Assay Detail
Binding
CHEMBL913919
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Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells
23
Total Activities
23
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
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.14 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL114606 | — | — | 1 | 9.55 |
| CHEMBL225155 | — | — | 1 | 9.17 |
| CHEMBL425563 | — | — | 1 | 8.92 |
| CHEMBL224005 | — | — | 1 | 8.74 |
| CHEMBL334213 | — | — | 1 | 8.64 |
| CHEMBL389880 | — | — | 1 | 8.57 |
| CHEMBL224571 | — | — | 1 | 8.49 |
| CHEMBL375488 | — | — | 1 | 8.46 |
| CHEMBL224853 | — | — | 1 | 8.40 |
| CHEMBL117723 | — | — | 1 | 8.39 |
| CHEMBL224799 | — | — | 1 | 8.37 |
| CHEMBL184349 | — | — | 1 | 8.16 |
| CHEMBL426191 | — | — | 1 | 8.12 |
| CHEMBL224549 | — | — | 1 | 8.11 |
| CHEMBL225575 | — | — | 1 | 8.08 |
| CHEMBL224599 | — | — | 1 | 7.89 |
| CHEMBL224623 | — | — | 1 | 7.75 |
| CHEMBL224703 | — | — | 1 | 7.70 |
| CHEMBL389012 | — | — | 1 | 7.60 |
| CHEMBL224800 | — | — | 1 | 7.48 |
| CHEMBL224720 | — | — | 1 | 7.43 |
| CHEMBL374614 | — | — | 1 | 7.11 |
| CHEMBL314854 | FINGOLIMOD | 4.0 | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL114606 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL225155 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL425563 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL224005 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL334213 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL389880 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL224571 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL375488 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL224853 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL117723 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL224799 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL184349 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL426191 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL224549 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL225575 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL224599 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL224623 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL224703 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL389012 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL224800 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL224720 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL374614 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL314854 | FINGOLIMOD | IC50 | = | 840.0 | nM | 6.08 |