Assay Detail
Binding
CHEMBL1273772
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Cholecystokinin receptor type A (CHEMBL2871) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.87 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1269261 | — | — | 1 | 8.70 |
| CHEMBL1269258 | CE-326597 | 2.0 | 1 | 7.91 |
| CHEMBL1269260 | — | — | 1 | 7.77 |
| CHEMBL1269263 | — | — | 1 | 7.68 |
| CHEMBL1269257 | — | — | 1 | 7.28 |
| CHEMBL1269262 | — | — | 1 | - |
| CHEMBL1269264 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1269261 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1269258 | CE-326597 | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL1269260 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1269263 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1269257 | — | IC50 | = | 52.6 | nM | 7.28 |
| CHEMBL1269262 | — | IC50 | - | — | - | |
| CHEMBL1269264 | — | IC50 | - | — | - |