Assay Detail
Binding
CHEMBL2174993
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]granisetron from 5HT3A receptor expressed in HEK293 cells after 24 hrs by scintillation counting in presence of quipazine
32
Total Activities
32
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
Design, synthesis, and structure-activity relationships of highly potent 5-HT₃ receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 7.50 | 10.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475331 | — | — | 1 | 10.29 |
| CHEMBL288591 | — | — | 1 | 9.34 |
| CHEMBL489062 | — | — | 1 | 8.95 |
| CHEMBL443764 | — | — | 1 | 8.87 |
| CHEMBL2169970 | — | — | 1 | 8.84 |
| CHEMBL2169966 | — | — | 1 | 8.79 |
| CHEMBL489271 | — | — | 1 | 8.57 |
| CHEMBL454890 | — | — | 1 | 8.55 |
| CHEMBL2169965 | — | — | 1 | 8.53 |
| CHEMBL123137 | — | — | 1 | 8.33 |
| CHEMBL2169971 | — | — | 1 | 8.23 |
| CHEMBL489060 | — | — | 1 | 8.18 |
| CHEMBL2169890 | — | — | 1 | 8.13 |
| CHEMBL473302 | — | — | 1 | 7.92 |
| CHEMBL2169969 | — | — | 1 | 7.87 |
| CHEMBL490071 | — | — | 1 | 7.86 |
| CHEMBL489664 | — | — | 1 | 7.83 |
| CHEMBL511699 | — | — | 1 | 7.74 |
| CHEMBL2169964 | — | — | 1 | 7.33 |
| CHEMBL490072 | — | — | 1 | 7.10 |
| CHEMBL490073 | — | — | 1 | 6.78 |
| CHEMBL2169973 | — | — | 1 | 6.69 |
| CHEMBL2169972 | — | — | 1 | 6.66 |
| CHEMBL2169974 | — | — | 1 | 6.48 |
| CHEMBL2169967 | — | — | 1 | 6.39 |
| CHEMBL2169975 | — | — | 1 | 6.33 |
| CHEMBL2169968 | — | — | 1 | 6.27 |
| CHEMBL471712 | — | — | 1 | 6.24 |
| CHEMBL461360 | — | — | 1 | 5.63 |
| CHEMBL461729 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475331 | — | Ki | = | 0.05129 | nM | 10.29 |
| CHEMBL288591 | — | Ki | = | 0.4571 | nM | 9.34 |
| CHEMBL489062 | — | Ki | = | 1.122 | nM | 8.95 |
| CHEMBL443764 | — | Ki | = | 1.349 | nM | 8.87 |
| CHEMBL2169970 | — | Ki | = | 1.445 | nM | 8.84 |
| CHEMBL2169966 | — | Ki | = | 1.622 | nM | 8.79 |
| CHEMBL489271 | — | Ki | = | 2.692 | nM | 8.57 |
| CHEMBL454890 | — | Ki | = | 2.818 | nM | 8.55 |
| CHEMBL2169965 | — | Ki | = | 2.951 | nM | 8.53 |
| CHEMBL123137 | — | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL2169971 | — | Ki | = | 5.888 | nM | 8.23 |
| CHEMBL489060 | — | Ki | = | 6.607 | nM | 8.18 |
| CHEMBL2169890 | — | Ki | = | 7.413 | nM | 8.13 |
| CHEMBL473302 | — | Ki | = | 12.02 | nM | 7.92 |
| CHEMBL2169969 | — | Ki | = | 13.49 | nM | 7.87 |
| CHEMBL490071 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL489664 | — | Ki | = | 14.79 | nM | 7.83 |
| CHEMBL511699 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL2169964 | — | Ki | = | 46.77 | nM | 7.33 |
| CHEMBL490072 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL490073 | — | Ki | = | 165.96 | nM | 6.78 |
| CHEMBL2169973 | — | Ki | = | 204.17 | nM | 6.69 |
| CHEMBL2169972 | — | Ki | = | 218.78 | nM | 6.66 |
| CHEMBL2169974 | — | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL2169967 | — | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL2169975 | — | Ki | = | 467.74 | nM | 6.33 |
| CHEMBL2169968 | — | Ki | = | 537.03 | nM | 6.27 |
| CHEMBL471712 | — | Ki | = | 575.44 | nM | 6.24 |
| CHEMBL461360 | — | Ki | = | 2344.23 | nM | 5.63 |
| CHEMBL461729 | — | Ki | = | 3548.13 | nM | 5.45 |
| CHEMBL462417 | — | Ki | = | 11748.98 | nM | 4.93 |
| CHEMBL489061 | — | Ki | = | 16595.87 | nM | 4.78 |