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Assay Detail

CHEMBL4357639

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

Binding
Inhibition of recombinant human SphK2 expressed in baculovirus infected Sf9 cells assessed as decrease in [33P]S1P production using varying level of D-erythro-sphingosine as substrate in presence of [gamma33P]-ATP by scintillation proximity assay
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

Target

Sphingosine kinase 2 (CHEMBL3023)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Small Side Cavity in Sphingosine Kinase 2 that Enhances Inhibitor Potency and Selectivity.
Sibley CD, Morris EA, Kharel Y, Brown AM, Huang T, Bevan DR, Lynch KR, Santos WL.
J Med Chem (2020) 63 : 1178 -1198
PubMed 31895563 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.72 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4453931 1 7.05
CHEMBL4456325 1 6.73
CHEMBL4593983 1 6.72
CHEMBL4570134 1 6.71
CHEMBL4462152 1 6.70
CHEMBL4466524 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4453931 Ki = 89.0 nM 7.05
CHEMBL4456325 Ki = 186.0 nM 6.73
CHEMBL4593983 Ki = 192.0 nM 6.72
CHEMBL4570134 Ki = 197.0 nM 6.71
CHEMBL4462152 Ki = 201.0 nM 6.70
CHEMBL4466524 Ki = 370.0 nM 6.43