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ChEMBL ligand: CHEMBL3764617 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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] |
ChEMBL | Inhibition of recombinant human SphK1 expressed in baculovirus infected Sf9 cells assessed as decrease in [33P]SIP production using D-erythro-sphingosine as substrate in presence of [gamma33P]-ATP by scintillation counting method | B | 4.57 | pKi | 27000 | nM | Ki | Bioorg Med Chem (2021) 30: 115941-115941 [PMID:33385956] |
ChEMBL | Inhibition of recombinant human SphK1 expressed in baculovirus infected Sf9 cells using d-erythro-sphingosine and [gamma-32P]ATP as substrate by liquid scintillation counting method | B | 4.57 | pKi | 27000 | nM | Ki | Eur J Med Chem (2021) 213: 113164-113164 [PMID:33454547] |
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 | Inhibition of recombinant human SphK2 assessed as decrease in [33P]SIP production using sphingosine as substrate in presence of [gamma33P]-ATP by scintillation counting method | B | 5.16 | pKi | 6900 | nM | Ki | Bioorg Med Chem (2021) 30: 115941-115941 [PMID:33385956] |
ChEMBL | Inhibition of recombinant human SphK2 expressed in baculovirus infected Sf9 cells using d-erythro-sphingosine and [gamma-32P]ATP as substrate by liquid scintillation counting method | B | 5.16 | pKi | 6900 | nM | Ki | Eur J Med Chem (2021) 213: 113164-113164 [PMID:33454547] |
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]