Assay Detail
Binding
CHEMBL863065
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]CCK-8(SO3) from human CCK2 receptor expressed in HEK293 cells
33
Total Activities
17
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL298) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.70 | 9.66 |
| Ki | 16 | 7.70 | 9.66 |
| Log IC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL382409 | — | — | 2 | 9.66 |
| CHEMBL218327 | — | — | 2 | 8.96 |
| CHEMBL206974 | — | — | 2 | 8.82 |
| CHEMBL382349 | — | — | 2 | 8.80 |
| CHEMBL407057 | — | — | 2 | 8.68 |
| CHEMBL205965 | — | — | 2 | 8.57 |
| CHEMBL408330 | — | — | 2 | 8.42 |
| CHEMBL336381 | — | — | 2 | 8.32 |
| CHEMBL208479 | — | — | 2 | 7.82 |
| CHEMBL218763 | — | — | 2 | 7.82 |
| CHEMBL382051 | — | — | 2 | 7.59 |
| CHEMBL262172 | — | — | 2 | 6.84 |
| CHEMBL408083 | — | — | 2 | 5.96 |
| CHEMBL379405 | — | — | 2 | 5.77 |
| CHEMBL205306 | — | — | 2 | 5.66 |
| CHEMBL383458 | — | — | 2 | 5.57 |
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL382409 | — | IC50 | = | 0.2188 | nM | 9.66 |
| CHEMBL382409 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL218327 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL218327 | — | IC50 | = | 1.096 | nM | 8.96 |
| CHEMBL206974 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL206974 | — | IC50 | = | 1.549 | nM | 8.81 |
| CHEMBL382349 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL382349 | — | IC50 | = | 1.622 | nM | 8.79 |
| CHEMBL407057 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL407057 | — | IC50 | = | 2.138 | nM | 8.67 |
| CHEMBL205965 | — | IC50 | = | 2.692 | nM | 8.57 |
| CHEMBL205965 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL408330 | — | IC50 | = | 3.802 | nM | 8.42 |
| CHEMBL408330 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL336381 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL336381 | — | IC50 | = | 4.786 | nM | 8.32 |
| CHEMBL208479 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL218763 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL208479 | — | IC50 | = | 15.14 | nM | 7.82 |
| CHEMBL218763 | — | IC50 | = | 15.14 | nM | 7.82 |
| CHEMBL382051 | — | IC50 | = | 25.7 | nM | 7.59 |
| CHEMBL382051 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL262172 | — | IC50 | = | 144.54 | nM | 6.84 |
| CHEMBL262172 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL408083 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL408083 | — | IC50 | = | 1096.48 | nM | 5.96 |
| CHEMBL379405 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL379405 | — | IC50 | = | 1737.8 | nM | 5.76 |
| CHEMBL205306 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL205306 | — | IC50 | = | 2187.76 | nM | 5.66 |
| CHEMBL383458 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL383458 | — | IC50 | = | 2691.53 | nM | 5.57 |
| CHEMBL1121 | SINCALIDE | Log IC50 | - | — | - |