Assay Detail
Binding
CHEMBL880432
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Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 4 expressed in CHO cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.75 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL196534 | — | — | 1 | 7.40 |
| CHEMBL198976 | — | — | 1 | 7.31 |
| CHEMBL198415 | — | — | 1 | 7.17 |
| CHEMBL193789 | — | — | 1 | 7.16 |
| CHEMBL194419 | — | — | 1 | 7.16 |
| CHEMBL372066 | — | — | 1 | 7.12 |
| CHEMBL195014 | — | — | 1 | 7.05 |
| CHEMBL366181 | — | — | 1 | 7.05 |
| CHEMBL194578 | — | — | 1 | 6.82 |
| CHEMBL195025 | — | — | 1 | 6.62 |
| CHEMBL195141 | — | — | 1 | 6.43 |
| CHEMBL196357 | — | — | 1 | 6.43 |
| CHEMBL381872 | — | — | 1 | 6.37 |
| CHEMBL194898 | — | — | 1 | 6.28 |
| CHEMBL364899 | — | — | 1 | 6.19 |
| CHEMBL196149 | — | — | 1 | 5.37 |
| CHEMBL371985 | — | — | 1 | - |
| CHEMBL371743 | — | — | 1 | - |
| CHEMBL371670 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL196534 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL198976 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL198415 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL193789 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL194419 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL372066 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL195014 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL366181 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL194578 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL195025 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL195141 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL196357 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL381872 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL194898 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL364899 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL196149 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL371985 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL371743 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL371670 | — | IC50 | > | 10000.0 | nM | - |