Assay Detail
Functional
CHEMBL889353
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]BH-CCK8-8S from CCK2 receptor in canine gastric mucosa
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Canis lupus familiaris |
| Tissue | Gastric mucosa |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL5595) ↗| Type | SINGLE PROTEIN |
| Organism | Canis lupus familiaris |
Publication
Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.22 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL389711 | — | — | 1 | 8.62 |
| CHEMBL226533 | — | — | 1 | 8.50 |
| CHEMBL227330 | — | — | 1 | 8.37 |
| CHEMBL227276 | — | — | 1 | 8.35 |
| CHEMBL226583 | — | — | 1 | 8.35 |
| CHEMBL227254 | — | — | 1 | 8.33 |
| CHEMBL227333 | — | — | 1 | 8.32 |
| CHEMBL226673 | — | — | 1 | 8.28 |
| CHEMBL389639 | — | — | 1 | 8.24 |
| CHEMBL387948 | — | — | 1 | 8.20 |
| CHEMBL226620 | — | — | 1 | 8.15 |
| CHEMBL390519 | — | — | 1 | 7.94 |
| CHEMBL205455 | — | — | 1 | 7.91 |
| CHEMBL390276 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL389711 | — | Ki | = | 2.399 | nM | 8.62 |
| CHEMBL226533 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL227330 | — | Ki | = | 4.266 | nM | 8.37 |
| CHEMBL227276 | — | Ki | = | 4.467 | nM | 8.35 |
| CHEMBL226583 | — | Ki | = | 4.467 | nM | 8.35 |
| CHEMBL227254 | — | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL227333 | — | Ki | = | 4.786 | nM | 8.32 |
| CHEMBL226673 | — | Ki | = | 5.248 | nM | 8.28 |
| CHEMBL389639 | — | Ki | = | 5.754 | nM | 8.24 |
| CHEMBL387948 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL226620 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL390519 | — | Ki | = | 11.48 | nM | 7.94 |
| CHEMBL205455 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL390276 | — | Ki | = | 26.3 | nM | 7.58 |