Assay Detail
Functional
CHEMBL1941557
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Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization into cytoplasm using Hoechst dye staining
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 6.97 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL314854 | FINGOLIMOD | 4.0 | 1 | 8.70 |
| CHEMBL225155 | — | — | 1 | 7.75 |
| CHEMBL1938949 | — | — | 1 | 7.70 |
| CHEMBL1938940 | — | — | 1 | 7.62 |
| CHEMBL1938941 | — | — | 1 | 7.54 |
| CHEMBL1938952 | — | — | 1 | 7.46 |
| CHEMBL1938938 | — | — | 1 | 7.39 |
| CHEMBL1938943 | — | — | 1 | 7.38 |
| CHEMBL1938946 | — | — | 1 | 7.22 |
| CHEMBL1938937 | — | — | 1 | 7.16 |
| CHEMBL1938942 | — | — | 1 | 6.72 |
| CHEMBL1938950 | — | — | 1 | 6.70 |
| CHEMBL1938951 | — | — | 1 | 6.68 |
| CHEMBL224720 | — | — | 1 | 6.57 |
| CHEMBL1938947 | — | — | 1 | 6.51 |
| CHEMBL1938948 | — | — | 1 | 6.35 |
| CHEMBL1938944 | — | — | 1 | 5.96 |
| CHEMBL1938945 | — | — | 1 | 5.54 |
| CHEMBL1938939 | — | — | 1 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL314854 | FINGOLIMOD | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL225155 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1938949 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1938940 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1938941 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1938952 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1938938 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1938943 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1938946 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1938937 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1938942 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1938950 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1938951 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL224720 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1938947 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1938948 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1938944 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1938945 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL1938939 | — | EC50 | = | 4100.0 | nM | 5.39 |