Assay Detail
Binding
CHEMBL4009722
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Inhibition of human C-terminal His6-tagged SPHK1 expressed in fall armyworm sf9 cells assessed as reduction in ADP formation using sphingosine as substrate preincubated for 15 mins followed by substrate addition after 1 hr by transcreener-based fluorescence polarization assay
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 | 7.34 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4066270 | — | — | 1 | 9.15 |
| CHEMBL4086094 | — | — | 1 | 9.10 |
| CHEMBL4090361 | — | — | 1 | 8.70 |
| CHEMBL3134157 | — | — | 1 | 8.70 |
| CHEMBL4061789 | — | — | 1 | 8.70 |
| CHEMBL4077280 | — | — | 1 | 8.52 |
| CHEMBL4063424 | — | — | 1 | 8.41 |
| CHEMBL4104017 | — | — | 1 | 8.35 |
| CHEMBL4103414 | — | — | 1 | 8.28 |
| CHEMBL4086161 | — | — | 1 | 8.15 |
| CHEMBL4091588 | — | — | 1 | 8.10 |
| CHEMBL4069327 | — | — | 1 | 8.00 |
| CHEMBL4104070 | — | — | 1 | 7.96 |
| CHEMBL4077075 | — | — | 1 | 7.55 |
| CHEMBL3348835 | — | — | 1 | 7.11 |
| CHEMBL4082814 | — | — | 1 | 6.72 |
| CHEMBL4066355 | — | — | 1 | 6.54 |
| CHEMBL4093921 | — | — | 1 | 6.36 |
| CHEMBL4093845 | — | — | 1 | 6.36 |
| CHEMBL4101573 | — | — | 1 | 5.77 |
| CHEMBL4063506 | — | — | 1 | 5.43 |
| CHEMBL4067356 | — | — | 1 | 5.34 |
| CHEMBL4088607 | — | — | 1 | 4.51 |
| CHEMBL4101628 | — | — | 1 | 4.32 |
| CHEMBL4101485 | — | — | 1 | - |
| CHEMBL4064624 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4066270 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4086094 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4090361 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3134157 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4061789 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4077280 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4063424 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4104017 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4103414 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4086161 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4091588 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4069327 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4104070 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4077075 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3348835 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4082814 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4066355 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4093921 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4093845 | — | IC50 | = | 439.0 | nM | 6.36 |
| CHEMBL4101573 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4063506 | — | IC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL4067356 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4088607 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL4101628 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL4101485 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4064624 | — | IC50 | > | 100000.0 | nM | - |