MP-A08 [Ligand Id: 10219] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3764617
  • sphingosine kinase 1/Sphingosine kinase 1 in Human [ChEMBL: CHEMBL4394] [GtoPdb: 2204] [UniProtKB: Q9NYA1]
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  • sphingosine kinase 2/Sphingosine kinase 2 in Human [ChEMBL: CHEMBL3023] [GtoPdb: 2205] [UniProtKB: Q9NRA0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
sphingosine kinase 1/Sphingosine kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4394] [GtoPdb: 2204] [UniProtKB: Q9NYA1]
ChEMBL Inhibition of human SK1 using D-erythro sphingosine as substrate and gamma[33P]ATP by Lineweaver-Burk plot analysis B 4.57 pKi 27000 nM Ki J. Med. Chem. (2016) 59: 965-984 [PMID:26780304]
ChEMBL Inhibition of recombinant human C-terminal TEV cleavage site-fused-His6-tagged SphK1 expressed in baculovirus infected sf9 insect cells using d-erythro-sphingosine as substrate in presence of [gamma32P]-ATP and ATP by radioactivity-based assay B 4.57 pKi 27000 nM Ki J Med Chem (2020) 63: 1178-1198 [PMID:31895563]
GtoPdb In vitro inhibition of substrate phosphorylation. - 4.57 pIC50 27000 nM IC50 Oncotarget (2015) 6: 7065-83 [PMID:25788259]
sphingosine kinase 2/Sphingosine kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3023] [GtoPdb: 2205] [UniProtKB: Q9NRA0]
GtoPdb In vitro inhibition of substrate phosphorylation. - 5.16 pKi 6900 nM Ki Oncotarget (2015) 6: 7065-83 [PMID:25788259]
ChEMBL Inhibition of human SK2 using D-erythro sphingosine as substrate and gamma[33P]ATP by Lineweaver-Burk plot analysis B 5.16 pKi 6900 nM Ki J. Med. Chem. (2016) 59: 965-984 [PMID:26780304]
ChEMBL Inhibition of recombinant human His6/HA-fusion-tagged SphK2 expressed in baculovirus infected sf9 insect cells using d-erythro-sphingosine as substrate in presence of [gamma32P]-ATP and ATP by radioactivity-based assay B 5.16 pKi 6900 nM Ki J Med Chem (2020) 63: 1178-1198 [PMID:31895563]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]