Assay Detail
Binding
CHEMBL860738
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]BH-CCK-8S from human recombinant CCK2 receptor expressed in NIH3T3 cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL298) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 22 | 7.73 | 9.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL324547 | NETAZEPIDE | 2.0 | 1 | 9.86 |
| CHEMBL205455 | — | — | 1 | 8.29 |
| CHEMBL203530 | — | — | 1 | 8.26 |
| CHEMBL205831 | — | — | 1 | 8.22 |
| CHEMBL205751 | — | — | 1 | 8.22 |
| CHEMBL9387 | L-365260 | — | 1 | 8.11 |
| CHEMBL204154 | — | — | 1 | 8.10 |
| CHEMBL378098 | — | — | 1 | 8.05 |
| CHEMBL380363 | — | — | 1 | 8.04 |
| CHEMBL378388 | — | — | 1 | 7.88 |
| CHEMBL379902 | — | — | 1 | 7.88 |
| CHEMBL205198 | — | — | 1 | 7.82 |
| CHEMBL380907 | — | — | 1 | 7.80 |
| CHEMBL380193 | — | — | 1 | 7.78 |
| CHEMBL202680 | — | — | 1 | 7.57 |
| CHEMBL381805 | — | — | 1 | 7.53 |
| CHEMBL206079 | — | — | 1 | 7.35 |
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | 7.29 |
| CHEMBL206709 | — | — | 1 | 7.13 |
| CHEMBL427387 | — | — | 1 | 6.71 |
| CHEMBL204683 | — | — | 1 | 6.54 |
| CHEMBL205423 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL324547 | NETAZEPIDE | Ki | = | 0.138 | nM | 9.86 |
| CHEMBL205455 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL203530 | — | Ki | = | 5.495 | nM | 8.26 |
| CHEMBL205831 | — | Ki | = | 6.026 | nM | 8.22 |
| CHEMBL205751 | — | Ki | = | 6.026 | nM | 8.22 |
| CHEMBL9387 | L-365260 | Ki | = | 7.762 | nM | 8.11 |
| CHEMBL204154 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL378098 | — | Ki | = | 8.913 | nM | 8.05 |
| CHEMBL380363 | — | Ki | = | 9.12 | nM | 8.04 |
| CHEMBL378388 | — | Ki | = | 13.18 | nM | 7.88 |
| CHEMBL379902 | — | Ki | = | 13.18 | nM | 7.88 |
| CHEMBL205198 | — | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL380907 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL380193 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL202680 | — | Ki | = | 26.92 | nM | 7.57 |
| CHEMBL381805 | — | Ki | = | 29.51 | nM | 7.53 |
| CHEMBL206079 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL9506 | DEVAZEPIDE | Ki | = | 51.29 | nM | 7.29 |
| CHEMBL206709 | — | Ki | = | 74.13 | nM | 7.13 |
| CHEMBL427387 | — | Ki | = | 194.98 | nM | 6.71 |
| CHEMBL204683 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL205423 | — | Ki | = | 2511.89 | nM | 5.60 |