Assay Detail
Binding
CHEMBL2184357
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells
25
Total Activities
25
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
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 |
|---|---|---|---|
| Ki | 25 | 8.71 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177130 | — | — | 1 | 10.10 |
| CHEMBL2179697 | — | — | 1 | 10.00 |
| CHEMBL356359 | PIBOSEROD | 2.0 | 1 | 9.80 |
| CHEMBL2179699 | — | — | 1 | 9.80 |
| CHEMBL3216126 | — | — | 1 | 9.70 |
| CHEMBL2179704 | — | — | 1 | 9.60 |
| CHEMBL2179702 | — | — | 1 | 9.50 |
| CHEMBL3215681 | — | — | 1 | 9.40 |
| CHEMBL2179703 | — | — | 1 | 9.30 |
| CHEMBL2179696 | — | — | 1 | 9.20 |
| CHEMBL2179701 | — | — | 1 | 9.10 |
| CHEMBL2179707 | — | — | 1 | 9.10 |
| CHEMBL2179705 | — | — | 1 | 8.90 |
| CHEMBL2179674 | — | — | 1 | 8.70 |
| CHEMBL2179678 | — | — | 1 | 8.70 |
| CHEMBL2179670 | — | — | 1 | 8.70 |
| CHEMBL2179676 | — | — | 1 | 8.60 |
| CHEMBL2179675 | — | — | 1 | 8.30 |
| CHEMBL2179679 | — | — | 1 | 8.10 |
| CHEMBL2179672 | — | — | 1 | 8.00 |
| CHEMBL2179671 | — | — | 1 | 7.70 |
| CHEMBL2179698 | — | — | 1 | 7.50 |
| CHEMBL2179677 | — | — | 1 | 6.90 |
| CHEMBL2179673 | — | — | 1 | 6.70 |
| CHEMBL2179680 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177130 | — | Ki | = | 0.07943 | nM | 10.10 |
| CHEMBL2179697 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL356359 | PIBOSEROD | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL2179699 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL3216126 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL2179704 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL2179702 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL3215681 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL2179703 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL2179696 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL2179701 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL2179707 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL2179705 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL2179674 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL2179678 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL2179670 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL2179676 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL2179675 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL2179679 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL2179672 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2179671 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL2179698 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL2179677 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL2179673 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL2179680 | — | Ki | = | 398.11 | nM | 6.40 |