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Assay Detail

CHEMBL4669268

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant His6x-tagged human SphK1 expressed in HEK293 cells assessed as reduction in S1P formation using D-erythro-sphingosine as substrate by Western blot analysis
2
Total Activities
2
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

Target

Sphingosine kinase 1 (CHEMBL4394)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of SKI-349, a dual-targeted inhibitor of sphingosine kinase and microtubule polymerization.
Hengst JA,Hegde S,Paulson RF,Yun JK
Bioorg Med Chem Lett (2020) 30 : 127453 -127453
PubMed 32736077 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.02 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1289102 1 5.52
CHEMBL552462 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1289102 IC50 = 3000.0 nM 5.52
CHEMBL552462 IC50 = 30000.0 nM 4.52