Assay Detail
Binding
CHEMBL619793
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Displacement of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor in rat brain cortical membranes
17
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094116) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.82 | 10.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333737 | — | — | 1 | 10.12 |
| CHEMBL122904 | — | — | 1 | 9.72 |
| CHEMBL333466 | — | — | 1 | 9.64 |
| CHEMBL332242 | — | — | 3 | 9.60 |
| CHEMBL122903 | — | — | 1 | 9.55 |
| CHEMBL421424 | — | — | 1 | 9.48 |
| CHEMBL332767 | — | — | 3 | 9.19 |
| CHEMBL331234 | — | — | 1 | 9.11 |
| CHEMBL123643 | — | — | 1 | 8.96 |
| CHEMBL123010 | — | — | 1 | 8.89 |
| CHEMBL46 | ONDANSETRON | 4.0 | 2 | 8.80 |
| CHEMBL2103778 | CILANSETRON | 2.0 | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333737 | — | Ki | = | 0.075 | nM | 10.12 |
| CHEMBL122904 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL333466 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL332242 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL122903 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL421424 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL332767 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL332767 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL331234 | — | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL332242 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL332767 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL332242 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL123643 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL123010 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL46 | ONDANSETRON | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL46 | ONDANSETRON | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL2103778 | CILANSETRON | Ki | = | 5600.0 | nM | 5.25 |