Assay Detail
Binding
CHEMBL618918
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Inhibition of [3H]granisetron binding to 5-hydroxytryptamine 3 receptor (5-HT 3 receptor) of rat cortex and hippocampus tissue
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Hippocampus |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Intermediate |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094116) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.84 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL43355 | — | — | 1 | 9.64 |
| CHEMBL41841 | — | — | 1 | 9.22 |
| CHEMBL41511 | — | — | 1 | 9.22 |
| CHEMBL289664 | — | — | 1 | 9.15 |
| CHEMBL289486 | — | — | 1 | 9.05 |
| CHEMBL43512 | — | — | 1 | 8.74 |
| CHEMBL290065 | — | — | 1 | 8.72 |
| CHEMBL39081 | — | — | 1 | 8.62 |
| CHEMBL3707024 | — | — | 1 | 8.52 |
| CHEMBL289732 | — | — | 1 | 8.44 |
| CHEMBL3707025 | — | — | 1 | 8.41 |
| CHEMBL289794 | — | — | 1 | 8.39 |
| CHEMBL417706 | — | — | 1 | 8.38 |
| CHEMBL41598 | — | — | 1 | 8.27 |
| CHEMBL43304 | — | — | 1 | 8.06 |
| CHEMBL288643 | — | — | 1 | 7.92 |
| CHEMBL288497 | — | — | 1 | 7.80 |
| CHEMBL290472 | — | — | 1 | 7.70 |
| CHEMBL38843 | — | — | 1 | 7.54 |
| CHEMBL43305 | — | — | 1 | 7.54 |
| CHEMBL41140 | 6-NITROQUIPAZINE | — | 1 | 7.24 |
| CHEMBL3707026 | — | — | 1 | 7.11 |
| CHEMBL41379 | — | — | 1 | 7.10 |
| CHEMBL41256 | — | — | 1 | 6.31 |
| CHEMBL41414 | — | — | 1 | 5.96 |
| CHEMBL38814 | — | — | 1 | 5.64 |
| CHEMBL290087 | — | — | 1 | 5.57 |
| CHEMBL289384 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL43355 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL41841 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL41511 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL289664 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL289486 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL43512 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL290065 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL39081 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3707024 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL289732 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL3707025 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL289794 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL417706 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL41598 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL43304 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL288643 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL288497 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL290472 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL38843 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL43305 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL41140 | 6-NITROQUIPAZINE | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL3707026 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL41379 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL41256 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL41414 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL38814 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL290087 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL289384 | — | Ki | = | 4900.0 | nM | 5.31 |