Assay Detail
Binding
CHEMBL615579
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against 5-hydroxytryptamine 1A receptor was measured using [3H]8-OH-DPAT as radioligand
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.34 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27403 | — | — | 1 | 7.33 |
| CHEMBL301765 | — | — | 1 | 7.23 |
| CHEMBL53490 | — | — | 1 | 7.19 |
| CHEMBL51118 | — | — | 1 | 7.17 |
| CHEMBL54914 | — | — | 1 | 7.01 |
| CHEMBL299231 | — | — | 1 | 6.93 |
| CHEMBL54720 | — | — | 1 | 6.40 |
| CHEMBL415933 | — | — | 1 | 6.31 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 5.84 |
| CHEMBL52612 | — | — | 1 | 5.64 |
| CHEMBL53416 | — | — | 1 | 5.59 |
| CHEMBL53573 | — | — | 1 | 5.53 |
| CHEMBL299097 | — | — | 1 | 5.34 |
| CHEMBL54125 | — | — | 1 | 5.27 |
| CHEMBL52625 | — | — | 1 | 5.17 |
| CHEMBL416662 | — | — | 1 | 5.02 |
| CHEMBL49932 | — | — | 1 | 4.96 |
| CHEMBL299524 | — | — | 1 | 4.94 |
| CHEMBL300692 | — | — | 1 | 4.89 |
| CHEMBL52772 | — | — | 1 | 4.84 |
| CHEMBL52867 | — | — | 1 | 4.64 |
| CHEMBL300725 | — | — | 1 | 4.39 |
| CHEMBL410531 | — | — | 1 | 4.39 |
| CHEMBL53662 | — | — | 1 | 4.38 |
| CHEMBL54246 | — | — | 1 | 4.30 |
| CHEMBL51675 | — | — | 1 | 4.26 |
| CHEMBL52800 | — | — | 1 | 4.25 |
| CHEMBL50456 | — | — | 1 | 4.21 |
| CHEMBL50740 | — | — | 1 | 4.20 |
| CHEMBL432897 | — | — | 1 | 4.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27403 | — | IC50 | = | 46.77 | nM | 7.33 |
| CHEMBL301765 | — | IC50 | = | 58.88 | nM | 7.23 |
| CHEMBL53490 | — | IC50 | = | 64.57 | nM | 7.19 |
| CHEMBL51118 | — | IC50 | = | 67.61 | nM | 7.17 |
| CHEMBL54914 | — | IC50 | = | 97.72 | nM | 7.01 |
| CHEMBL299231 | — | IC50 | = | 117.49 | nM | 6.93 |
| CHEMBL54720 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL415933 | — | IC50 | = | 489.78 | nM | 6.31 |
| CHEMBL18772 | QUIPAZINE | IC50 | = | 1445.44 | nM | 5.84 |
| CHEMBL52612 | — | IC50 | = | 2290.87 | nM | 5.64 |
| CHEMBL53416 | — | IC50 | = | 2570.4 | nM | 5.59 |
| CHEMBL53573 | — | IC50 | = | 2951.21 | nM | 5.53 |
| CHEMBL299097 | — | IC50 | = | 4570.88 | nM | 5.34 |
| CHEMBL54125 | — | IC50 | = | 5370.32 | nM | 5.27 |
| CHEMBL52625 | — | IC50 | = | 6760.83 | nM | 5.17 |
| CHEMBL416662 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL49932 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL299524 | — | IC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL300692 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL52772 | — | IC50 | = | 14454.4 | nM | 4.84 |
| CHEMBL52867 | — | IC50 | = | 22908.68 | nM | 4.64 |
| CHEMBL300725 | — | IC50 | = | 40738.03 | nM | 4.39 |
| CHEMBL410531 | — | IC50 | = | 40738.03 | nM | 4.39 |
| CHEMBL53662 | — | IC50 | = | 41686.94 | nM | 4.38 |
| CHEMBL54246 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL51675 | — | IC50 | = | 54954.09 | nM | 4.26 |
| CHEMBL52800 | — | IC50 | = | 56234.13 | nM | 4.25 |
| CHEMBL50456 | — | IC50 | = | 61659.5 | nM | 4.21 |
| CHEMBL50740 | — | IC50 | = | 63095.73 | nM | 4.20 |
| CHEMBL432897 | — | IC50 | = | 89125.09 | nM | 4.05 |
| CHEMBL298649 | — | IC50 | = | 97723.72 | nM | 4.01 |
| CHEMBL51225 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL53195 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL52007 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL299634 | — | IC50 | > | 100000.0 | nM | - |