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Assay Detail

CHEMBL4009730

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

Binding
Binding affinity to human C-terminal His6-tagged SPHK1 S225A mutant expressed in fall armyworm sf9 cells after 1 hr by ITC analysis
4
Total Activities
4
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

Target

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

Publication

Discovery of a Potent and Selective Sphingosine Kinase 1 Inhibitor through the Molecular Combination of Chemotype-Distinct Screening Hits.
Schnute ME, McReynolds MD, Carroll J, Chrencik J, Highkin MK, Iyanar K, Jerome G, Rains JW, Saabye M, Scholten JA, Yates M, Nagiec MM.
J Med Chem (2017) 60 : 2562 -2572
PubMed 28231433 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 5.23 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4082814 1 5.54
CHEMBL4067356 1 4.92
CHEMBL4088607 1 -
CHEMBL4064624 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4082814 Kd = 2900.0 nM 5.54
CHEMBL4067356 Kd = 12000.0 nM 4.92
CHEMBL4088607 Kd - -
CHEMBL4064624 Kd - -