BDBM50355501 INCB-018424::RUXOLITINIB::RUXOLITINIB PHOSPHATE::US10112907, Example 00016::US10766894, Compound TABLE 1.1::US10875847, Compound JAKAFI::US11203595, TABLE 1.1::US11279703, TABLE 6.147
SMILES N#CC[C@H](C1CCCC1)n1cc(cn1)-c1ncnc2[nH]ccc12
InChI Key InChIKey=HFNKQEVNSGCOJV-OAHLLOKOSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 58 hits for monomerid = 50355501
Affinity DataKi: 0.100nMAssay Description:Inhibition of human JAK2 (828-1132) expressed in baculovirus-infected Sf9 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assayMore data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataKi: 0.100nMAssay Description:Inhibition of JAK2 kinase domain using N-terminal 5-carboxyfluorescein-tagged Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 m...More data for this Ligand-Target Pair
Affinity DataKi: 0.240nMAssay Description:Inhibition of purified JAK2 incubated for 30 minsMore data for this Ligand-Target Pair
Affinity DataIC50: 8.80nMAssay Description:Inhibition of JAK2 (unknown origin)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: 298nMAssay 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: 677nMAssay Description:Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincub...More 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: 818nMAssay 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
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 1.09E+3nMAssay Description: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-1...More data for this Ligand-Target Pair
Affinity DataIC50: 4.98E+3nMAssay Description:Inhibition of JAK2 in human whole blood assessed as inhibition of GM-CSF-induced pSTAT5More data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMAssay Description:Inhibition of human recombinant JAK2More data for this Ligand-Target Pair
Affinity DataIC50: 8nMAssay Description:Inhibition of JAK2 in human CD34+ cells assessed as inhibition of EPO-mediated cell proliferationMore data for this Ligand-Target Pair
Affinity DataIC50: 0.120nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before ...More data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKd: 68nMAssay Description:Binding constant for DCAMKL1 kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for YES kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 0.0360nMAssay Description:Binding constant for JAK2(JH1domain-catalytic) kinase domainMore data for this Ligand-Target Pair
Affinity DataEC50: 12nMAssay Description:Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins prior to EPO-induction measur...More data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 31nMAssay 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: 26nMAssay 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 DataEC50: 12nMAssay Description:Inhibition of JAK2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 6.85nMAssay Description:Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPOMore data for this Ligand-Target Pair
Affinity DataIC50: 2nMpH: 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: 2.80nMAssay Description:Inhibition of human JAK2 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of human recombinant JAK2 by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay 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: 677nMAssay Description:Inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptorMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0560nMAssay Description:Inhibition of human JAK2 using poly[Glu:Tyr] as substrate in presence of [gamma-33P]-ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0560nMAssay Description:Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 60nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: <1nMAssay Description:Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma33P]-ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 2.80nMAssay Description:Inhibition of human JAK2 (828 to 1132 residues) expressed in baculovirus infected Sf9 insect cells using EQEDEPEGDYFEWLE as substrate after 1 hr by f...More data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKd: 28nMAssay Description:Binding affinity to human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infec...More data for this Ligand-Target Pair
Affinity DataIC50: 0.600nMAssay Description:Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf...More data for this Ligand-Target Pair
Affinity DataIC50: 2.80nMAssay Description:Inhibition of recombinant human N-terminal epitope-tagged JAK2 (828 to 1132 residues) expressed in baculovirus infected Sf21 insect cells using EQEDE...More data for this Ligand-Target Pair
Affinity DataIC50: 2.80nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay 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
Affinity DataIC50: 4.10nMAssay Description:Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP b...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Mus musculus)
Gwangju Institute Of Science And Technology (Gist)
Curated by ChEMBL
Gwangju Institute Of Science And Technology (Gist)
Curated by ChEMBL
Affinity DataEC50: 186nMAssay Description:Inhibition of JAK2 V617F mutant expressed in mouse BaF3 cells cells assessed as reduction in cell viabilityMore data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 pep...More data for this Ligand-Target Pair
Affinity DataEC50: 3.80E+3nMAssay Description:Stabilization of human JAK2 KD expressed in Expi293F (HEK293F) cells assessed as increase in JAK2 protein levels incubated for 3 mins by isothermal d...More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human JAK2 by radiometric assayMore data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:Inhibition of recombinant epitope tagged JAK2 (828 to 1132 residues) (unknown origin) using Chk2 as substrate by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 18nMAssay Description:Inhibition of recombinant human JAK2 JH1 domain expressed in baculovirus infected insect cells using poly-Glu-Tyr (51 to 68 residues) as substrate in...More data for this Ligand-Target Pair
Affinity DataIC50: 3.80nMAssay Description:1. Add 20 μl of the diluted compound to each well of the 384-well opti plate2. Tap the plate gently3. Add 10 μl of the enzyme to each well ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:1. Add 20 μl of the diluted compound to each well of the 384-well opti plate2. Tap the plate gently3. Add 10 μl of the enzyme to each well ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:1. Add 20 μl of the diluted compound to each well of the 384-well opti plate2. Tap the plate gently3. Add 10 μl of the enzyme to each well ...More data for this Ligand-Target Pair