JAK inhibitor I [Ligand Id: 5992] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL21156
  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
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  • inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
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  • maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
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  • platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human [ChEMBL: CHEMBL2095189] [GtoPdb: 1804, 1803] [UniProtKB: P09619, P16234]
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  • protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
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  • Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
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  • C-terminal Src kinase/Tyrosine-protein kinase CSK in Human [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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  • HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
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  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Mouse [ChEMBL: CHEMBL2968] [GtoPdb: 2047] [UniProtKB: P52332]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
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  • tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
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  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of cyclin dependent kinase 2 B 5.48 pIC50 3300 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
ChEMBL Inhibition of Fibroblast growth factor receptor 2 B 6.03 pIC50 940 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
ChEMBL Inhibition of I-kappa-B kinase 2 B 6.52 pIC50 300 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
ChEMBL Inhibition of His6-tagged MELK catalytic domain (1 to 340 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using Bcl-GL as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method B 6.48 pIC50 330 nM IC50 Bioorg Med Chem (2017) 25: 2609-2616 [PMID:28351607]
platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095189] [GtoPdb: 1804, 1803] [UniProtKB: P09619, P16234]
ChEMBL Inhibition of Platelet-derived growth factor receptor B 5.83 pIC50 1490 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684]
ChEMBL Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. (2015) 23: 4839-4845 [PMID:26088337]
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Inhibition of protein kinase C alpha B 5.92 pIC50 1200 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
ChEMBL Inhibition of protein kinase Raf B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
ChEMBL Inhibition of Tyrosine-protein kinase CSK B 5.68 pIC50 2100 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL Inhibition of protein kinase Fyn B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
ChEMBL Inhibition of protein kinase Hck B 5.11 pIC50 7700 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL Inhibition of JAK1 (unknown origin) using 1 mM of ATP and Tyr6 peptide by Z'-LYTE kinase assay B 6.22 pIC50 600 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of JAK1 B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2008) 51: 7015-7019 [PMID:18844338]
ChEMBL Inhibition of JAK1 (unknown origin) using 87 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay B 8.4 pIC50 4 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2968] [GtoPdb: 2047] [UniProtKB: P52332]
ChEMBL Inhibition of murine Jak 1 protein kinase B 7.82 pIC50 15 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
ChEMBL Inhibition of mouse JAK1 B 7.82 pIC50 15 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 (unknown origin) using 1 mM of ATP and Tyr6 peptide by Z'-LYTE kinase assay B 5.85 pIC50 1400 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
GtoPdb - - 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2002) 12: 1219-23 [PMID:11934592]
ChEMBL Inhibition of protein kinase Jak 2 B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
ChEMBL Inhibition of JAK2 B 9 pIC50 1 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of JAK2 B 9 pIC50 1 nM IC50 J. Med. Chem. (2008) 51: 7015-7019 [PMID:18844338]
ChEMBL Inhibition of JAK2 (unknown origin) using 35 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay B 9 pIC50 1 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of JAK3 (unknown origin) using 1 mM of ATP and Tyr6 peptide by Z'-LYTE kinase assay B 6.05 pIC50 900 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of JAK3 (unknown origin) using 16 uM of ATP and Tyr6 peptide by Z'-LYTE kinase assay B 8 pIC50 10 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
GtoPdb - - 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2002) 12: 1219-23 [PMID:11934592]
ChEMBL Inhibition of protein kinase Jak 3 B 8.3 pIC50 5 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
ChEMBL Inhibition of JAK3 B 8.3 pIC50 5 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of JAK3 B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2008) 51: 7015-7019 [PMID:18844338]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of p56 Lck tyrosine kinase B 5.1 pIC50 >8000 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
ChEMBL Inhibition of p56 Lck tyrosine kinase B 5.1 pIC50 >8000 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of Src protein tyrosine kinase B 5.1 pIC50 >8000 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL Inhibition of Tek kinase B 4.62 pIC50 24000 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
ChEMBL Inhibition of Tyk2 (unknown origin) using 1 mM of ATP and Tyr3 peptide by Z'-LYTE kinase assay B 5.77 pIC50 1700 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of Tyk2 (unknown origin) using 25 uM of ATP and Tyr3 peptide by Z'-LYTE kinase assay B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
GtoPdb - - 9 pIC50 1 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
ChEMBL Inhibition of Tyrosine kinase 2 kinase B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
ChEMBL Inhibition of Tyk2 B 9 pIC50 1 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of TYK2 B 9 pIC50 1 nM IC50 J. Med. Chem. (2008) 51: 7015-7019 [PMID:18844338]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
ChEMBL Inhibition of Vascular endothelial growth factor receptor 1 B 5.82 pIC50 1520 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of Vascular endothelial growth factor receptor 2 B 5.85 pIC50 1400 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL Inhibition of Vascular endothelial growth factor receptor 3 B 6.16 pIC50 690 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1219-1223 [PMID:11934592]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]