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::US20240140952, Compound Ruxolitinib
SMILES c1c[nH]c2c1c(ncn2)c3cnn(c3)[C@H](CC#N)C4CCCC4
InChI Key InChIKey=HFNKQEVNSGCOJV-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 634 hits for monomerid = 50355501
Affinity DataIC50: 1nMpH: 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: 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
3D Structure (crystal)Affinity DataIC50: 200nMpH: 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: 6nMpH: 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: 1nMAssay 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: 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: 200nMAssay 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: 6nMAssay 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: 1nMAssay 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: 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: 200nMAssay 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: 6nMAssay 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: 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
Affinity DataIC50: 3.10nMAssay 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
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK1(Human)
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 194nMAssay 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
Affinity DataIC50: 6nMAssay 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: 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 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: 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: 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: 60nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 38nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.94E+3nMAssay Description:Inhibition of JAK3 (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: 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: 4nMAssay Description:Inhibition of human recombinant N-terminal hexahistidine tagged JAK1 JH1 catalytic domain (854 to 1154 residues) expressed in baculovirus infected Sf...More data for this Ligand-Target Pair
Affinity DataIC50: 51nMAssay Description:Inhibition of human recombinant C-terminal hexahistidine tagged JAK3 JH1 catalytic domain (811 to 1124 residues) expressed in baculovirus infected Sf...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: 11nMAssay Description:Inhibition of TYK2 (unknown origin) using peptide as substrate preincubated for 10 mins followed by substrate addition by mobility shift assayMore 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: 15nMAssay Description:Inhibition of recombinant human HDAC6 using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrateMore data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 487nMAssay Description:Inhibition of JAK3 (unknown origin)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: 3.30nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 428nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged JAK1 (866 to 1154 residues) expressed in insect cells using FITC-labeled C6-KKHTDDGYMPMSPGVA-NH...More 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 DataIC50: 428nMAssay Description:Inhibition of JAK3 (unknown origin) measured after 1 hr in presence of ATP by TR-FRET assayMore 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
Affinity DataIC50: 3.20nMAssay Description:Inhibition of human JAK1 using GEEPLYWSFPAKKK as substrate measured after 40 mins in presence of ATP by scintillation counting methodMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Mouse)
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: 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