Assay Detail
Functional
CHEMBL1293142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.34 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1290486 | — | — | 1 | 9.20 |
| CHEMBL1290487 | — | — | 1 | 9.10 |
| CHEMBL1290716 | — | — | 1 | 9.10 |
| CHEMBL1289394 | — | — | 1 | 9.10 |
| CHEMBL513715 | — | — | 1 | 9.00 |
| CHEMBL469345 | — | — | 1 | 8.80 |
| CHEMBL1290715 | — | — | 1 | 8.70 |
| CHEMBL1289163 | — | — | 1 | 7.50 |
| CHEMBL1289510 | — | — | 1 | 6.50 |
| CHEMBL1287827 | — | — | 1 | 6.40 |
| CHEMBL1289276 | — | — | 1 | - |
| CHEMBL1289277 | — | — | 1 | - |
| CHEMBL1289509 | — | — | 1 | - |
| CHEMBL1289617 | — | — | 1 | - |
| CHEMBL1289618 | — | — | 1 | - |
| CHEMBL1289721 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1290486 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL1290487 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL1290716 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL1289394 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL513715 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL469345 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL1290715 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL1289163 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1289510 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1287827 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1289276 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1289277 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1289509 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1289617 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1289618 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1289721 | — | Ki | > | 1000.0 | nM | - |