Assay Detail
Binding
CHEMBL663086
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Binding affinity against cholecystokinin type B receptor on guinea pig cortex.
35
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL298) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 35 | 7.84 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL411271 | — | — | 1 | 9.82 |
| CHEMBL262197 | — | — | 1 | 9.55 |
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 9.52 |
| CHEMBL120150 | — | — | 1 | 9.27 |
| CHEMBL333477 | — | — | 1 | 9.10 |
| CHEMBL118610 | — | — | 1 | 8.86 |
| CHEMBL120827 | — | — | 1 | 8.74 |
| CHEMBL261934 | — | — | 1 | 8.60 |
| CHEMBL339421 | — | — | 1 | 8.57 |
| CHEMBL321456 | — | — | 1 | 8.44 |
| CHEMBL120335 | — | — | 1 | 8.42 |
| CHEMBL333516 | — | — | 1 | 8.39 |
| CHEMBL331517 | — | — | 1 | 8.32 |
| CHEMBL408389 | — | — | 1 | 8.19 |
| CHEMBL330785 | — | — | 1 | 8.14 |
| CHEMBL120452 | — | — | 1 | 8.11 |
| CHEMBL120528 | — | — | 1 | 7.92 |
| CHEMBL177799 | — | — | 1 | 7.82 |
| CHEMBL120632 | TETRAGASTRIN | -1.0 | 1 | 7.71 |
| CHEMBL123056 | — | — | 1 | 7.62 |
| CHEMBL64605 | — | — | 1 | 7.38 |
| CHEMBL122012 | — | — | 1 | 7.02 |
| CHEMBL332180 | — | — | 1 | 6.64 |
| CHEMBL119960 | — | — | 1 | 6.00 |
| CHEMBL431676 | — | — | 1 | 5.84 |
| CHEMBL120401 | — | — | 2 | 5.48 |
| CHEMBL122934 | — | — | 1 | 5.33 |
| CHEMBL331394 | — | — | 1 | 4.64 |
| CHEMBL59865 | — | — | 1 | - |
| CHEMBL100538 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL411271 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL262197 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL1121 | SINCALIDE | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL120150 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL333477 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL118610 | — | Ki | = | 1.37 | nM | 8.86 |
| CHEMBL120827 | — | Ki | = | 1.81 | nM | 8.74 |
| CHEMBL261934 | — | Ki | = | 2.52 | nM | 8.60 |
| CHEMBL339421 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL321456 | — | Ki | = | 3.61 | nM | 8.44 |
| CHEMBL120335 | — | Ki | = | 3.84 | nM | 8.42 |
| CHEMBL333516 | — | Ki | = | 4.07 | nM | 8.39 |
| CHEMBL331517 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL408389 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL330785 | — | Ki | = | 7.31 | nM | 8.14 |
| CHEMBL120452 | — | Ki | = | 7.76 | nM | 8.11 |
| CHEMBL120528 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL177799 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL120632 | TETRAGASTRIN | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL123056 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL64605 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL122012 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL332180 | — | Ki | = | 228.0 | nM | 6.64 |
| CHEMBL119960 | — | Ki | = | 992.0 | nM | 6.00 |
| CHEMBL431676 | — | Ki | = | 1460.0 | nM | 5.84 |
| CHEMBL120401 | — | Ki | = | 3340.0 | nM | 5.48 |
| CHEMBL122934 | — | Ki | = | 4620.0 | nM | 5.33 |
| CHEMBL331394 | — | Ki | = | 22800.0 | nM | 4.64 |
| CHEMBL59865 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL120401 | — | Ki | = | 224.0 | — | - |
| CHEMBL100538 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL334114 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL333762 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL119992 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL122872 | — | Ki | > | 6000.0 | nM | - |