Assay Detail
Functional
CHEMBL863072
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CCK2 receptor expressed in HEK293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
43
Total Activities
17
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL298) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 7.42 | 8.56 |
| Emax | 13 | - | - |
| Log EC50 | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218327 | — | — | 3 | 8.56 |
| CHEMBL382349 | — | — | 3 | 8.34 |
| CHEMBL206974 | — | — | 3 | 8.18 |
| CHEMBL262172 | — | — | 3 | 8.10 |
| CHEMBL218763 | — | — | 3 | 7.80 |
| CHEMBL408330 | — | — | 3 | 7.72 |
| CHEMBL1121 | SINCALIDE | 4.0 | 3 | 7.57 |
| CHEMBL336381 | — | — | 3 | 7.50 |
| CHEMBL205965 | — | — | 3 | 7.44 |
| CHEMBL382051 | — | — | 3 | 6.97 |
| CHEMBL383458 | — | — | 3 | 6.49 |
| CHEMBL208479 | — | — | 3 | 5.72 |
| CHEMBL407057 | — | — | 3 | 4.71 |
| CHEMBL382409 | — | — | 1 | - |
| CHEMBL408083 | — | — | 1 | - |
| CHEMBL379405 | — | — | 1 | - |
| CHEMBL205306 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218327 | — | EC50 | = | 2.754 | nM | 8.56 |
| CHEMBL218327 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL382349 | — | EC50 | = | 4.571 | nM | 8.34 |
| CHEMBL382349 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL206974 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL206974 | — | EC50 | = | 6.607 | nM | 8.18 |
| CHEMBL262172 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL262172 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL218763 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL218763 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL408330 | — | EC50 | = | 19.05 | nM | 7.72 |
| CHEMBL408330 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1121 | SINCALIDE | EC50 | = | 26.92 | nM | 7.57 |
| CHEMBL1121 | SINCALIDE | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL336381 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL336381 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL205965 | — | EC50 | = | 36.31 | nM | 7.44 |
| CHEMBL205965 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL382051 | — | EC50 | = | 107.15 | nM | 6.97 |
| CHEMBL382051 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL383458 | — | EC50 | = | 323.59 | nM | 6.49 |
| CHEMBL383458 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL208479 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL208479 | — | EC50 | = | 1905.46 | nM | 5.72 |
| CHEMBL407057 | — | EC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL379405 | — | Log EC50 | - | — | - | |
| CHEMBL408083 | — | Log EC50 | - | — | - | |
| CHEMBL206974 | — | Emax | = | 13.0 | % | - |
| CHEMBL205306 | — | Log EC50 | - | — | - | |
| CHEMBL1121 | SINCALIDE | Emax | = | 16.0 | % | - |
| CHEMBL218327 | — | Emax | = | 14.0 | % | - |
| CHEMBL208479 | — | Emax | = | 11.0 | % | - |
| CHEMBL262172 | — | Emax | = | 13.0 | % | - |
| CHEMBL383458 | — | Emax | = | 16.0 | % | - |
| CHEMBL336381 | — | Emax | = | 15.0 | % | - |
| CHEMBL382409 | — | Log EC50 | - | — | - | |
| CHEMBL407057 | — | Emax | = | 14.0 | % | - |
| CHEMBL407057 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL382349 | — | Emax | = | 22.0 | % | - |
| CHEMBL218763 | — | Emax | = | 11.0 | % | - |
| CHEMBL382051 | — | Emax | = | 9.5 | % | - |
| CHEMBL408330 | — | Emax | = | 12.0 | % | - |
| CHEMBL205965 | — | Emax | = | 15.0 | % | - |