Assay Detail
Binding
CHEMBL661969
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Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.22 | 8.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL122934 | — | — | 1 | 8.87 |
| CHEMBL331394 | — | — | 1 | 8.69 |
| CHEMBL333762 | — | — | 1 | 8.59 |
| CHEMBL100538 | — | — | 1 | 8.52 |
| CHEMBL122872 | — | — | 1 | 8.36 |
| CHEMBL334114 | — | — | 1 | 7.82 |
| CHEMBL59865 | — | — | 1 | 7.75 |
| CHEMBL119992 | — | — | 1 | 7.70 |
| CHEMBL411271 | — | — | 1 | 7.02 |
| CHEMBL177799 | — | — | 1 | 5.66 |
| CHEMBL408389 | — | — | 1 | 5.54 |
| CHEMBL64605 | — | — | 1 | 4.92 |
| CHEMBL120632 | TETRAGASTRIN | -1.0 | 1 | 4.44 |
| CHEMBL262197 | — | — | 1 | - |
| CHEMBL333477 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL122934 | — | Ki | = | 1.35 | nM | 8.87 |
| CHEMBL331394 | — | Ki | = | 2.05 | nM | 8.69 |
| CHEMBL333762 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL100538 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL122872 | — | Ki | = | 4.35 | nM | 8.36 |
| CHEMBL334114 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL59865 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL119992 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL411271 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL177799 | — | Ki | = | 2210.0 | nM | 5.66 |
| CHEMBL408389 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL64605 | — | Ki | = | 11900.0 | nM | 4.92 |
| CHEMBL120632 | TETRAGASTRIN | Ki | = | 36133.0 | nM | 4.44 |
| CHEMBL262197 | — | Ki | > | 0.7 | nM | - |
| CHEMBL333477 | — | Ki | > | 0.7 | nM | - |