Assay Detail
Functional
CHEMBL1060394
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
15
Total Activities
15
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 | Intermediate |
Publication
Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.58 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL562248 | — | — | 1 | 7.25 |
| CHEMBL564148 | — | — | 1 | 7.24 |
| CHEMBL551909 | — | — | 1 | 7.16 |
| CHEMBL551304 | — | — | 1 | 7.16 |
| CHEMBL551964 | — | — | 1 | 6.99 |
| CHEMBL551107 | — | — | 1 | 6.93 |
| CHEMBL550700 | — | — | 1 | 6.81 |
| CHEMBL559778 | — | — | 1 | 6.79 |
| CHEMBL560170 | — | — | 1 | 6.75 |
| CHEMBL556474 | — | — | 1 | 6.53 |
| CHEMBL551105 | — | — | 1 | 6.23 |
| CHEMBL559579 | — | — | 1 | 6.11 |
| CHEMBL565234 | — | — | 1 | 5.72 |
| CHEMBL550169 | — | — | 1 | 5.67 |
| CHEMBL550576 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL562248 | — | IC50 | = | 56.7 | nM | 7.25 |
| CHEMBL564148 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL551909 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL551304 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL551964 | — | IC50 | = | 102.1 | nM | 6.99 |
| CHEMBL551107 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL550700 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL559778 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL560170 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL556474 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL551105 | — | IC50 | = | 588.0 | nM | 6.23 |
| CHEMBL559579 | — | IC50 | = | 781.0 | nM | 6.11 |
| CHEMBL565234 | — | IC50 | = | 1899.0 | nM | 5.72 |
| CHEMBL550169 | — | IC50 | = | 2165.0 | nM | 5.67 |
| CHEMBL550576 | — | IC50 | = | 4870.0 | nM | 5.31 |