Assay Detail
Binding
CHEMBL1065651
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Displacement of [3H]granisetron from human 5HT3A receptor expressed in HEK293 cells by scintillation counting
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Toward biophysical probes for the 5-HT3 receptor: structure-activity relationship study of granisetron derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.52 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL596951 | — | — | 1 | 9.77 |
| CHEMBL605772 | — | — | 1 | 9.64 |
| CHEMBL599011 | — | — | 1 | 9.17 |
| CHEMBL289469 | GRANISETRON | 4.0 | 1 | 8.84 |
| CHEMBL2309589 | — | — | 1 | 8.72 |
| CHEMBL598804 | — | — | 1 | 8.14 |
| CHEMBL596952 | — | — | 1 | 7.58 |
| CHEMBL597984 | — | — | 1 | 7.23 |
| CHEMBL599012 | — | — | 1 | 7.15 |
| CHEMBL596758 | — | — | 1 | 6.62 |
| CHEMBL603673 | — | — | 1 | 6.55 |
| CHEMBL598803 | — | — | 1 | 6.43 |
| CHEMBL604083 | — | — | 1 | 6.13 |
| CHEMBL598805 | — | — | 1 | 5.52 |
| CHEMBL605562 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL596951 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL605772 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL599011 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL289469 | GRANISETRON | Ki | = | 1.45 | nM | 8.84 |
| CHEMBL2309589 | — | Ki | = | 1.89 | nM | 8.72 |
| CHEMBL598804 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL596952 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL597984 | — | Ki | = | 59.3 | nM | 7.23 |
| CHEMBL599012 | — | Ki | = | 71.1 | nM | 7.15 |
| CHEMBL596758 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL603673 | — | Ki | = | 279.0 | nM | 6.55 |
| CHEMBL598803 | — | Ki | = | 375.0 | nM | 6.43 |
| CHEMBL604083 | — | Ki | = | 749.0 | nM | 6.13 |
| CHEMBL598805 | — | Ki | = | 3029.0 | nM | 5.52 |
| CHEMBL605562 | — | Ki | = | 5306.0 | nM | 5.28 |