Assay Detail
Functional
CHEMBL2184351
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Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and pharmacological profile of new 1H-indazole-3-carboxamide and 2H-pyrrolo[3,4-c]quinoline derivatives as selective serotonin 4 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kb | 3 | - | - |
| IC50 | 3 | 8.75 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL33884 | — | — | 2 | 9.68 |
| CHEMBL2179674 | — | — | 2 | 8.55 |
| CHEMBL2179707 | — | — | 2 | 8.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL33884 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL2179674 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL2179707 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL33884 | — | Kb | = | 0.03 | nM | - |
| CHEMBL2179674 | — | Kb | = | 0.41 | nM | - |
| CHEMBL2179707 | — | Kb | = | 1.4 | nM | - |