Assay Detail
Functional
CHEMBL859934
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for CCK2 receptor assessed by inhibition of pentagastrin-stimulated acid secretion in perfused rat stomach
20
Total Activities
20
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
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 |
|---|---|---|---|
| Kd | 20 | 7.40 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL324547 | NETAZEPIDE | 2.0 | 1 | 10.10 |
| CHEMBL205455 | — | — | 1 | 9.01 |
| CHEMBL204154 | — | — | 1 | 8.88 |
| CHEMBL205198 | — | — | 1 | 7.77 |
| CHEMBL380193 | — | — | 1 | 7.74 |
| CHEMBL378388 | — | — | 1 | 7.56 |
| CHEMBL205751 | — | — | 1 | 7.55 |
| CHEMBL379902 | — | — | 1 | 7.54 |
| CHEMBL9387 | L-365260 | — | 1 | 7.54 |
| CHEMBL202680 | — | — | 1 | 7.44 |
| CHEMBL204683 | — | — | 1 | 7.30 |
| CHEMBL205831 | — | — | 1 | 7.04 |
| CHEMBL206079 | — | — | 1 | 6.98 |
| CHEMBL381805 | — | — | 1 | 6.93 |
| CHEMBL206709 | — | — | 1 | 6.88 |
| CHEMBL380907 | — | — | 1 | 6.84 |
| CHEMBL427387 | — | — | 1 | 6.65 |
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | 6.14 |
| CHEMBL380363 | — | — | 1 | 6.06 |
| CHEMBL205423 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL324547 | NETAZEPIDE | Kd | = | 0.07943 | nM | 10.10 |
| CHEMBL205455 | — | Kd | = | 0.9772 | nM | 9.01 |
| CHEMBL204154 | — | Kd | = | 1.318 | nM | 8.88 |
| CHEMBL205198 | — | Kd | = | 16.98 | nM | 7.77 |
| CHEMBL380193 | — | Kd | = | 18.2 | nM | 7.74 |
| CHEMBL378388 | — | Kd | = | 27.54 | nM | 7.56 |
| CHEMBL205751 | — | Kd | = | 28.18 | nM | 7.55 |
| CHEMBL379902 | — | Kd | = | 28.84 | nM | 7.54 |
| CHEMBL9387 | L-365260 | Kd | = | 28.84 | nM | 7.54 |
| CHEMBL202680 | — | Kd | = | 36.31 | nM | 7.44 |
| CHEMBL204683 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL205831 | — | Kd | = | 91.2 | nM | 7.04 |
| CHEMBL206079 | — | Kd | = | 104.71 | nM | 6.98 |
| CHEMBL381805 | — | Kd | = | 117.49 | nM | 6.93 |
| CHEMBL206709 | — | Kd | = | 131.83 | nM | 6.88 |
| CHEMBL380907 | — | Kd | = | 144.54 | nM | 6.84 |
| CHEMBL427387 | — | Kd | = | 223.87 | nM | 6.65 |
| CHEMBL9506 | DEVAZEPIDE | Kd | = | 724.44 | nM | 6.14 |
| CHEMBL380363 | — | Kd | = | 870.96 | nM | 6.06 |
| CHEMBL205423 | — | Kd | = | 1047.13 | nM | 5.98 |