Kinase Profiling Inhibitor Database

This is a searchable database of specificities of 367 commonly used signal transduction inhibitors. These results have been provided by the International Centre for Kinase profiling within the MRC Protein Phosphorylation Unit at the University of Dundee.

We strongly recommend undertaking kinase profiling of any kinase inhibitor to be used in a biological experiment. It is essential to have a good feel for the specificity of the kinase inhibitor you are working with in order to be able to properly interpret your data.

If you have additional kinase inhibitors that you would like the International Centre for Kinase profiling team to profile for you please contact us here for further details.

If you have any feedback or suggestions on how to improve this resource we welcome your input. Pass on your ideas to us here.

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Inhibitor Brutto MW Action Reference Reference 2
Genistein C15H10O5 270.20 Tyrosine-kinases Constantinou A. and Huberman E. (1995) Proc. Soc. Exp. Biol. Med. 208 109 Wei H. (1995) Proc. Soc. Exp. Biol. Med. 208 124
GF 109203X (Go 6850) C25H24N4O2 412.50 PKC Hers I. (1999) FEBS Lett. 460 433 Ku W.-C. (1997) Biochem. Biophys. Res. Commun. 241 730
Gilteritinib C29H44N8O3 552.70 FLT3; RTKs
Gö 6976 C24H18N4O 378.40 PKC Gschwendt M. (1996) FEBS Lett. 392 77 Wenzel-Seifert K. (1994) Biochem. Biophys. Res. Commun. 200 1536
Gö 7874 C27H26N4O4 • HCl 507.00 PKC Kleinschroth J. (1995) Bioorg. Med. Chem. Lett. 5 55
GSK2334470 C25H34N8O 462.59 PDK1 Najafov A. (2011) Biochem. J. 433 357-69
GSK2578215A C24H18FN3O2 399.42 LRRK2 Reith A. (2012) Bioorg. Med. Chem. Lett.
GSK2606414 C24H20F3N5O 451.44 PERK Axten JM. (2012) J. Med. Chem. 23 55(16) 7193-207
GSK269962A C29H30N8O5 570.61 ROCK Doe C. (2007) J Pharmacol Exp Ther 320 89-98
GSK429286 C21H16F4N4O2 432.37 ROCK Goodman K. (2007) J. Med. Chem. 50 (1), 6-9 Nichols (2009) Biochem.J. 424 47
GSK461364 C27H28F3N5O2S 543.60 PLK1 T. R. Rheault (2010) Bioorg. Med. Chem. Lett. 20(15) 4587-92 K. A. Emmitte (2009) Bioorg. Med. Chem. Lett. 19(6) 1694-7
GSK650394A C25H22N2O2 382.45 SGK Sherk A. B. (2008) Cancer Res 68 7475–7483
GW441756 hydrochloride C17H13N3O • HCl 311.77 Trk A Wood E.R. (2004) Bioorg. Med. Chem. Lett. 14 953-957
GW501516 C21H18F3NO3S2 453.50 PPARd Sznaidman M.L. (2003) Bioorg Med Chem Lett 13(9) 1517-21
GW5074 (Raf1 Kinase Inhibitor I) C15H8Br2INO2 520.90 cRAF1 Lackey K. (2000) Bioorg. Med. Chem. Lett. 10 223
GW843682X (GSK-PLK1 Compound 2) C22H18F3N3O4S 477.46 PLK1 Emmitte K.A. (2009) Bioorganic and Medicinal Chemistry Letters 19 1018-1021
H-1152 (Rho Kinase Inhibitor) C16H21N3O2S • 2HCl 392.30 ROCK Ikenoya M. (2002) J. Neurochem. 81 9 Sasaki Y. (2002) Pharmacol. Ther. 93 225
H-7, Dihydrochloride C14H17N3O2S • 2HCl 364.30 serine/threonine kinases Ku W.C. (1997) Biochem. Biophys. Res. Commun. 241 730 Jarvis W.D. (1994) Cancer Res. 54 1707
H-8, Dihydrochloride C12H15N3O2S • 2HCl 338.30 serine/threonine kinases Ido M. (1991) Br. J. Cancer 64 1103 Hagiwara M. (1987) Mol. Pharmacol. 31 523
H-89, Dihydrochloride C20H20BrN3O2S • 2HCl 519.30 PKA Leemhuis J. (2002) J. Pharmacol. Exp. Ther. 300 1000 Davies S.P. (2000) Biochem. J. 351 95
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