Assay Detail
Binding
CHEMBL661736
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Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger".
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.06 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 9.20 |
| CHEMBL443825 | — | — | 1 | 7.40 |
| CHEMBL321761 | — | — | 1 | 7.30 |
| CHEMBL345869 | — | — | 1 | 7.20 |
| CHEMBL108130 | — | — | 1 | 7.10 |
| CHEMBL345786 | — | — | 1 | 7.00 |
| CHEMBL154615 | — | — | 1 | 5.70 |
| CHEMBL346179 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL443825 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL321761 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL345869 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL108130 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL345786 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL154615 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL346179 | — | IC50 | = | 2511.89 | nM | 5.60 |