Assay Detail
Functional
CHEMBL975276
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.99 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL513715 | — | — | 1 | 9.00 |
| CHEMBL522257 | — | — | 1 | 8.70 |
| CHEMBL513875 | — | — | 1 | 8.70 |
| CHEMBL511815 | — | — | 1 | 8.60 |
| CHEMBL469374 | — | — | 1 | 8.60 |
| CHEMBL469345 | — | — | 1 | 8.40 |
| CHEMBL472290 | — | — | 1 | 8.40 |
| CHEMBL469567 | — | — | 1 | 8.30 |
| CHEMBL469568 | — | — | 1 | 8.30 |
| CHEMBL469995 | — | — | 1 | 8.20 |
| CHEMBL511279 | — | — | 1 | 7.80 |
| CHEMBL471047 | — | — | 1 | 7.80 |
| CHEMBL512724 | — | — | 1 | 7.50 |
| CHEMBL470217 | — | — | 1 | 6.80 |
| CHEMBL490417 | — | — | 1 | 6.60 |
| CHEMBL469589 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL513715 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL522257 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL513875 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL511815 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL469374 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL469345 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL472290 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL469567 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL469568 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL469995 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL511279 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL471047 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL512724 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL470217 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL490417 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL469589 | — | Ki | = | 794.33 | nM | 6.10 |