Assay Detail
Binding
CHEMBL618141
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094132) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
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 | 7.65 | 10.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL416662 | — | — | 1 | 10.09 |
| CHEMBL299634 | — | — | 1 | 9.54 |
| CHEMBL53416 | — | — | 1 | 9.45 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 9.35 |
| CHEMBL49932 | — | — | 1 | 9.10 |
| CHEMBL51118 | — | — | 1 | 9.04 |
| CHEMBL54914 | — | — | 1 | 9.01 |
| CHEMBL52772 | — | — | 1 | 8.93 |
| CHEMBL54720 | — | — | 1 | 8.85 |
| CHEMBL53490 | — | — | 1 | 8.83 |
| CHEMBL54125 | — | — | 1 | 8.62 |
| CHEMBL52625 | — | — | 1 | 8.58 |
| CHEMBL53662 | — | — | 1 | 8.18 |
| CHEMBL301765 | — | — | 1 | 7.92 |
| CHEMBL300692 | — | — | 1 | 7.87 |
| CHEMBL300725 | — | — | 1 | 7.85 |
| CHEMBL299097 | — | — | 1 | 7.71 |
| CHEMBL410531 | — | — | 1 | 7.71 |
| CHEMBL432897 | — | — | 1 | 7.69 |
| CHEMBL52867 | — | — | 1 | 7.55 |
| CHEMBL50740 | — | — | 1 | 7.51 |
| CHEMBL52612 | — | — | 1 | 7.34 |
| CHEMBL53195 | — | — | 1 | 7.06 |
| CHEMBL52800 | — | — | 1 | 6.93 |
| CHEMBL50456 | — | — | 1 | 5.89 |
| CHEMBL27403 | — | — | 1 | 5.88 |
| CHEMBL299524 | — | — | 1 | 5.59 |
| CHEMBL54246 | — | — | 1 | 5.52 |
| CHEMBL51225 | — | — | 1 | 4.56 |
| CHEMBL52007 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL416662 | — | IC50 | = | 0.08128 | nM | 10.09 |
| CHEMBL299634 | — | IC50 | = | 0.2884 | nM | 9.54 |
| CHEMBL53416 | — | IC50 | = | 0.3548 | nM | 9.45 |
| CHEMBL18772 | QUIPAZINE | IC50 | = | 0.4467 | nM | 9.35 |
| CHEMBL49932 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL51118 | — | IC50 | = | 0.912 | nM | 9.04 |
| CHEMBL54914 | — | IC50 | = | 0.9772 | nM | 9.01 |
| CHEMBL52772 | — | IC50 | = | 1.175 | nM | 8.93 |
| CHEMBL54720 | — | IC50 | = | 1.413 | nM | 8.85 |
| CHEMBL53490 | — | IC50 | = | 1.479 | nM | 8.83 |
| CHEMBL54125 | — | IC50 | = | 2.399 | nM | 8.62 |
| CHEMBL52625 | — | IC50 | = | 2.63 | nM | 8.58 |
| CHEMBL53662 | — | IC50 | = | 6.607 | nM | 8.18 |
| CHEMBL301765 | — | IC50 | = | 12.02 | nM | 7.92 |
| CHEMBL300692 | — | IC50 | = | 13.49 | nM | 7.87 |
| CHEMBL300725 | — | IC50 | = | 14.13 | nM | 7.85 |
| CHEMBL410531 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL299097 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL432897 | — | IC50 | = | 20.42 | nM | 7.69 |
| CHEMBL52867 | — | IC50 | = | 28.18 | nM | 7.55 |
| CHEMBL50740 | — | IC50 | = | 30.9 | nM | 7.51 |
| CHEMBL52612 | — | IC50 | = | 45.71 | nM | 7.34 |
| CHEMBL53195 | — | IC50 | = | 87.1 | nM | 7.06 |
| CHEMBL52800 | — | IC50 | = | 117.49 | nM | 6.93 |
| CHEMBL50456 | — | IC50 | = | 1288.25 | nM | 5.89 |
| CHEMBL27403 | — | IC50 | = | 1318.26 | nM | 5.88 |
| CHEMBL299524 | — | IC50 | = | 2570.4 | nM | 5.59 |
| CHEMBL54246 | — | IC50 | = | 3019.95 | nM | 5.52 |
| CHEMBL51225 | — | IC50 | = | 27542.29 | nM | 4.56 |
| CHEMBL52007 | — | IC50 | = | 28183.83 | nM | 4.55 |
| CHEMBL51675 | — | IC50 | = | 37153.52 | nM | 4.43 |
| CHEMBL415933 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL53573 | — | IC50 | = | 0.0008128 | nM | - |
| CHEMBL298649 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL299231 | — | IC50 | = | 0.003981 | nM | - |