filgotinib [Ligand Id: 7913] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3301607 (Filgotinib, G-146034, GLPG-0634)
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  • colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
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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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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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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 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
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG channel by patch clamp assay B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL Inhibition of human ERG expressed in HEK293 cells by automated patch clamp method B 4.07 pIC50 85000 nM IC50 Bioorg Med Chem (2018) 26: 1495-1510 [PMID:29452839]
ChEMBL Inhibition of human ERG expressed in HEK293 cells after 5 mins by automated planar patch clamp method B 4.07 pIC50 85000 nM IC50 MedChemComm (2018) 9: 477-489
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 - - 5.59 pIC50 2600 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 5.62 pIC50 2400 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 6.04 pIC50 918 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
GtoPdb - - 6.44 pIC50 363 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 6.94 pIC50 116 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
GtoPdb - - 7.49 pIC50 28 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
GtoPdb - - 7.96 pIC50 10 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
Jak1 protein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3351191] [UniProtKB: Q5FVF5]
ChEMBL Inhibition of rat JAK1 B 7.54 pIC50 29 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
Janus kinase 1/tyrosine kinase 2/JAK1/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301391] [GtoPdb: 20472269] [UniProtKB: P23458P29597]
GtoPdb - - 5.59 pIC50 2600 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
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 5.82 pIC50 1500 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK1/TYK2 in IFN-alphaB2-induced human U2OS cells assessed as pSTAT1 B 6.36 pIC50 436 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
GtoPdb - - 6.44 pIC50 363 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 6.94 pIC50 116 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
GtoPdb - - 7.96 pIC50 10 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
Janus kinase 2/Janus kinase 1/JAK2/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038492] [GtoPdb: 20482047] [UniProtKB: O60674P23458]
ChEMBL Inhibition of JAK1/JAK2 in IFNgamma-induced human THP1 cells assessed as pSTAT1 B 5.47 pIC50 3364 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
GtoPdb - - 5.62 pIC50 2400 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK1/JAK2 in OSM-induced human HeLa cells assessed as STAT1 reporter B 5.98 pIC50 1045 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
GtoPdb - - 6.44 pIC50 363 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 7.49 pIC50 28 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
GtoPdb - - 7.96 pIC50 10 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
Janus kinase 2/tyrosine kinase 2/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301392] [GtoPdb: 20482269] [UniProtKB: O60674P29597]
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 4.87 pIC50 13362 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 4.99 pIC50 10123 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
GtoPdb - - 5.59 pIC50 2600 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 5.62 pIC50 2400 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 6.94 pIC50 116 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
GtoPdb - - 7.49 pIC50 28 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
Janus kinase 1/Janus kinase 3/JAK3/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038491] [GtoPdb: 20472049] [UniProtKB: P23458P52333]
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 5.67 pIC50 2140 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
GtoPdb - - 6.44 pIC50 363 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 6.52 pIC50 810 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
ChEMBL Inhibition of JAK1/JAK3 in IL4-induced human THP1 cells assessed as pSTAT6 B 6.81 pIC50 154 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL Inhibition of JAK1/JAK3 in IL2-induced human NK92 cells assessed as pSTAT5 B 6.83 pIC50 148 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
GtoPdb - - 7.96 pIC50 10 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
ChEMBL Inhibition of human CSF1R (unknown origin) B 6.31 pIC50 489 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL Inhibition of JAK1 in human whole blood assessed as inhibition of IL-6-induced pSTAT1 B 6.2 pIC50 629 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
GtoPdb - - 6.44 pIC50 363 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK1 (unknown origin) B 6.44 pIC50 363 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 7.25 pIC50 55.66 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 7.3 pIC50 50.1 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 7.32 pIC50 48.29 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 7.33 pIC50 47.07 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
GtoPdb - - 7.96 pIC50 10 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
ChEMBL Inhibition of JAK1 (unknown origin) B 8 pIC50 10 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of human recombinant JAK1 B 8 pIC50 10 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL Inhibition of human JAK1 using GEEPLYWSFPAKKK as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method B 8 pIC50 10 nM IC50 MedChemComm (2018) 9: 477-489
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 whole blood assessed as inhibition of GM-CSF-induced pSTAT5 B 4.76 pIC50 17453 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
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 4.88 pIC50 13200 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK2 in EPO-induced human UT7-EPO cells assessed as pSTAT5 B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL Inhibition of JAK2 in PRL-induced human 22Rv1 cells assessed as pSTAT5 B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL Inhibition of JAK2 in IL3-induced human BaF3 cells assessed as cell proliferation B 5.34 pIC50 4546 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL Inhibition of JAK2 in IL3-induced human TF1 cells assessed as pSTAT5 B 5.45 pIC50 3524 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL Inhibition of JAK2 (unknown origin) B 5.62 pIC50 2400 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
GtoPdb - - 5.62 pIC50 2400 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 6.78 pIC50 167.34 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 7.26 pIC50 55.49 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 7.39 pIC50 41.16 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
GtoPdb - - 7.49 pIC50 28 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 7.5 pIC50 31.37 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition of JAK2 (unknown origin) B 7.6 pIC50 25 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) B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK3 (unknown origin) B 6.09 pIC50 810 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of human JAK3 using GGEEEEYFELVKKKK as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method B 6.09 pIC50 810 nM IC50 MedChemComm (2018) 9: 477-489
GtoPdb - - 6.52 pIC50 810 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 6.71 pIC50 194.7 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 6.72 pIC50 189.3 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 6.73 pIC50 187.3 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 6.83 pIC50 149.35 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of human FLT3 (unknown origin) B 6.47 pIC50 338 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]
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) B 5.59 pIC50 2600 nM IC50 J. Med. Chem. (2014) 57: 5023-5038 [PMID:24417533]
GtoPdb - - 5.59 pIC50 2600 nM IC50 J. Med. Chem. (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of human TYK2 using GGMEDIYFEFMGGKKK as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method B 6.94 pIC50 116 nM IC50 MedChemComm (2018) 9: 477-489
ChEMBL Inhibition of Tyk2 (unknown origin) B 6.94 pIC50 116 nM IC50 J. Med. Chem. (2015) 58: 7596-7602 [PMID:26351728]
GtoPdb - - 6.94 pIC50 116 nM IC50 J. Immunol. (2013) 191: 3568-77 [PMID:24006460]
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 7.06 pIC50 86.77 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 7.1 pIC50 79.07 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 7.13 pIC50 73.75 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL Inhibition Assay: In vitro inhibition assay using various enzyme. B 7.14 pIC50 72.7 nM IC50 US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
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 human FLT4 (unknown origin) B 6.56 pIC50 274 nM IC50 J. Med. Chem. (2014) 57: 9323-9342 [PMID:25369270]

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]