Assay Detail
Functional
CHEMBL889352
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CCK2 receptor in perfused rat stomach assessed as inhibition of pentagastrin-stimulated gastric acid secretion
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Stomach |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL3508) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 |
|---|---|---|---|
| Kd | 16 | 8.65 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL324547 | NETAZEPIDE | 2.0 | 1 | 10.10 |
| CHEMBL387948 | — | — | 1 | 9.13 |
| CHEMBL389711 | — | — | 1 | 9.07 |
| CHEMBL390519 | — | — | 1 | 9.06 |
| CHEMBL205455 | — | — | 1 | 9.01 |
| CHEMBL227330 | — | — | 1 | 8.91 |
| CHEMBL227333 | — | — | 1 | 8.83 |
| CHEMBL227276 | — | — | 1 | 8.74 |
| CHEMBL226620 | — | — | 1 | 8.71 |
| CHEMBL389639 | — | — | 1 | 8.56 |
| CHEMBL226675 | — | — | 1 | 8.35 |
| CHEMBL390276 | — | — | 1 | 8.12 |
| CHEMBL226533 | — | — | 1 | 8.11 |
| CHEMBL226583 | — | — | 1 | 8.02 |
| CHEMBL226673 | — | — | 1 | 8.01 |
| CHEMBL227254 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL324547 | NETAZEPIDE | Kd | = | 0.07943 | nM | 10.10 |
| CHEMBL387948 | — | Kd | = | 0.7413 | nM | 9.13 |
| CHEMBL389711 | — | Kd | = | 0.8511 | nM | 9.07 |
| CHEMBL390519 | — | Kd | = | 0.871 | nM | 9.06 |
| CHEMBL205455 | — | Kd | = | 0.9772 | nM | 9.01 |
| CHEMBL227330 | — | Kd | = | 1.23 | nM | 8.91 |
| CHEMBL227333 | — | Kd | = | 1.479 | nM | 8.83 |
| CHEMBL227276 | — | Kd | = | 1.82 | nM | 8.74 |
| CHEMBL226620 | — | Kd | = | 1.95 | nM | 8.71 |
| CHEMBL389639 | — | Kd | = | 2.754 | nM | 8.56 |
| CHEMBL226675 | — | Kd | = | 4.467 | nM | 8.35 |
| CHEMBL390276 | — | Kd | = | 7.586 | nM | 8.12 |
| CHEMBL226533 | — | Kd | = | 7.762 | nM | 8.11 |
| CHEMBL226583 | — | Kd | = | 9.55 | nM | 8.02 |
| CHEMBL226673 | — | Kd | = | 9.772 | nM | 8.01 |
| CHEMBL227254 | — | Kd | = | 23.99 | nM | 7.62 |