Assay Detail
Binding
CHEMBL4009731
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Inhibition of SPHK1 in human whole-blood using C17-sphingosine as substrate assessed as reduction in C17-S1P production preincubated for 30 mins followed by substrate addition measured after 10 mins by MS analysis
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Potent and Selective Sphingosine Kinase 1 Inhibitor through the Molecular Combination of Chemotype-Distinct Screening Hits.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.43 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4066270 | — | — | 1 | 8.82 |
| CHEMBL4077280 | — | — | 1 | 8.28 |
| CHEMBL4061789 | — | — | 1 | 8.19 |
| CHEMBL4086094 | — | — | 1 | 7.72 |
| CHEMBL3134157 | — | — | 1 | 7.70 |
| CHEMBL4090361 | — | — | 1 | 7.46 |
| CHEMBL4063424 | — | — | 1 | 7.42 |
| CHEMBL4104017 | — | — | 1 | 6.76 |
| CHEMBL3348835 | — | — | 1 | 6.15 |
| CHEMBL4069327 | — | — | 1 | 5.83 |
| CHEMBL4077075 | — | — | 1 | - |
| CHEMBL4103414 | — | — | 1 | - |
| CHEMBL4093845 | — | — | 1 | - |
| CHEMBL4063506 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4066270 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4077280 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4061789 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4086094 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3134157 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4090361 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4063424 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4104017 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL3348835 | — | IC50 | = | 703.0 | nM | 6.15 |
| CHEMBL4069327 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL4077075 | — | IC50 | - | — | - | |
| CHEMBL4103414 | — | IC50 | - | — | - | |
| CHEMBL4093845 | — | IC50 | - | — | - | |
| CHEMBL4063506 | — | IC50 | > | 8800.0 | nM | - |