baricitinib [Ligand Id: 7792] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2105759 (INCB-028050, Baricitinib, INCB-28050, LY-3009104, Olumiant)
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  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
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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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  • tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
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  • AP2 associated kinase 1 in Human [GtoPdb: 1921] [UniProtKB: Q2M2I8]
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  • BMP2 inducible kinase in Human [GtoPdb: 1941] [UniProtKB: Q9NSY1]
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  • cyclin G associated kinase in Human [GtoPdb: 2027] [UniProtKB: O14976]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Janus kinase 2/Janus kinase 1/tyrosine kinase 2/JAK1/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301390] [GtoPdb: 204820472269] [UniProtKB: O60674P23458P29597]
GtoPdb - - 7.21 pIC50 61 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK1/JAK2/TYK2 in human whole blood assessed as inhibition of IL-6-induced STAT-1 phosphorylation preincubated for 45 mins followed by IL-6 addition measured after 15 mins by FACS analysis B 7.68 pIC50 21.1 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK1/JAK2/TYK2 in human PBMC assessed as reduction in IL-6-induced STAT1 phosphorylation preincubated for 5 mins followed by IL-6 stimulation for 15 to 60 mins by flow cytometry analysis B 7.8 pIC50 16 nM IC50 J. Med. Chem. (2016) 59: 733-749 [PMID:26701356]
GtoPdb - - 8.15 pIC50 7 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 8.23 pIC50 5.9 nM IC50 J. Immunol. (2010) 184: 5298-307 [PMID:20363976]
GtoPdb - - 8.24 pIC50 5.7 nM IC50 J. Immunol. (2010) 184: 5298-307 [PMID:20363976]
GtoPdb - - 8.4 pIC50 4 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
Janus kinase 1/tyrosine kinase 2/JAK1/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301391] [GtoPdb: 20472269] [UniProtKB: P23458P29597]
GtoPdb - - 7.21 pIC50 61 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFNalpha induced STAT3 phosphorylation preincubated for 45 mins followed by IFNalpha addition measured after 15 mins by flow cytometric analysis B 7.54 pIC50 29 nM IC50 J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL Inhibition of JAK1/TYK2 in human whole blood assessed as inhibition of IFN-alpha-induced STAT-3 phosphorylation preincubated for 45 mins followed by IFN-alpha addition measured after 15 mins by FACS analysis B 7.54 pIC50 28.7 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of TYK2/JAK1 in human PBMC assessed as reduction in IFNalpha-induced STAT1 phosphorylation preincubated for 5 mins followed by IFNalpha stimulation for 15 to 60 mins by flow cytometry analysis B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2016) 59: 733-749 [PMID:26701356]
GtoPdb - - 8.23 pIC50 5.9 nM IC50 J. Immunol. (2010) 184: 5298-307 [PMID:20363976]
GtoPdb - - 8.4 pIC50 4 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
Janus kinase 2/tyrosine kinase 2/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301392] [GtoPdb: 20482269] [UniProtKB: O60674P29597]
ChEMBL Inhibition of TYK2/JAK2 in human PBMC assessed as reduction in IL-23-induced STAT4 phosphorylation preincubated for 5 mins followed by IL-23 stimulation for 15 to 60 mins by flow cytometry analysis B 6.7 pIC50 200 nM IC50 J. Med. Chem. (2016) 59: 733-749 [PMID:26701356]
ChEMBL Inhibition of JAK2/TYK2 in human whole blood assessed as inhibition of IL-12-induced STAT-4 phosphorylation preincubated for 45 mins followed by IL-12 addition measured after 15 mins by FACS analysis B 6.83 pIC50 149 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK2/TYK2 in human whole blood assessed as inhibition of IL-23-induced STAT-3 phosphorylation preincubated for 45 mins followed by IL-23 addition measured after 15 mins by FACS analysis B 7.09 pIC50 81.9 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
GtoPdb - - 7.21 pIC50 61 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 8.15 pIC50 7 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 8.24 pIC50 5.7 nM IC50 J. Immunol. (2010) 184: 5298-307 [PMID:20363976]
Janus kinase 1/Janus kinase 3/JAK3/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038491] [GtoPdb: 20472049] [UniProtKB: P23458P52333]
GtoPdb - - 6.1 pIC50 787 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK1/JAK3 in human whole blood assessed as inhibition of IL-15-induced STAT-5 phosphorylation preincubated for 45 mins followed by IL-15 addition measured after 15 mins by FACS analysis B 6.59 pIC50 259 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK1/JAK3 in human PBMC assessed as reduction in IL-21-induced STAT3 phosphorylation preincubated for 5 mins followed by IL-21 stimulation for 15 to 60 mins by flow cytometry analysis B 7.17 pIC50 67 nM IC50 J. Med. Chem. (2016) 59: 733-749 [PMID:26701356]
GtoPdb - - 8.23 pIC50 5.9 nM IC50 J. Immunol. (2010) 184: 5298-307 [PMID:20363976]
GtoPdb - - 8.4 pIC50 4 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
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) B 8.22 pIC50 6 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
GtoPdb - - 8.23 pIC50 5.9 nM IC50 J. Immunol. (2010) 184: 5298-307 [PMID:20363976]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.4 pIC50 4 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. (2016) 24: 2660-2672 [PMID:27137359]
ChEMBL Inhibition of recombinant human JAK1 using 5'FAM-KKSRGDYMTMQID as substrate in presence of 1 mM ATP by mobility shift assay B 8.4 pIC50 4 nM IC50 J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
GtoPdb - - 8.4 pIC50 4 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK1 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay B 9 pIC50 0.99 nM IC50 J. Med. Chem. (2016) 59: 733-749 [PMID:26701356]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation preincubated for 5 mins followed by GM-CSF stimulation for 15 to 60 mins by flow cytometry analysis B 6.54 pIC50 290 nM IC50 J. Med. Chem. (2016) 59: 733-749 [PMID:26701356]
ChEMBL Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis B 7.06 pIC50 87.8 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
GtoPdb - - 8.15 pIC50 7 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.15 pIC50 7 nM IC50 Bioorg. Med. Chem. (2016) 24: 2660-2672 [PMID:27137359]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.18 pIC50 6.6 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.22 pIC50 6 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
GtoPdb - - 8.24 pIC50 5.7 nM IC50 J. Immunol. (2010) 184: 5298-307 [PMID:20363976]
ChEMBL Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay B 9.1 pIC50 0.8 nM IC50 J. Med. Chem. (2016) 59: 733-749 [PMID:26701356]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of recombinant human JAK3 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay B 5.1 pIC50 >=8000 nM IC50 J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
GtoPdb - - 6.1 pIC50 787 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK3 (unknown origin) B 6.1 pIC50 787 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK3 (unknown origin) B 6.1 pIC50 787 nM IC50 Bioorg. Med. Chem. (2016) 24: 2660-2672 [PMID:27137359]
ChEMBL Inhibition of JAK3 (unknown origin) B 6.4 pIC50 >400 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of JAK3 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay B 7.6 pIC50 25 nM IC50 J. Med. Chem. (2016) 59: 733-749 [PMID:26701356]
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
GtoPdb - - 7.21 pIC50 61 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of TYK2 (unknown origin) B 7.21 pIC50 61 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of Tyk2 (unknown origin) B 7.28 pIC50 53 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay B 8.06 pIC50 8.7 nM IC50 J. Med. Chem. (2016) 59: 733-749 [PMID:26701356]
AP2 associated kinase 1 in Human [GtoPdb: 1921] [UniProtKB: Q2M2I8]
GtoPdb Binding affinity determined in a cell-free biochemical assay. - 7.77 pKd 17 nM Kd Lancet Infect Dis (2020) 20: 400-402 [PMID:32113509]
BMP2 inducible kinase in Human [GtoPdb: 1941] [UniProtKB: Q9NSY1]
GtoPdb Binding affinity determined in a cell-free biochemical assay. - 7.4 pKd 40 nM Kd Lancet Infect Dis (2020) 20: 400-402 [PMID:32113509]
cyclin G associated kinase in Human [GtoPdb: 2027] [UniProtKB: O14976]
GtoPdb Binding affinity determined in a cell-free biochemical assay. - 6.87 pKd 136 nM Kd Lancet Infect Dis (2020) 20: 400-402 [PMID:32113509]

ChEMBL data shown on this page come from version 27:

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]