SKF-86002 [Ligand Id: 6040] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL313417 (SK-86002, SK&F-86002)
  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
ChEMBL Inhibitory concentration against 5-lipoxygenase in rat RBL-1 cells B 5 pIC50 10000 nM IC50 J. Med. Chem. (1996) 39: 3929-3937 [PMID:8831759]
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL Inhibitory concentration against Prostaglandin H2 synthase 1 (PGHS-1) from ram seminal vesicle B 5.27 pIC50 5400 nM IC50 J. Med. Chem. (1996) 39: 3929-3937 [PMID:8831759]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Displacement of N,N'-(2,2'-(3,3'-disulfanediylbis(2,5-dioxopyrrolidine-3,1-diyl))bis(ethane-2,1-diyl))bis(2-(3-(3-tert-butyl-5-(3-naphthalen-1-ylureido)-1H-pyrazol-1-yl)phenylamino)acetamide) from inactive form of p38alpha expressed in Escherichia coli BL21(DE3) cells by enzyme fragment complementation assay B 6.09 pIC50 820 nM IC50 J. Med. Chem. (2010) 53: 357-367 [PMID:19928858]
ChEMBL In vitro inhibitory concentration against Mitogen-activated protein kinase p38 alpha B 6.4 pIC50 400 nM IC50 J. Med. Chem. (2003) 46: 4702-4713 [PMID:14561090]
ChEMBL Inhibition of p38alpha active form expressed in Escherichia coli BL21(DE3) cells by HTRF assay B 6.96 pIC50 110 nM IC50 J. Med. Chem. (2010) 53: 357-367 [PMID:19928858]
GtoPdb Measured using a classic homogeneous time-resolved fluorescence (HTRF) kinase assay - 6.96 pIC50 110 nM IC50 J Med Chem (2010) 53: 357-67 [PMID:19928858]

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]