Assay Detail
Binding
CHEMBL4736174
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Inhibition of recombinant human Sphk1 expressed in baculovirus infected Sf9 insect cells using d-erythro-sphingosine as substrate measured after 20 mins in presence of [gamma-32P]ATP by liquid scintillation counting analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Probing the substitution pattern of indole-based scaffold reveals potent and selective sphingosine kinase 2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.12 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3814580 | — | — | 1 | 8.14 |
| CHEMBL4783605 | — | — | 1 | 8.10 |
| CHEMBL4755938 | — | — | 1 | - |
| CHEMBL4750447 | — | — | 1 | - |
| CHEMBL4782021 | — | — | 1 | - |
| CHEMBL3814849 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3814580 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL4783605 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4755938 | — | Ki | > | 10.0 | nM | - |
| CHEMBL4750447 | — | Ki | > | 10.0 | nM | - |
| CHEMBL4782021 | — | Ki | > | 10.0 | nM | - |
| CHEMBL3814849 | — | Ki | > | 20.0 | nM | - |