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]
ChEMBL Inhibition of IKK2 (unknown origin) B 6.52 pIC50 300 nM IC50 Bioorg Med Chem Lett (2021) 38: 127849-127849 [PMID:33609656]
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]
ChEMBL Inhibition of FynT (unknown origin) B 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (2021) 38: 127849-127849 [PMID:33609656]
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) B 7.82 pIC50 15 nM IC50 Bioorg Med Chem Lett (2021) 38: 127849-127849 [PMID:33609656]
ChEMBL Inhibition of JAK1 (unknown origin) B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
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]
ChEMBL Inhibition of N-terminal flag tagged mouse JAK1 expressed in baculovirus infected Sf9 cells using biotin-EQEDEPEGDYFEWLE-NH2 as substrate in the presence of [gamma p33]-ATP by FRET assay B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
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 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]
ChEMBL Inhibition of human JAK2 (835 to 1132 residues) B 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2021) 38: 127849-127849 [PMID:33609656]
ChEMBL Inhibition of N-terminal flag tagged human JAK2 expressed in baculovirus infected Sf9 cells using biotin-EQEDEPEGDYFEWLE-NH2 as substrate in the presence of [gamma p33]-ATP by FRET assay B 9 pIC50 1 nM IC50 Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
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 (unknown origin) B 9 pIC50 1 nM IC50 Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
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 JAK3 B 8.3 pIC50 5 nM IC50 J Med Chem (2008) 51: 7015-7019 [PMID:18844338]
ChEMBL Inhibition of JAK3 (unknown origin) B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2021) 38: 127849-127849 [PMID:33609656]
ChEMBL Inhibition of N-terminal flag tagged human JAK3 expressed in baculovirus infected Sf9 cells using biotin-EQEDEPEGDYFEWLE-NH2 as substrate in the presence of [gamma p33]-ATP by FRET assay B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
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 (unknown origin) B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
ChEMBL Inhibition of JAK3 B 8.3 pIC50 5 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
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 TYK2 B 9 pIC50 1 nM IC50 J Med Chem (2008) 51: 7015-7019 [PMID:18844338]
ChEMBL Inhibition of TYK2 (unknown origin) B 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2021) 38: 127849-127849 [PMID:33609656]
ChEMBL Inhibition of N-terminal flag tagged human TYK2 expressed in baculovirus infected Sf9 cells using biotin-EQEDEPEGDYFEWLE-NH2 as substrate in the presence of [gamma p33]-ATP by FRET assay B 9 pIC50 1 nM IC50 Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
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 (unknown origin) B 9 pIC50 1 nM IC50 Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
ChEMBL Inhibition of Tyk2 B 9 pIC50 1 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
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 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]