Assay Detail
Binding
CHEMBL3095863
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Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design of fluorinated 5-HT(4)R antagonists: influence of the basicity and lipophilicity toward the 5-HT(4)R binding affinities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.83 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2181170 | — | — | 1 | 8.66 |
| CHEMBL3093187 | — | — | 1 | 8.38 |
| CHEMBL3093186 | — | — | 1 | 8.05 |
| CHEMBL3093184 | — | — | 1 | 7.85 |
| CHEMBL2181189 | — | — | 1 | 7.70 |
| CHEMBL3093194 | — | — | 1 | 7.66 |
| CHEMBL2177145 | — | — | 1 | 7.29 |
| CHEMBL3093185 | — | — | 1 | 7.04 |
| CHEMBL3093193 | — | — | 1 | - |
| CHEMBL3093192 | — | — | 1 | - |
| CHEMBL3093191 | — | — | 1 | - |
| CHEMBL3093190 | — | — | 1 | - |
| CHEMBL3093189 | — | — | 1 | - |
| CHEMBL3093188 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2181170 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3093187 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3093186 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3093184 | — | Ki | = | 14.1 | nM | 7.85 |
| CHEMBL2181189 | — | Ki | = | 20.1 | nM | 7.70 |
| CHEMBL3093194 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2177145 | — | Ki | = | 51.5 | nM | 7.29 |
| CHEMBL3093185 | — | Ki | = | 91.4 | nM | 7.04 |
| CHEMBL3093193 | — | Ki | - | — | - | |
| CHEMBL3093192 | — | Ki | - | — | - | |
| CHEMBL3093191 | — | Ki | - | — | - | |
| CHEMBL3093190 | — | Ki | - | — | - | |
| CHEMBL3093189 | — | Ki | - | — | - | |
| CHEMBL3093188 | — | Ki | - | — | - |