Assay Detail
Functional
CHEMBL2341527
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Agonist activity at human S1P3 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 5.55 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2336066 | — | — | 1 | 5.96 |
| CHEMBL2336069 | — | — | 1 | 5.89 |
| CHEMBL2336086 | — | — | 1 | 5.82 |
| CHEMBL2336085 | — | — | 1 | 5.80 |
| CHEMBL2336065 | — | — | 1 | 5.72 |
| CHEMBL2336064 | — | — | 1 | 5.66 |
| CHEMBL2336063 | — | — | 1 | 5.60 |
| CHEMBL2336061 | — | — | 1 | 5.58 |
| CHEMBL2336083 | — | — | 1 | 5.52 |
| CHEMBL2336070 | — | — | 1 | 5.50 |
| CHEMBL2336062 | — | — | 1 | 5.40 |
| CHEMBL2336087 | — | — | 1 | 5.37 |
| CHEMBL2336071 | SIPONIMOD | 4.0 | 1 | 5.30 |
| CHEMBL2336067 | — | — | 1 | 5.23 |
| CHEMBL2336084 | — | — | 1 | 5.23 |
| CHEMBL2336068 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2336066 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2336069 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2336086 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2336085 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2336065 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2336064 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2336063 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2336061 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL2336083 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2336070 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL2336062 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2336087 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL2336071 | SIPONIMOD | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2336067 | — | EC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL2336084 | — | EC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL2336068 | — | EC50 | = | 7200.0 | nM | 5.14 |