Assay Detail
Binding
CHEMBL662393
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Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Cholecystokinin receptor type A (CHEMBL2871) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structurally similar small molecule photoaffinity CCK-A agonists and antagonists as novel tools for directly probing 7TM receptors-ligand interactions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.79 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 9.10 |
| CHEMBL108130 | — | — | 1 | 7.30 |
| CHEMBL320980 | — | — | 1 | 7.10 |
| CHEMBL323512 | — | — | 1 | 6.80 |
| CHEMBL321761 | — | — | 1 | 6.60 |
| CHEMBL321321 | — | — | 1 | 6.54 |
| CHEMBL325987 | — | — | 1 | 6.51 |
| CHEMBL317668 | — | — | 1 | 6.46 |
| CHEMBL105775 | — | — | 1 | 6.41 |
| CHEMBL321700 | — | — | 1 | 6.39 |
| CHEMBL326251 | — | — | 1 | 6.36 |
| CHEMBL321915 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL108130 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL320980 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL323512 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL321761 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL321321 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL325987 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL317668 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL105775 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL321700 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL326251 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL321915 | — | IC50 | = | 1300.0 | nM | 5.89 |