Assay Detail
Binding
CHEMBL4367995
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting method
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 29 | 7.33 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 8.44 |
| CHEMBL93240 | METITEPINE | 2.0 | 1 | 8.32 |
| CHEMBL4455658 | — | — | 1 | 8.10 |
| CHEMBL4469537 | — | — | 1 | 7.89 |
| CHEMBL4470437 | — | — | 1 | 7.82 |
| CHEMBL4475730 | — | — | 1 | 7.64 |
| CHEMBL4462825 | — | — | 1 | 7.60 |
| CHEMBL4476164 | — | — | 1 | 7.57 |
| CHEMBL4531647 | — | — | 1 | 7.55 |
| CHEMBL4469633 | — | — | 1 | 7.52 |
| CHEMBL4582567 | — | — | 1 | 7.51 |
| CHEMBL4466243 | — | — | 1 | 7.40 |
| CHEMBL4533362 | — | — | 1 | 7.38 |
| CHEMBL4442394 | — | — | 1 | 7.33 |
| CHEMBL4458537 | — | — | 1 | 7.30 |
| CHEMBL4530671 | — | — | 1 | 7.30 |
| CHEMBL4471755 | — | — | 1 | 7.28 |
| CHEMBL4467024 | — | — | 1 | 7.28 |
| CHEMBL4545518 | — | — | 1 | 7.21 |
| CHEMBL4458712 | — | — | 1 | 7.18 |
| CHEMBL4444099 | — | — | 1 | 7.12 |
| CHEMBL4515025 | — | — | 1 | 6.99 |
| CHEMBL4543669 | — | — | 1 | 6.98 |
| CHEMBL4472972 | — | — | 1 | 6.85 |
| CHEMBL4460224 | — | — | 1 | 6.63 |
| CHEMBL4449982 | — | — | 1 | 6.63 |
| CHEMBL4464118 | — | — | 1 | 6.62 |
| CHEMBL4471395 | — | — | 1 | 6.59 |
| CHEMBL4465006 | — | — | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL93240 | METITEPINE | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL4455658 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4469537 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4470437 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4475730 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4462825 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4476164 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL4531647 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4469633 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4582567 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4466243 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4533362 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4442394 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL4458537 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4530671 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4471755 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL4467024 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL4545518 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4458712 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL4444099 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL4515025 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL4543669 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL4472972 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL4460224 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL4449982 | — | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL4464118 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL4471395 | — | Ki | = | 259.0 | nM | 6.59 |
| CHEMBL4465006 | — | Ki | = | 321.0 | nM | 6.49 |