Assay Detail
Functional
CHEMBL4270322
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of Preclinical Metabolism for Somatostatin Receptor Subtype 5-Selective Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 8.37 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4286244 | — | — | 1 | 10.00 |
| CHEMBL4287248 | — | — | 1 | 9.40 |
| CHEMBL4289661 | — | — | 1 | 9.40 |
| CHEMBL4285917 | — | — | 1 | 9.40 |
| CHEMBL4293458 | — | — | 1 | 9.30 |
| CHEMBL4278328 | — | — | 1 | 9.15 |
| CHEMBL4277006 | — | — | 1 | 9.10 |
| CHEMBL4278915 | — | — | 1 | 9.00 |
| CHEMBL4288391 | — | — | 1 | 8.96 |
| CHEMBL3670722 | — | — | 1 | 8.96 |
| CHEMBL4281446 | — | — | 1 | 8.92 |
| CHEMBL3665800 | — | — | 1 | 8.82 |
| CHEMBL4279392 | — | — | 1 | 8.82 |
| CHEMBL4289325 | — | — | 1 | 8.62 |
| CHEMBL4284956 | — | — | 1 | 8.49 |
| CHEMBL4277991 | — | — | 1 | 8.49 |
| CHEMBL4288334 | — | — | 1 | 8.49 |
| CHEMBL4277613 | — | — | 1 | 8.24 |
| CHEMBL4292738 | — | — | 1 | 8.08 |
| CHEMBL4280432 | — | — | 1 | 7.70 |
| CHEMBL4282854 | — | — | 1 | 7.55 |
| CHEMBL4284867 | — | — | 1 | 7.52 |
| CHEMBL4290073 | — | — | 1 | 7.52 |
| CHEMBL4295189 | — | — | 1 | 7.44 |
| CHEMBL4288259 | — | — | 1 | 7.43 |
| CHEMBL4286833 | — | — | 1 | 7.18 |
| CHEMBL4291751 | — | — | 1 | 7.11 |
| CHEMBL4284442 | — | — | 1 | 6.96 |
| CHEMBL4281783 | — | — | 1 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4286244 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4287248 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4289661 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4285917 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4293458 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4278328 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4277006 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4278915 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4288391 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3670722 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4281446 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3665800 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4279392 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4289325 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4284956 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4277991 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4288334 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4277613 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4292738 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4280432 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4282854 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4284867 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4290073 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4295189 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4288259 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4286833 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4291751 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4284442 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4281783 | — | IC50 | = | 276.0 | nM | 6.56 |