Assay Detail
Binding
CHEMBL662464
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Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type B receptor from rat cerebral cortex membrane
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL3508) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.09 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 8.25 |
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | 6.16 |
| CHEMBL2112823 | — | — | 1 | 5.46 |
| CHEMBL140320 | — | — | 1 | 5.36 |
| CHEMBL332261 | — | — | 1 | 5.21 |
| CHEMBL143270 | — | — | 1 | - |
| CHEMBL1794878 | — | — | 1 | - |
| CHEMBL2112828 | — | — | 1 | - |
| CHEMBL2111993 | — | — | 1 | - |
| CHEMBL342912 | — | — | 1 | - |
| CHEMBL337362 | — | — | 1 | - |
| CHEMBL139779 | — | — | 1 | - |
| CHEMBL2112273 | — | — | 1 | - |
| CHEMBL113718 | IQM-95333 | — | 1 | - |
| CHEMBL2112824 | — | — | 1 | - |
| CHEMBL140262 | — | — | 1 | - |
| CHEMBL140098 | — | — | 1 | - |
| CHEMBL2112829 | — | — | 1 | - |
| CHEMBL143672 | — | — | 1 | - |
| CHEMBL3350871 | — | — | 1 | - |
| CHEMBL343560 | — | — | 1 | - |
| CHEMBL2112825 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL9506 | DEVAZEPIDE | IC50 | = | 696.0 | nM | 6.16 |
| CHEMBL2112823 | — | IC50 | = | 3430.0 | nM | 5.46 |
| CHEMBL140320 | — | IC50 | = | 4390.0 | nM | 5.36 |
| CHEMBL332261 | — | IC50 | = | 6153.0 | nM | 5.21 |
| CHEMBL143270 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1794878 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2112828 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2111993 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL342912 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL337362 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL139779 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2112273 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL113718 | IQM-95333 | IC50 | > | 10000.0 | nM | - |
| CHEMBL2112824 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL140262 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL140098 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2112829 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL143672 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3350871 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL343560 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2112825 | — | IC50 | > | 10000.0 | nM | - |