Assay Detail
Binding
CHEMBL5732216
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Functional Activity (Agonism) on Human S1P1 Receptors (Method B): The CHO-K1-Human S1P1-c-AMP assay was performed at Euroscreenfast, Brussels (Euroscreen, Human S1P1 coupling Gi/0, (Edg1) receptor, catalog no: FAST-0197C, December 2009).Recombinant CHO-K1 cells expressing human S1P1, grown to mid-log Phase in culture media without antibiotics, detached, centrifuged and re-suspended. For agonist testing cells are mixed with compound and Forskolin and incubated at room temperature. Cells are lyses and cAMP concentration are estimated, according to the manufacturer specification, With the HTRF kit from CIS-BIO International (cat no 62AM2PEB).Agonistic effects of compounds are expressed as a percentage of the activity of the reference compound at its EC100 concentration, EC50 is calculated and results are reported as pEC50. Compounds were tested at a 10 points half log concentration range duplicated in 1 experiment.
42
Total Activities
14
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Spiro-cyclic amine derivatives as S1P modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 5.70 | 5.70 |
| kon | 14 | - | - |
| k_off | 14 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5801829 | — | — | 3 | 5.70 |
| CHEMBL4302356 | — | — | 3 | - |
| CHEMBL5822937 | — | — | 3 | - |
| CHEMBL4300404 | — | — | 3 | - |
| CHEMBL5744004 | — | — | 3 | - |
| CHEMBL4300295 | — | — | 3 | - |
| CHEMBL4301966 | — | — | 3 | - |
| CHEMBL4204437 | — | — | 3 | - |
| CHEMBL5955870 | — | — | 3 | - |
| CHEMBL4300415 | — | — | 3 | - |
| CHEMBL5840606 | — | — | 3 | - |
| CHEMBL6055621 | — | — | 3 | - |
| CHEMBL6021443 | — | — | 3 | - |
| CHEMBL5762419 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5801829 | — | EC50 | = | 1995.0 | nM | 5.70 |
| CHEMBL5744004 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL5744004 | — | kon | = | - | — | - |
| CHEMBL4302356 | — | kon | = | - | — | - |
| CHEMBL4302356 | — | k_off | = | - | s-1 | - |
| CHEMBL5822937 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL5822937 | — | kon | = | - | — | - |
| CHEMBL5822937 | — | k_off | = | - | s-1 | - |
| CHEMBL4300404 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL4300404 | — | kon | = | - | — | - |
| CHEMBL4300404 | — | k_off | = | - | s-1 | - |
| CHEMBL5762419 | — | k_off | = | - | s-1 | - |
| CHEMBL4302356 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL5744004 | — | k_off | = | - | s-1 | - |
| CHEMBL4300295 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL4300295 | — | kon | = | - | — | - |
| CHEMBL4300295 | — | k_off | = | - | s-1 | - |
| CHEMBL5801829 | — | kon | = | - | — | - |
| CHEMBL5801829 | — | k_off | = | - | s-1 | - |
| CHEMBL4301966 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL4301966 | — | kon | = | - | — | - |
| CHEMBL4301966 | — | k_off | = | - | s-1 | - |
| CHEMBL5840606 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL5840606 | — | kon | = | - | — | - |
| CHEMBL4204437 | — | kon | = | - | — | - |
| CHEMBL4204437 | — | k_off | = | - | s-1 | - |
| CHEMBL5955870 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL5955870 | — | kon | = | - | — | - |
| CHEMBL5955870 | — | k_off | = | - | s-1 | - |
| CHEMBL4300415 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL4300415 | — | kon | = | - | — | - |
| CHEMBL4300415 | — | k_off | = | - | s-1 | - |
| CHEMBL5762419 | — | kon | = | - | — | - |
| CHEMBL4204437 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL5840606 | — | k_off | = | - | s-1 | - |
| CHEMBL6055621 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL6055621 | — | kon | = | - | — | - |
| CHEMBL6055621 | — | k_off | = | - | s-1 | - |
| CHEMBL6021443 | — | EC50 | < | 3162.0 | nM | - |
| CHEMBL6021443 | — | kon | = | - | — | - |
| CHEMBL6021443 | — | k_off | = | - | s-1 | - |
| CHEMBL5762419 | — | EC50 | < | 3162.0 | nM | - |