Assay Detail
Binding
CHEMBL2188202
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Displacement of [3H]GR113808 from human recombinant 5HT4R expressed in HEK293T cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| 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 | 21 | 7.76 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2181189 | — | — | 1 | 8.51 |
| CHEMBL2181188 | — | — | 1 | 8.30 |
| CHEMBL2181171 | — | — | 1 | 8.12 |
| CHEMBL2181187 | — | — | 1 | 7.77 |
| CHEMBL2181185 | — | — | 1 | 7.48 |
| CHEMBL2181172 | — | — | 1 | 6.39 |
| CHEMBL2181173 | — | — | 1 | - |
| CHEMBL2181174 | — | — | 1 | - |
| CHEMBL2181175 | — | — | 1 | - |
| CHEMBL2181176 | — | — | 1 | - |
| CHEMBL2181177 | — | — | 1 | - |
| CHEMBL2181190 | — | — | 1 | - |
| CHEMBL2181186 | — | — | 1 | - |
| CHEMBL2181184 | — | — | 1 | - |
| CHEMBL2181183 | — | — | 1 | - |
| CHEMBL2177145 | — | — | 1 | - |
| CHEMBL2181181 | — | — | 1 | - |
| CHEMBL2181180 | — | — | 1 | - |
| CHEMBL2181179 | — | — | 1 | - |
| CHEMBL2181178 | — | — | 1 | - |
| CHEMBL2181182 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2181189 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL2181188 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2181171 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL2181187 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2181185 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL2181172 | — | Ki | = | 403.0 | nM | 6.39 |
| CHEMBL2181173 | — | Ki | - | — | - | |
| CHEMBL2181174 | — | Ki | - | — | - | |
| CHEMBL2181175 | — | Ki | - | — | - | |
| CHEMBL2181176 | — | Ki | - | — | - | |
| CHEMBL2181177 | — | Ki | - | — | - | |
| CHEMBL2181190 | — | Ki | - | — | - | |
| CHEMBL2181186 | — | Ki | - | — | - | |
| CHEMBL2181184 | — | Ki | - | — | - | |
| CHEMBL2181183 | — | Ki | - | — | - | |
| CHEMBL2177145 | — | Ki | - | — | - | |
| CHEMBL2181181 | — | Ki | - | — | - | |
| CHEMBL2181180 | — | Ki | - | — | - | |
| CHEMBL2181179 | — | Ki | - | — | - | |
| CHEMBL2181178 | — | Ki | - | — | - | |
| CHEMBL2181182 | — | Ki | - | — | - |