Assay Detail
Binding
CHEMBL860739
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 cell line
10
Total Activities
10
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
Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.74 | 10.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | 10.63 |
| CHEMBL324547 | NETAZEPIDE | 2.0 | 1 | 7.52 |
| CHEMBL9387 | L-365260 | — | 1 | 6.76 |
| CHEMBL379902 | — | — | 1 | 6.14 |
| CHEMBL205751 | — | — | 1 | 5.93 |
| CHEMBL205198 | — | — | 1 | 5.23 |
| CHEMBL205455 | — | — | 1 | 4.95 |
| CHEMBL206079 | — | — | 1 | - |
| CHEMBL380907 | — | — | 1 | - |
| CHEMBL204154 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9506 | DEVAZEPIDE | Ki | = | 0.02344 | nM | 10.63 |
| CHEMBL324547 | NETAZEPIDE | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL9387 | L-365260 | Ki | = | 173.78 | nM | 6.76 |
| CHEMBL379902 | — | Ki | = | 724.44 | nM | 6.14 |
| CHEMBL205751 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL205198 | — | Ki | = | 5888.44 | nM | 5.23 |
| CHEMBL205455 | — | Ki | = | 11220.18 | nM | 4.95 |
| CHEMBL206079 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL380907 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL204154 | — | Ki | < | 10000.0 | nM | - |