Assay Detail
Binding
CHEMBL972310
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Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst2 receptor expressed in chinese hamster CCL39 cells by autoradiography
6
Total Activities
6
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
Ring size in octreotide amide modulates differently agonist versus antagonist binding affinity and selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.82 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219375 | — | — | 1 | 8.72 |
| CHEMBL442494 | — | — | 1 | 8.62 |
| CHEMBL455435 | — | — | 1 | 8.31 |
| CHEMBL452074 | — | — | 1 | 8.24 |
| CHEMBL455760 | — | — | 1 | 6.57 |
| CHEMBL526550 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219375 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL442494 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL455435 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL452074 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL455760 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL526550 | — | IC50 | = | 337.0 | nM | 6.47 |