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Assay Detail

CHEMBL3816945

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

Binding
Inhibition of human recombinant SphK1 using sphingosine as substrate incubated for 20 mins by scintillation counting analysis in presence of [gamma-32P]ATP
6
Total Activities
6
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

Structure-Activity Relationship Studies and Molecular Modeling of Naphthalene-Based Sphingosine Kinase 2 Inhibitors.
Congdon MD, Kharel Y, Brown AM, Lewis SN, Bevan DR, Lynch KR, Santos WL.
ACS Med Chem Lett (2016) 7 : 229 -234
PubMed 26985306 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.53 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814505 1 6.14
CHEMBL3814234 1 6.03
CHEMBL3813833 1 5.14
CHEMBL3416830 1 4.80
CHEMBL3813772 1 -
CHEMBL3814849 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814505 Ki = 730.0 nM 6.14
CHEMBL3814234 Ki = 930.0 nM 6.03
CHEMBL3813833 Ki = 7200.0 nM 5.14
CHEMBL3416830 Ki = 16000.0 nM 4.80
CHEMBL3813772 Ki > 10000.0 nM -
CHEMBL3814849 Ki > 20000.0 nM -