Assay Detail
Binding
CHEMBL662410
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Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Cholecystokinin receptor type A (CHEMBL2871) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Rationally designed "dipeptoid" analogues of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist CI-988.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.15 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 10.00 |
| CHEMBL9387 | L-365260 | — | 1 | 6.64 |
| CHEMBL83244 | — | — | 1 | 6.32 |
| CHEMBL86879 | — | — | 1 | 6.29 |
| CHEMBL1328 | PENTAGASTRIN | 4.0 | 1 | 6.22 |
| CHEMBL2112333 | — | — | 1 | 6.18 |
| CHEMBL2112330 | — | — | 1 | 6.17 |
| CHEMBL313559 | — | — | 1 | 6.10 |
| CHEMBL407857 | — | — | 1 | 6.07 |
| CHEMBL88090 | — | — | 1 | 6.01 |
| CHEMBL2112338 | — | — | 1 | 6.00 |
| CHEMBL313499 | — | — | 1 | 5.89 |
| CHEMBL85607 | — | — | 1 | 5.89 |
| CHEMBL312894 | — | — | 1 | 5.82 |
| CHEMBL87470 | — | — | 1 | 5.77 |
| CHEMBL314178 | — | — | 1 | 5.57 |
| CHEMBL433148 | — | — | 1 | 5.36 |
| CHEMBL263969 | — | — | 1 | 5.35 |
| CHEMBL315055 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL9387 | L-365260 | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL83244 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL86879 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1328 | PENTAGASTRIN | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2112333 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL2112330 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL313559 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL407857 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL88090 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL2112338 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL313499 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL85607 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL312894 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL87470 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL314178 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL433148 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL263969 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL315055 | — | IC50 | = | 5200.0 | nM | 5.28 |