Assay Detail
Functional
CHEMBL4032272
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Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as increase in S1P-stimulated calcium influx preincubated for 5 mins followed by S1P stimulation measured every 3 secs by fluorescence method
22
Total Activities
22
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
Discovery of a 1-Methyl-3,4-dihydronaphthalene-Based Sphingosine-1-Phosphate (S1P) Receptor Agonist Ceralifimod (ONO-4641). A S1P1 and S1P5 Selective Agonist for the Treatment of Autoimmune Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 8.29 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4092538 | — | — | 1 | 9.24 |
| CHEMBL4074505 | — | — | 1 | 9.24 |
| CHEMBL4085321 | — | — | 1 | 9.00 |
| CHEMBL4093489 | — | — | 1 | 9.00 |
| CHEMBL4095920 | — | — | 1 | 8.92 |
| CHEMBL4087932 | — | — | 1 | 8.92 |
| CHEMBL4071753 | — | — | 1 | 8.85 |
| CHEMBL4093077 | — | — | 1 | 8.77 |
| CHEMBL4084786 | — | — | 1 | 8.59 |
| CHEMBL4095501 | — | — | 1 | 8.52 |
| CHEMBL1962532 | — | — | 1 | 8.52 |
| CHEMBL4065871 | — | — | 1 | 8.46 |
| CHEMBL4075067 | — | — | 1 | 8.35 |
| CHEMBL4103252 | — | — | 1 | 8.30 |
| CHEMBL4101237 | — | — | 1 | 8.18 |
| CHEMBL4100785 | — | — | 1 | 8.10 |
| CHEMBL4063139 | — | — | 1 | 7.89 |
| CHEMBL4074023 | — | — | 1 | 7.72 |
| CHEMBL4062652 | — | — | 1 | 7.27 |
| CHEMBL4077888 | — | — | 1 | 7.24 |
| CHEMBL4065407 | — | — | 1 | 7.01 |
| CHEMBL4059628 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4092538 | — | EC50 | = | 0.58 | nM | 9.24 |
| CHEMBL4074505 | — | EC50 | = | 0.58 | nM | 9.24 |
| CHEMBL4085321 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4093489 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4095920 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4087932 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4071753 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4093077 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4084786 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4095501 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1962532 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4065871 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4075067 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4103252 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4101237 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4100785 | — | EC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4063139 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4074023 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4062652 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4077888 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4065407 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4059628 | — | EC50 | = | 540.0 | nM | 6.27 |