Assay Detail
Binding
CHEMBL2188201
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Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
26
Total Activities
26
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
Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.32 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2181170 | — | — | 1 | 8.66 |
| CHEMBL2181166 | — | — | 1 | 8.60 |
| CHEMBL2181168 | — | — | 1 | 8.34 |
| CHEMBL2181171 | — | — | 1 | 7.88 |
| CHEMBL2181169 | — | — | 1 | 7.87 |
| CHEMBL2181189 | — | — | 1 | 7.70 |
| CHEMBL2181190 | — | — | 1 | 7.67 |
| CHEMBL2181188 | — | — | 1 | 7.66 |
| CHEMBL2181172 | — | — | 1 | 7.64 |
| CHEMBL2181187 | — | — | 1 | 7.46 |
| CHEMBL2177145 | — | — | 1 | 7.29 |
| CHEMBL2181185 | — | — | 1 | 7.00 |
| CHEMBL2181186 | — | — | 1 | 7.00 |
| CHEMBL2181167 | — | — | 1 | 6.94 |
| CHEMBL2181175 | — | — | 1 | 6.81 |
| CHEMBL2181173 | — | — | 1 | 6.68 |
| CHEMBL2181181 | — | — | 1 | 6.63 |
| CHEMBL2181180 | — | — | 1 | 6.61 |
| CHEMBL2181184 | — | — | 1 | 6.16 |
| CHEMBL2181183 | — | — | 1 | 5.72 |
| CHEMBL2181174 | — | — | 1 | - |
| CHEMBL2181178 | — | — | 1 | - |
| CHEMBL2181179 | — | — | 1 | - |
| CHEMBL2181182 | — | — | 1 | - |
| CHEMBL2181177 | — | — | 1 | - |
| CHEMBL2181176 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2181170 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL2181166 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL2181168 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL2181171 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL2181169 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL2181189 | — | Ki | = | 20.1 | nM | 7.70 |
| CHEMBL2181190 | — | Ki | = | 21.6 | nM | 7.67 |
| CHEMBL2181188 | — | Ki | = | 21.9 | nM | 7.66 |
| CHEMBL2181172 | — | Ki | = | 22.8 | nM | 7.64 |
| CHEMBL2181187 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL2177145 | — | Ki | = | 51.5 | nM | 7.29 |
| CHEMBL2181185 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL2181186 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2181167 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL2181175 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL2181173 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL2181181 | — | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL2181180 | — | Ki | = | 246.0 | nM | 6.61 |
| CHEMBL2181184 | — | Ki | = | 691.0 | nM | 6.16 |
| CHEMBL2181183 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL2181174 | — | Ki | - | — | - | |
| CHEMBL2181178 | — | Ki | - | — | - | |
| CHEMBL2181179 | — | Ki | - | — | - | |
| CHEMBL2181182 | — | Ki | - | — | - | |
| CHEMBL2181177 | — | Ki | - | — | - | |
| CHEMBL2181176 | — | Ki | - | — | - |