Assay Detail
Binding
CHEMBL619077
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Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
2,3-Dihydro-2-oxo-1H-benzimidazole-1-carboxamides with selective affinity for the 5-HT(4) receptor: synthesis and structure-affinity and structure-activity relationships of a new series of partial agonist and antagonist derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.36 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL33884 | — | — | 1 | 9.96 |
| CHEMBL97019 | — | — | 1 | 8.17 |
| CHEMBL95661 | — | — | 1 | 8.09 |
| CHEMBL99590 | — | — | 1 | 7.99 |
| CHEMBL97755 | — | — | 1 | 7.88 |
| CHEMBL100199 | — | — | 1 | 7.77 |
| CHEMBL318764 | — | — | 1 | 7.75 |
| CHEMBL99147 | — | — | 1 | 7.60 |
| CHEMBL93611 | — | — | 1 | 7.47 |
| CHEMBL319886 | — | — | 1 | 7.41 |
| CHEMBL99723 | — | — | 1 | 7.40 |
| CHEMBL99452 | — | — | 1 | 7.31 |
| CHEMBL99299 | — | — | 1 | 7.25 |
| CHEMBL59834 | — | — | 1 | 7.19 |
| CHEMBL95968 | — | — | 1 | 7.18 |
| CHEMBL97903 | — | — | 1 | 7.16 |
| CHEMBL99515 | — | — | 1 | 7.12 |
| CHEMBL95808 | — | — | 1 | 7.06 |
| CHEMBL95235 | — | — | 1 | 7.05 |
| CHEMBL99591 | — | — | 1 | 7.04 |
| CHEMBL100317 | — | — | 1 | 6.99 |
| CHEMBL100088 | — | — | 1 | 6.96 |
| CHEMBL317146 | — | — | 1 | 6.67 |
| CHEMBL97508 | — | — | 1 | 6.60 |
| CHEMBL99141 | — | — | 1 | 6.58 |
| CHEMBL99578 | — | — | 1 | 6.51 |
| CHEMBL421187 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL33884 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL97019 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL95661 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL99590 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL97755 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL100199 | — | Ki | = | 16.9 | nM | 7.77 |
| CHEMBL318764 | — | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL99147 | — | Ki | = | 25.2 | nM | 7.60 |
| CHEMBL93611 | — | Ki | = | 34.1 | nM | 7.47 |
| CHEMBL319886 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL99723 | — | Ki | = | 39.7 | nM | 7.40 |
| CHEMBL99452 | — | Ki | = | 49.4 | nM | 7.31 |
| CHEMBL99299 | — | Ki | = | 56.3 | nM | 7.25 |
| CHEMBL59834 | — | Ki | = | 63.9 | nM | 7.19 |
| CHEMBL95968 | — | Ki | = | 66.3 | nM | 7.18 |
| CHEMBL97903 | — | Ki | = | 68.5 | nM | 7.16 |
| CHEMBL99515 | — | Ki | = | 75.4 | nM | 7.12 |
| CHEMBL95808 | — | Ki | = | 87.3 | nM | 7.06 |
| CHEMBL95235 | — | Ki | = | 89.8 | nM | 7.05 |
| CHEMBL99591 | — | Ki | = | 91.1 | nM | 7.04 |
| CHEMBL100317 | — | Ki | = | 103.6 | nM | 6.99 |
| CHEMBL100088 | — | Ki | = | 108.4 | nM | 6.96 |
| CHEMBL317146 | — | Ki | = | 216.4 | nM | 6.67 |
| CHEMBL97508 | — | Ki | = | 252.9 | nM | 6.60 |
| CHEMBL99141 | — | Ki | = | 262.0 | nM | 6.58 |
| CHEMBL99578 | — | Ki | = | 305.8 | nM | 6.51 |
| CHEMBL421187 | — | Ki | = | 375.0 | nM | 6.43 |