Found 67 Enz. Inhib. hit(s) for PDB: 3FUP 
Affinity DataKi: 0.700nMAssay Description:Inhibition of recombinant JAK2 (unknown origin) using Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 mins in presence of ATPMore data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataKi: 0.700nMAssay Description:Inhibition of human GST-fused JAK2 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 3...More data for this Ligand-Target Pair
Affinity DataKi: 0.990nMAssay Description:Inhibition of human recombinant JAK2 kinase domain using FITC-KGGEEEEYFELVKK as substrate by peptide mobility shift assayMore data for this Ligand-Target Pair
Affinity DataKi: 5.00E+3nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
Affinity DataIC50: 0.600nMAssay Description:Inhibition of human recombinant JAK2More data for this Ligand-Target Pair
Affinity DataIC50: 1.09nMAssay Description:Reagents used in JAK inhibition assay: Base Reaction buffer; 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/ml BSA, 0.1 mM Na3VO...More data for this Ligand-Target Pair
Affinity DataIC50: 1.10nMAssay Description:Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding methodMore data for this Ligand-Target Pair
Affinity DataIC50: 1.40nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.40nMAssay Description:Displacement of [35S]-MK499 from human ERG expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
Affinity DataIC50: 1.60nMAssay Description:Inhibition of JAK2 by solution phase kinase assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 10 uM [gamma33P]ATP by radiometric methodMore data for this Ligand-Target Pair
Affinity DataIC50: 2.20nMAssay Description:A commercial assay by Reaction Biology Corp.More data for this Ligand-Target Pair
Affinity DataIC50: 2.5nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2.80nMAssay Description:Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by s...More data for this Ligand-Target Pair
Affinity DataIC50: 3.10nMAssay Description:Inhibition of human JAK2 kinase domain using biotin-Lyn-substrate-2 as substrate and ATP incubated for 1 hr by ELISA methodMore data for this Ligand-Target Pair
Affinity DataIC50: 3.10nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of recombinant human GST-tagged JAK2 expressed in baculovirus expression system using Z'-LYTE Try6 peptide as substrate incubated for 1 hr...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured afte...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of JAK2 (unknown origin) using [33gammaP]ATP and Biotin-KAIETDKEYYTVKD as substrate incubated for 10 mins prior to substrate addition meas...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured afte...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FR...More data for this Ligand-Target Pair
Affinity DataIC50: 4.10nMAssay Description:Inhibition of recombinant JAK2 kinase domain (unknown origin) using FITC-KGGEEEEYFELVKK as substrate assessed as inhibition of substrate phosphorylat...More data for this Ligand-Target Pair
Affinity DataIC50: 4.20nMAssay Description:Inhibition of recombinant GST-tagged human JAK2 (809 to 1153 residues) catalytic cytoplasmic domain expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
Affinity DataIC50: 4.30nMAssay Description:Inhibition of recombinant human GST-tagged JAK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated fo...More data for this Ligand-Target Pair
Affinity DataIC50: 9.90nMAssay Description:Inhibition of recombinant human JAK2 (808-end residues) in presence of ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of JAK2 by kinase-Glo luminescent assayMore data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 12nMAssay Description:Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 30nMpH: 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
Affinity DataIC50: 33nMAssay Description:Inhibition of GST-tagged JAK2 kinaseMore data for this Ligand-Target Pair
Affinity DataIC50: 71nMAssay Description:Inhibition of JAK2 in human CD34+ cells assessed as inhibition of EPO-mediated cell proliferationMore data for this Ligand-Target Pair
Affinity DataIC50: 72nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK1/Tyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 75nMAssay Description: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 ...More data for this Ligand-Target Pair
Affinity DataIC50: 77nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 77nMAssay 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: 77nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 95nMAssay Description:Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stim...More data for this Ligand-Target Pair
Affinity DataIC50: 107nMAssay Description:Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elemen...More data for this Ligand-Target Pair
Affinity DataIC50: 155nMAssay Description:Inhibition of JAK2 in human PBMC assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measu...More data for this Ligand-Target Pair
Affinity DataIC50: 170nMAssay Description:Inhibition of JAK1/2 in human PBMC expressing CD14 assessed as inhibition of IFNgamma-induced STAT1 phosphorylationMore data for this Ligand-Target Pair
Affinity DataIC50: 170nMAssay Description:Inhibition of JAK2/1 in human T cells expressing CD3 assessed as inhibition of IFNgamma-stimulated STAT1 phosphorylationMore data for this Ligand-Target Pair
Affinity DataIC50: 184nMAssay Description:Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylation after 30 mins by flow cytometric ...More data for this Ligand-Target Pair
Affinity DataIC50: 184nMAssay Description:Inhibition of JAK2 in human monocytes expressing CD14 assessed as inhibition of GM-CSF-stimulated STAT5a phosphorylationMore data for this Ligand-Target Pair
Affinity DataIC50: 190nMAssay Description:Inhibition of JAK2 in human PBMC expressing CD14 assessed as inhibition of GM-CSF-induced STAT5a phosphorylationMore data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 229nMAssay Description: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-2...More data for this Ligand-Target Pair
