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Assay Detail

CHEMBL4009723

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Binding
Inhibition of SPHK2 (unknown origin) by FITC-based caliper assay
19
Total Activities
19
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 2 (CHEMBL3023)
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
IC50 19 5.91 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4104017 1 8.62
CHEMBL4063506 1 6.84
CHEMBL4069327 1 6.79
CHEMBL4090361 1 6.79
CHEMBL3134157 1 6.45
CHEMBL4077280 1 6.35
CHEMBL4061789 1 6.33
CHEMBL4063424 1 5.14
CHEMBL4103414 1 4.46
CHEMBL4101573 1 4.40
CHEMBL3348835 1 4.37
CHEMBL4082814 1 4.34
CHEMBL4077075 1 -
CHEMBL4064624 1 -
CHEMBL4093845 1 -
CHEMBL4066270 1 -
CHEMBL4086094 1 -
CHEMBL4088607 1 -
CHEMBL4067356 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4104017 IC50 = 2.4 nM 8.62
CHEMBL4063506 IC50 = 145.0 nM 6.84
CHEMBL4069327 IC50 = 164.0 nM 6.79
CHEMBL4090361 IC50 = 164.0 nM 6.79
CHEMBL3134157 IC50 = 356.0 nM 6.45
CHEMBL4077280 IC50 = 443.0 nM 6.35
CHEMBL4061789 IC50 = 465.0 nM 6.33
CHEMBL4063424 IC50 = 7230.0 nM 5.14
CHEMBL4103414 IC50 = 35100.0 nM 4.46
CHEMBL4101573 IC50 = 39600.0 nM 4.40
CHEMBL3348835 IC50 = 42600.0 nM 4.37
CHEMBL4082814 IC50 = 46000.0 nM 4.34
CHEMBL4077075 IC50 - -
CHEMBL4064624 IC50 > 100000.0 nM -
CHEMBL4093845 IC50 - -
CHEMBL4066270 IC50 < 1.7 nM -
CHEMBL4086094 IC50 < 1.7 nM -
CHEMBL4088607 IC50 > 100000.0 nM -
CHEMBL4067356 IC50 > 100000.0 nM -