Assay Detail
Binding
CHEMBL659590
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Inhibition of [3H]- pCCK-8 binding to Cholecystokinin type B receptor of rat cerebral cortex membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL3508) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.28 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 8.55 |
| CHEMBL419764 | — | — | 1 | 6.47 |
| CHEMBL325070 | — | — | 1 | 5.81 |
| CHEMBL324294 | — | — | 1 | 5.72 |
| CHEMBL431858 | — | — | 1 | 5.56 |
| CHEMBL113718 | IQM-95333 | — | 1 | 5.54 |
| CHEMBL116001 | — | — | 1 | - |
| CHEMBL116127 | — | — | 1 | - |
| CHEMBL113699 | — | — | 1 | - |
| CHEMBL326064 | — | — | 1 | - |
| CHEMBL114517 | — | — | 1 | - |
| CHEMBL332261 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL419764 | — | Ki | = | 342.0 | nM | 6.47 |
| CHEMBL325070 | — | Ki | = | 1560.0 | nM | 5.81 |
| CHEMBL324294 | — | Ki | = | 1890.0 | nM | 5.72 |
| CHEMBL431858 | — | Ki | = | 2730.0 | nM | 5.56 |
| CHEMBL113718 | IQM-95333 | Ki | = | 2910.0 | nM | 5.54 |
| CHEMBL116001 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL116127 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL113699 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL326064 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL114517 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL332261 | — | Ki | > | 5000.0 | nM | - |