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 118 hits for monomerid = 50355501
Affinity DataIC50: 6.40nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 8.80nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataIC50: 30nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer
Curated by ChEMBL
Pfizer
Curated by ChEMBL
Affinity DataIC50: 194nMAssay Description:Inhibition of JAK1/TYK2 in human whole blood assessed as inhibition of IFN-alpha-induced STAT-3 phosphorylation preincubated for 45 mins followed by ...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: 487nMAssay Description:Inhibition of JAK3 (unknown origin)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: 1.85E+3nMAssay Description:Inhibition of JAK1/JAK3 in human whole blood assessed as inhibition of IL-15-induced STAT-5 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: 1.05E+3nMAssay Description:Inhibition of JAK1 in human whole blood assessed as inhibition of IL-6-induced pSTAT1More data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMAssay Description:Inhibition of human recombinant JAK2More data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Inhibition of human recombinant JAK1More data for this Ligand-Target Pair
Affinity DataIC50: 0.430nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Inhibition of JAK1 in human PBMC cells assessed as inhibition of IL-6-induced MCP1 secretionMore 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: 0.720nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2.80nMAssay Description:Inhibition of JAK3 (unknown origin)More 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: >300nMAssay Description:Inhibition of human recombinant JAK3 assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and m...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: 3nMAssay Description:Inhibition of human recombinant JAK1 assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and m...More data for this Ligand-Target Pair
Affinity DataIC50: 7nMAssay Description:Inhibition of JAK1 (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: 15nMAssay Description:Inhibition of JAK3 (unknown origin)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: 0.600nMAssay Description:Inhibition of JAK1 (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 DataIC50: 23nMAssay Description:Inhibition of JAK3/1 in human T cells expressing CD3 assessed as inhibition of IL2-stimulated STAT5a phosphorylationMore data for this Ligand-Target Pair
Affinity DataIC50: 0.800nMAssay Description:Inhibition of JAK1 (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: 11nMAssay Description:Inhibition of JAK3 (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: 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: 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
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: 3.30nMAssay Description:Inhibition of human JAK1 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assayMore 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: 428nMAssay Description:Inhibition of human JAK3 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 19nMAssay Description:Inhibition of human TYK2 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 JAK1 by TR-FRET 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: 430nMAssay Description:Inhibition of human recombinant JAK3 by TR-FRET assayMore data for this Ligand-Target Pair