Assay Detail
Binding
CHEMBL1009181
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Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CCL39 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Highly potent 4-amino-indolo[2,3-c]azepin-3-one-containing somatostatin mimetics with a range of sst receptor selectivities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.09 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL466609 | — | — | 1 | 9.00 |
| CHEMBL504930 | — | — | 1 | 8.89 |
| CHEMBL442494 | — | — | 1 | 8.70 |
| CHEMBL503379 | — | — | 1 | 8.68 |
| CHEMBL499398 | — | — | 1 | 8.64 |
| CHEMBL473160 | — | — | 1 | 8.62 |
| CHEMBL447455 | — | — | 1 | 8.62 |
| CHEMBL504838 | — | — | 1 | 8.48 |
| CHEMBL499681 | — | — | 1 | 8.36 |
| CHEMBL454202 | — | — | 1 | 8.16 |
| CHEMBL501699 | — | — | 1 | 8.15 |
| CHEMBL442605 | — | — | 1 | 8.15 |
| CHEMBL448026 | — | — | 1 | 8.09 |
| CHEMBL448713 | — | — | 1 | 7.85 |
| CHEMBL476240 | — | — | 1 | 7.85 |
| CHEMBL505888 | — | — | 1 | 7.77 |
| CHEMBL443084 | — | — | 1 | 7.46 |
| CHEMBL462020 | — | — | 1 | 7.25 |
| CHEMBL509513 | — | — | 1 | 7.23 |
| CHEMBL453938 | — | — | 1 | 7.14 |
| CHEMBL453412 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL466609 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL504930 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL442494 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL503379 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL499398 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL473160 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL447455 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL504838 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL499681 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL454202 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL501699 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL442605 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL448026 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL448713 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL476240 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL505888 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL443084 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL462020 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL509513 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL453938 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL453412 | — | IC50 | = | 161.0 | nM | 6.79 |