Assay Detail
Binding
CHEMBL4392250
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Inhibition of GFP-tagged SK1 (unknown origin) expressed in HEK293 cells using Sph as substrate measured after 30 mins in presence of [gamma32P]ATP by Cerenkov counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Topographical Mapping of Isoform-Selectivity Determinants for J-Channel-Binding Inhibitors of Sphingosine Kinases 1 and 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.05 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4474024 | — | — | 1 | 8.05 |
| CHEMBL4444218 | — | — | 1 | 7.96 |
| CHEMBL4574678 | — | — | 1 | 7.85 |
| CHEMBL4472026 | — | — | 1 | 7.58 |
| CHEMBL3134157 | — | — | 1 | 7.55 |
| CHEMBL4454855 | — | — | 1 | 7.41 |
| CHEMBL4551903 | — | — | 1 | 7.39 |
| CHEMBL4455113 | — | — | 1 | 7.36 |
| CHEMBL4578165 | — | — | 1 | 6.86 |
| CHEMBL4090361 | — | — | 1 | 6.84 |
| CHEMBL4456309 | — | — | 1 | 6.77 |
| CHEMBL4593030 | — | — | 1 | 6.12 |
| CHEMBL4453199 | — | — | 1 | 5.63 |
| CHEMBL4551657 | — | — | 1 | 5.38 |
| CHEMBL4448423 | — | — | 1 | - |
| CHEMBL4555776 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4474024 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4444218 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4574678 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4472026 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3134157 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4454855 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4551903 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4455113 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4578165 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4090361 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4456309 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4593030 | — | IC50 | = | 765.0 | nM | 6.12 |
| CHEMBL4453199 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL4551657 | — | IC50 | = | 4130.0 | nM | 5.38 |
| CHEMBL4448423 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4555776 | — | IC50 | > | 3000.0 | nM | - |