BDBM103727 US10112907, Example 00033::US10206907, Compound 200::US10708263, Compound 1::US10766894, Compound TABLE 1.18::US10919890, Compound 1::US10961228, Example Filgotinib::US11000528, Cpd # 1::US11203595, TABLE 1.18::US11279699, Compound Filgotinib::US8563545, 1

SMILES O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1

InChI Key InChIKey=RIJLVEAXPNLDTC-UHFFFAOYSA-N

Data  106 IC50  1 Kd

PDB links: 2 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 28 hits for monomerid = 103727   

TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  31.4nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  41.2nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  55.5nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  167nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  1.75E+4nMAssay Description:Inhibition of JAK2 in human whole blood assessed as inhibition of GM-CSF-induced pSTAT5More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  3.52E+3nMAssay Description:Inhibition of JAK2 in IL3-induced human TF1 cells assessed as pSTAT5More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  4.55E+3nMAssay Description:Inhibition of JAK2 in IL3-induced human BaF3 cells assessed as cell proliferationMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of JAK2 in EPO-induced human UT7-EPO cells assessed as pSTAT5More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of JAK2 in PRL-induced human 22Rv1 cells assessed as pSTAT5More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  25nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2 [808-1132](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  460nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2 [808-1132](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50: <100nMAssay Description:Recombinant human JAK2 catalytic domain (amino acids 808-1132; catalog number PV4210) was purchased from Invitrogen. 0.025 mU of JAK2 was incubated w...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2 [808-1132](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  74nMAssay Description:JAK1 (KI): For the determination of Ki, different amounts of compound are mixed with the enzyme and the enzymatic reaction is followed as a function ...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  460nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2 [831-1132](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  6.77E+3nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  73.4nMAssay Description:Recombinant human JAK2 catalytic domain (amino acids 808-1132; catalog number PV4210) is purchased from Invitrogen. 0.025 mU of JAK2 is incubated wit...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  74nMAssay Description:Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assayMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  4.45E+3nMAssay Description:Inhibition of JAK2 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assayMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  171nMAssay Description:Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measure...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  2.40E+3nMAssay Description:Inhibition of recombinant human JAK2 assessed as phosphorylation level in presence of 1 mM ATPMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2 [808-1132](Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  31.4nMAssay Description:Recombinant human JAK2 catalytic domain (amino acids 808-1132; catalog number PV4210) was purchased from Invitrogen. 0.025 mU of JAK2 was incubated w...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  55nMAssay Description:The study of the effect of compounds on the activity of purified recombinant JAK was performed by studying the inhibitory activity of the compounds o...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2 [808-1132](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  460nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  28nMAssay Description:Inhibition of JAK 2 (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  122nMAssay Description:Inhibition of recombinant human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate incubated for 40 mins in presence of Mg/ATP mixture b...More data for this Ligand-Target Pair
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  407nMAssay Description:Inhibition of JAK1/JAK2/TYK2 signalling in human whole blood assessed as inhibition of IL-6 stimulated STAT1 phosphorylation in CD4+ lymphocytes prei...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  5.33E+3nMAssay Description:Inhibition of JAK2 signalling in human whole blood assessed as inhibition of GM-CSF stimulated STAT5 phosphorylation in CD33+ monocytes preincubated ...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM103727(US10112907, Example 00033 | US10206907, Compound 2...)
Affinity DataIC50:  28nMAssay Description:Inhibition of recombinant JAK2 (unknown origin) in the presence of ATPMore data for this Ligand-Target Pair