SK1-I [Ligand Id: 6622] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2376441
  • 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 sphingosine kinase 1 (unknown origin) B 5 pKi 10000 nM Ki J Med Chem (2013) 56: 9310-9327 [PMID:24164513]
ChEMBL Inhibition of human recombinant SphK1 expressed in Sf9 cells assessed as radiolabeled products using 5 uM sphingosine and 10 uM gamma[32P]ATP by liquid scintillation counting B 5 pKi 10000 nM Ki J Med Chem (2015) 58: 1879-1899 [PMID:25643074]
ChEMBL Inhibition of V5-His-tagged human SphK1 using sphingosine as substrate in presence of [gamma-32P]ATP B 5 pKi 10000 nM Ki Eur J Med Chem (2017) 139: 461-481 [PMID:28822281]
sphingosine kinase 2/Sphingosine kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3023] [GtoPdb: 2205] [UniProtKB: Q9NRA0]
ChEMBL Inhibition of human recombinant SphK2 expressed in Sf9 cells assessed as radiolabeled products using 10 uM sphingosine and 10 uM gamma[32P]ATP by liquid scintillation counting B 4 pKi >100000 nM Ki J Med Chem (2015) 58: 1879-1899 [PMID:25643074]
ChEMBL Competitive inhibition of V5-His-tagged human SphK2 expressed in HEK293 cells assessed as S1P production using sphingosine and [gamma-32P]ATP as substrate by thin layer chromatography B 5 pIC50 10000 nM IC50 J Med Chem (2014) 57: 5509-5524 [PMID:24471412]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]