Assay Detail
Functional
CHEMBL1941620
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Agonist activity at human S1P3 receptor expressed in CHO-K1 cells co-expressing Gq/i5 G-protein assessed as calcium mobilization by FLIPR assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 18 | 5.74 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL366208 | FTY720-P | -1.0 | 1 | 7.57 |
| CHEMBL1938937 | — | — | 1 | 5.82 |
| CHEMBL1938944 | — | — | 1 | 5.60 |
| CHEMBL1938951 | — | — | 1 | 5.60 |
| CHEMBL1938949 | — | — | 1 | 5.60 |
| CHEMBL1938948 | — | — | 1 | 5.60 |
| CHEMBL1938947 | — | — | 1 | 5.60 |
| CHEMBL1938946 | — | — | 1 | 5.60 |
| CHEMBL1938945 | — | — | 1 | 5.60 |
| CHEMBL1938943 | — | — | 1 | 5.60 |
| CHEMBL1938942 | — | — | 1 | 5.60 |
| CHEMBL1938941 | — | — | 1 | 5.60 |
| CHEMBL1938940 | — | — | 1 | 5.60 |
| CHEMBL1938939 | — | — | 1 | 5.60 |
| CHEMBL1938938 | — | — | 1 | 5.60 |
| CHEMBL1938950 | — | — | 1 | 5.60 |
| CHEMBL224720 | — | — | 1 | - |
| CHEMBL1938952 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL366208 | FTY720-P | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1938937 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1938944 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938951 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938949 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938948 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938947 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938946 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938945 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938943 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938942 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938941 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938940 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938939 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938938 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1938950 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL224720 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL1938952 | — | EC50 | > | 25000.0 | nM | - |