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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] |
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 data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]