Assay Detail
Binding
CHEMBL889350
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC-3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
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 | 20 | 5.55 | 6.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL227369 | — | — | 1 | 6.43 |
| CHEMBL389639 | — | — | 1 | 6.19 |
| CHEMBL374388 | — | — | 1 | 5.72 |
| CHEMBL374390 | — | — | 1 | 5.53 |
| CHEMBL226729 | — | — | 1 | 5.39 |
| CHEMBL227147 | — | — | 1 | 5.24 |
| CHEMBL227254 | — | — | 1 | 5.19 |
| CHEMBL389019 | — | — | 1 | 5.15 |
| CHEMBL559157 | — | — | 1 | 5.07 |
| CHEMBL390275 | — | — | 1 | - |
| CHEMBL269790 | — | — | 1 | - |
| CHEMBL226571 | — | — | 1 | - |
| CHEMBL226570 | — | — | 1 | - |
| CHEMBL227097 | — | — | 1 | - |
| CHEMBL226620 | — | — | 1 | - |
| CHEMBL390276 | — | — | 1 | - |
| CHEMBL226673 | — | — | 1 | - |
| CHEMBL374389 | — | — | 1 | - |
| CHEMBL205455 | — | — | 1 | - |
| CHEMBL390519 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL227369 | — | Ki | = | 371.54 | nM | 6.43 |
| CHEMBL389639 | — | Ki | = | 645.65 | nM | 6.19 |
| CHEMBL374388 | — | Ki | = | 1905.46 | nM | 5.72 |
| CHEMBL374390 | — | Ki | = | 2951.21 | nM | 5.53 |
| CHEMBL226729 | — | Ki | = | 4073.8 | nM | 5.39 |
| CHEMBL227147 | — | Ki | = | 5754.4 | nM | 5.24 |
| CHEMBL227254 | — | Ki | = | 6456.54 | nM | 5.19 |
| CHEMBL389019 | — | Ki | = | 7079.46 | nM | 5.15 |
| CHEMBL559157 | — | Ki | = | 8511.38 | nM | 5.07 |
| CHEMBL390275 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL269790 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL226571 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL226570 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL227097 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL226620 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL390276 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL226673 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL374389 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL205455 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL390519 | — | Ki | < | 10000.0 | nM | - |