Assay Detail
Binding
CHEMBL3757929
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 6.51 | 6.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3752660 | — | — | 1 | 6.67 |
| CHEMBL3753300 | — | — | 1 | 6.47 |
| CHEMBL3753609 | — | — | 1 | 6.46 |
| CHEMBL3753479 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3752660 | — | EC50 | = | 215.0 | nM | 6.67 |
| CHEMBL3753300 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3753609 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3753479 | — | EC50 | = | 360.0 | nM | 6.44 |