Assay Detail
Binding
CHEMBL620725
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against 5-hydroxytryptamine 3 (5-HT3) receptor in rat brain cortical membranes using radioligand [3H]quipazine
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094116) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
2-(Quinuclidin-3-yl)pyrido[4,3-b]indol-1-ones and isoquinolin-1-ones. Potent conformationally restricted 5-HT3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 8.49 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1720 | PALONOSETRON HYDROCHLORIDE | 4.0 | 1 | 10.40 |
| CHEMBL540055 | — | — | 1 | 9.80 |
| CHEMBL544784 | — | — | 1 | 9.80 |
| CHEMBL542669 | — | — | 1 | 9.70 |
| CHEMBL542904 | — | — | 1 | 9.70 |
| CHEMBL542900 | — | — | 1 | 9.70 |
| CHEMBL28992 | — | — | 1 | 9.60 |
| CHEMBL555068 | — | — | 1 | 9.50 |
| CHEMBL540057 | — | — | 1 | 9.50 |
| CHEMBL2093898 | — | — | 1 | 9.40 |
| CHEMBL542903 | — | — | 1 | 9.40 |
| CHEMBL545719 | — | — | 1 | 9.20 |
| CHEMBL555038 | — | — | 1 | 9.20 |
| CHEMBL289469 | GRANISETRON | 4.0 | 1 | 9.10 |
| CHEMBL88565 | — | — | 1 | 9.10 |
| CHEMBL539020 | — | — | 1 | 9.00 |
| CHEMBL56564 | TROPISETRON | 3.0 | 1 | 8.70 |
| CHEMBL555199 | — | — | 1 | 8.70 |
| CHEMBL540040 | — | — | 1 | 8.60 |
| CHEMBL544785 | — | — | 1 | 8.60 |
| CHEMBL540568 | — | — | 1 | 8.60 |
| CHEMBL553733 | — | — | 1 | 8.60 |
| CHEMBL545717 | — | — | 1 | 8.60 |
| CHEMBL27846 | (R)ZACOPRIDE | — | 1 | 8.50 |
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | 8.50 |
| CHEMBL540820 | — | — | 1 | 8.40 |
| CHEMBL543136 | — | — | 1 | 8.40 |
| CHEMBL555582 | — | — | 1 | 8.30 |
| CHEMBL315518 | — | — | 1 | 8.30 |
| CHEMBL540547 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1720 | PALONOSETRON HYDROCHLORIDE | Ki | = | 0.03981 | nM | 10.40 |
| CHEMBL540055 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL544784 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL542669 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL542904 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL542900 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL28992 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL555068 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL540057 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL2093898 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL542903 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL545719 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL555038 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL289469 | GRANISETRON | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL88565 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL539020 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL56564 | TROPISETRON | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL555199 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL545717 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL553733 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL544785 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL540040 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL540568 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL27846 | (R)ZACOPRIDE | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL46 | ONDANSETRON | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL540820 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL543136 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL555582 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL315518 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL540547 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL539275 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL539785 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL554341 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL554259 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL540823 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL541844 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL538027 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL555523 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL542668 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL555402 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL541843 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL538775 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL555080 | — | Ki | = | 630.96 | nM | 6.20 |