Assay Detail
Binding
CHEMBL661840
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Evaluated for inhibition of cholecystokinin type B receptor by displacing [125I]-Bolton hunter CCK-8 radioligand in the mouse cerebral cortex
19
Total Activities
19
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 (CHEMBL2854) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Rationally designed "dipeptoid" analogues of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist CI-988.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.11 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 9.52 |
| CHEMBL1328 | PENTAGASTRIN | 4.0 | 1 | 9.10 |
| CHEMBL2112338 | — | — | 1 | 8.89 |
| CHEMBL263969 | — | — | 1 | 8.77 |
| CHEMBL2112330 | — | — | 1 | 8.60 |
| CHEMBL2112333 | — | — | 1 | 8.37 |
| CHEMBL9387 | L-365260 | — | 1 | 8.29 |
| CHEMBL88090 | — | — | 1 | 8.22 |
| CHEMBL85607 | — | — | 1 | 8.20 |
| CHEMBL83244 | — | — | 1 | 7.92 |
| CHEMBL87470 | — | — | 1 | 7.92 |
| CHEMBL313499 | — | — | 1 | 7.85 |
| CHEMBL407857 | — | — | 1 | 7.80 |
| CHEMBL312894 | — | — | 1 | 7.68 |
| CHEMBL314178 | — | — | 1 | 7.64 |
| CHEMBL433148 | — | — | 1 | 7.64 |
| CHEMBL315055 | — | — | 1 | 7.57 |
| CHEMBL86879 | — | — | 1 | 7.10 |
| CHEMBL313559 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1328 | PENTAGASTRIN | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL2112338 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL263969 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2112330 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2112333 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL9387 | L-365260 | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL88090 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL85607 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL83244 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL87470 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL313499 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL407857 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL312894 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL314178 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL433148 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL315055 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL86879 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL313559 | — | IC50 | = | 110.0 | nM | 6.96 |