Assay Detail
Binding
CHEMBL4009724
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Inhibition of SPHK1 in human MDA1483 cells using C17-sphingosine as substrate assessed as reduction in C17-S1P formation preincubated for 30 mins with substrate measured after 15 mins by LC-MS analysis
26
Total Activities
26
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 | 26 | 7.82 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4077280 | — | — | 1 | 10.52 |
| CHEMBL4066270 | — | — | 1 | 10.52 |
| CHEMBL4061789 | — | — | 1 | 9.77 |
| CHEMBL4090361 | — | — | 1 | 9.52 |
| CHEMBL4086094 | — | — | 1 | 9.22 |
| CHEMBL3134157 | — | — | 1 | 9.10 |
| CHEMBL4063424 | — | — | 1 | 9.00 |
| CHEMBL4069327 | — | — | 1 | 8.77 |
| CHEMBL4104017 | — | — | 1 | 8.77 |
| CHEMBL4103414 | — | — | 1 | 8.46 |
| CHEMBL4091588 | — | — | 1 | 8.40 |
| CHEMBL4086161 | — | — | 1 | 8.40 |
| CHEMBL4104070 | — | — | 1 | 8.00 |
| CHEMBL4077075 | — | — | 1 | 7.52 |
| CHEMBL3348835 | — | — | 1 | 7.37 |
| CHEMBL4082814 | — | — | 1 | 7.09 |
| CHEMBL4101573 | — | — | 1 | 6.75 |
| CHEMBL4093921 | — | — | 1 | 6.60 |
| CHEMBL4066355 | — | — | 1 | 6.36 |
| CHEMBL4093845 | — | — | 1 | 6.29 |
| CHEMBL4063506 | — | — | 1 | 5.92 |
| CHEMBL4067356 | — | — | 1 | 5.68 |
| CHEMBL4088607 | — | — | 1 | 5.01 |
| CHEMBL4101628 | — | — | 1 | 4.57 |
| CHEMBL4101485 | — | — | 1 | - |
| CHEMBL4064624 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4077280 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4066270 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4061789 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4090361 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4086094 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3134157 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4063424 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4069327 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4104017 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4103414 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4091588 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4086161 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4104070 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4077075 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3348835 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4082814 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4101573 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4093921 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4066355 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4093845 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL4063506 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4067356 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4088607 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL4101628 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4101485 | — | IC50 | - | — | - | |
| CHEMBL4064624 | — | IC50 | > | 100000.0 | nM | - |