BDBM159748 US10966980, Example 2::US9035074, 2
SMILES CCCS(=O)(=O)N[C@H]1C[C@H](C1)N(C)c1ncnc2[nH]ccc12
InChI Key InChIKey=IUEWXNHSKRWHDY-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 39 hits for monomerid = 159748
Affinity DataIC50: 1.00E+4nMAssay Description:Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovi...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of recombinant human JAK3 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assayMore data for this Ligand-Target Pair
Affinity DataIC50: 5.10nMAssay Description:Inhibition of N-terminal GST-tagged human JAK1 catalytic domain (850 to 1154 residues) incubated for 40 mins in presence of TK substrate-biotin by TR...More data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataIC50: 36nMAssay Description:Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 480nMAssay Description:Inhibition of N-terminal His-tagged human JAK3 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 160nMAssay Description:Inhibition of N-terminal GST-tagged human TYK2 catalytic domain (871 to 1187 residues) incubated for 40 mins in presence of TK substrate-biotin by TR...More data for this Ligand-Target Pair
Affinity DataIC50: 180nMAssay Description:Inhibition of JAK1 in human STAT6-bla-RA1 cells assessed as reduction in IL4-induced STAT6-signalling pre-incubated for 1 hrs before human recombinan...More data for this Ligand-Target Pair
Affinity DataIC50: 1.40E+3nMAssay Description:Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO additio...More data for this Ligand-Target Pair
Affinity DataIC50: 29nMAssay Description:Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovi...More data for this Ligand-Target Pair
Affinity DataIC50: 803nMAssay Description:Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovi...More data for this Ligand-Target Pair
Affinity DataIC50: 29nMAssay Description:Inhibition of recombinant human JAK1 using 5'FAM-KKSRGDYMTMQID as substrate in presence of 1 mM ATP by mobility shift assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.25E+3nMAssay Description:Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovi...More data for this Ligand-Target Pair
Affinity DataIC50: 29nMAssay Description:Inhibition of JAK 1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Inhibition of JAK1 JH1 domain (unknown origin) using FITC-Ahx-KKSRGDYMTMQIG-NH2 peptide as substrate incubated for 60 mins in the presence of ATP by ...More data for this Ligand-Target Pair
Affinity DataIC50: 412nMAssay Description:Inhibition of JAK2 JH1 domain (unknown origin) using Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK peptide as substrate incubated for 60 mins in the presenc...More data for this Ligand-Target Pair
Affinity DataIC50: 7.07E+3nMAssay Description:Inhibition of JAK3 JH1 domain (unknown origin) using Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK peptide as substrate incubated for 60 mins in the presenc...More data for this Ligand-Target Pair
Affinity DataIC50: 549nMAssay Description:Inhibition of TYK2 (unknown origin) by caliper technologyMore data for this Ligand-Target Pair
Affinity DataIC50: 47nMAssay Description:Inhibition of JAK1/JAK3 in human M07E cells assessed as reduction of IL-15 stimulated STAT phosphorylation preincubated for 30 mins followed by IL-15...More data for this Ligand-Target Pair
Affinity DataIC50: 284nMAssay Description:Inhibition of JAK1/TYK2 in human M07E cells assessed as reduction of IFN alpha stimulated STAT phosphorylation preincubated for 30 mins followed by I...More data for this Ligand-Target Pair
Affinity DataIC50: 90nMAssay Description:Inhibition of JAK1/JAK3 in human blood assessed as reduction of IL-2 stimulated STAT phosphorylation preincubated for 30 mins followed by IL-2 stimul...More data for this Ligand-Target Pair
Affinity DataIC50: 605nMAssay Description:Inhibition of recombinant human JAK3 using FITC-KGGEEEEYFELVKK as substrate in presence of 4 uM ATP by mobility shift assayMore data for this Ligand-Target Pair
Affinity DataIC50: 803nMpH: 7.4 T: 2°CAssay Description:Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovi...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+4nMpH: 7.4 T: 2°CAssay Description:Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovi...More data for this Ligand-Target Pair
Affinity DataIC50: 1.25E+3nMpH: 7.4 T: 2°CAssay Description:Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovi...More data for this Ligand-Target Pair
Affinity DataIC50: 803nMAssay Description:Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+5nMAssay Description:Inhibition of recombinant human TYK2 using 5'FAM-KKSRGDYMTMQID as substrate in presence of 1 mM ATP by mobility shift assayMore data for this Ligand-Target Pair
Affinity DataIC50: 6.00E+3nMAssay Description:Inhibition of MAOA (unknown origin)More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK1/Tyrosine-protein kinase JAK2(Human)
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 163nMAssay Description:Inhibition of JAK1/JAK2/TYK2 in CD14+ human whole blood assessed as reduction in IL-6 induced STAT1 phosphorylation preincubated for 45 mins followed...More data for this Ligand-Target Pair
Affinity DataIC50: 271nMAssay Description:Inhibition of JAK2/JAK1 in human whole blood assessed as reduction in IL-27 induced STAT3 phosphorylation preincubated for 45 mins followed by IL-27 ...More data for this Ligand-Target Pair
Affinity DataIC50: 7.18E+3nMAssay Description:Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP add...More data for this Ligand-Target Pair
Affinity DataIC50: 29nMpH: 7.4 T: 2°CAssay Description:Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovi...More data for this Ligand-Target Pair
Affinity DataIC50: 1.20E+3nMAssay Description:Inhibition of recombinant human VEGFR2 expressed in Sf9 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 163nMAssay Description:Inhibition of JAK2/JAK1 in human whole blood assessed as reduction in IFNgamma induced STAT1 phosphorylation preincubated for 45 mins followed by IFN...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK1(Human)
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 2.51E+3nMAssay Description:Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IL-10 induced STAT3 phosphorylation preincubated for 45 mins followed by IL-10 ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.30E+3nMAssay Description:Inhibition of JAK1/JAK3 in CD8+ human whole blood assessed as reduction in IL-15 induced STAT5 phosphorylation preincubated for 45 mins followed by I...More data for this Ligand-Target Pair
Affinity DataIC50: 511nMAssay Description:Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-21 induced STAT3 phosphorylation preincubated for 45 mins followed by IL-21 ...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK2(Human)
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 1.37E+4nMAssay Description:Inhibition of JAK2/TYK2 in human whole blood assessed as reduction in IL-12 induced STAT4 phosphorylation preincubated for 45 mins followed by IL-12 ...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK2(Human)
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 1.65E+4nMAssay Description:Inhibition of JAK2/TYK2 in human whole blood assessed as reduction in IL-23 induced STAT3 phosphorylation preincubated for 45 mins followed by IL-23 ...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK1(Human)
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 189nMAssay Description:Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFNalpha induced STAT3 phosphorylation preincubated for 45 mins followed by IFN...More data for this Ligand-Target Pair