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 Inhibition of p38alpha (unknown origin) B 5.82 pIC50 1500 nM IC50 J Med Chem (2022) 65: 15993-16032 [PMID:36490325]
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 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]