42 |
| CHEMBL4559071 | — | — | 1 | 6.42 |
| CHEMBL4466717 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4451231 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4469813 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4462139 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4587833 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4576769 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL4570209 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4441125 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4470492 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL4572860 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL4459776 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL4441004 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL4473888 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL4473005 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL4438147 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL4556098 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL4457041 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL4563197 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL4515193 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL4439370 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL4580595 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL4475065 | — | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL4570910 | — | Ki | = | 281.0 | nM | 6.55 |
| CHEMBL4567376 | — | Ki | = | 294.0 | nM | 6.53 |
| CHEMBL4518119 | — | Ki | = | 333.0 | nM | 6.48 |
| CHEMBL4451382 | — | Ki | = | 378.0 | nM | 6.42 |
| CHEMBL4559071 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL4466717 | — | Ki | = | 476.0 | nM | 6.32 |