Assay Detail
Binding
CHEMBL913923
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Displacement of [33P]sphingosine 1 phosphate from human S1P5 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 | 7.61 | 9.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225155 | — | — | 1 | 9.26 |
| CHEMBL114606 | — | — | 1 | 9.11 |
| CHEMBL184349 | — | — | 1 | 8.20 |
| CHEMBL117723 | — | — | 1 | 8.00 |
| CHEMBL375488 | — | — | 1 | 8.00 |
| CHEMBL224623 | — | — | 1 | 7.96 |
| CHEMBL224853 | — | — | 1 | 7.92 |
| CHEMBL334213 | — | — | 1 | 7.89 |
| CHEMBL224005 | — | — | 1 | 7.89 |
| CHEMBL225575 | — | — | 1 | 7.80 |
| CHEMBL224571 | — | — | 1 | 7.75 |
| CHEMBL224549 | — | — | 1 | 7.68 |
| CHEMBL425563 | — | — | 1 | 7.64 |
| CHEMBL224703 | — | — | 1 | 7.54 |
| CHEMBL426191 | — | — | 1 | 7.48 |
| CHEMBL389880 | — | — | 1 | 7.39 |
| CHEMBL224599 | — | — | 1 | 7.28 |
| CHEMBL224800 | — | — | 1 | 7.11 |
| CHEMBL224799 | — | — | 1 | 6.92 |
| CHEMBL314854 | FINGOLIMOD | 4.0 | 1 | 5.68 |
| CHEMBL224720 | — | — | 1 | 5.34 |
| CHEMBL389012 | — | — | 1 | - |
| CHEMBL374614 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225155 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL114606 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL184349 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL117723 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL375488 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL224623 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL224853 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL334213 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL224005 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL225575 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL224571 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL224549 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL425563 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL224703 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL426191 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL389880 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL224599 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL224800 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL224799 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL314854 | FINGOLIMOD | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL224720 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL389012 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL374614 | — | IC50 | > | 10000.0 | nM | - |