BDBM50503287 ABT-494::Rinvoq::US10961228, Example ABT-494::Upadacitinib
SMILES CC[C@@H]1CN(C[C@@H]1c1cnc2cnc3[nH]ccc3n12)C(=O)NCC(F)(F)F
InChI Key InChIKey=WYQFJHHDOKWSHR-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 153 hits for monomerid = 50503287
Affinity DataIC50: 0.800nMAssay 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 DataKi: 0.890nMAssay Description:Inhibition of recombinant human JAK1 (854 to 1154 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Affinity DataIC50: 1.60nMAssay Description:Inhibition of JAK1 in human TF-1 cells assessed as reduction in OSM-induced STAT3 phosphorylation by flow cytometry analysisMore data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
AbbVie Bioresearch Center
Curated by ChEMBL
AbbVie Bioresearch Center
Curated by ChEMBL
Affinity DataIC50: 2nMAssay Description:Inhibition of JAK1/JAK3 in human HEKa cells assessed as reduction in IL-4-induced STAT6 phosphorylation by flow cytometry analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of recombinant human JAK1 (845 to 1142 residues) expressed in Sf9 insect cells in presence of 0.001 mM of ATP by HTRF analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of recombinant human JAK2 expressed in Sf9 insect cells in presence of 0.001 mM ATP by HTRF analysisMore data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
AbbVie Bioresearch Center
Curated by ChEMBL
AbbVie Bioresearch Center
Curated by ChEMBL
Affinity DataIC50: 3nMAssay Description:Inhibition of JAK1/JAK2 in human HEKa cells assessed as reduction in IL-31-induced STAT3 phosphorylation by flow cytometry analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 3.10nMAssay 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
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
AbbVie Bioresearch Center
Curated by ChEMBL
AbbVie Bioresearch Center
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:Inhibition of JAK1/TYK2 in human HEKa cells assessed as reduction in IL-13-induced STAT6 phosphorylation by flow cytometry analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
Affinity DataIC50: 8nMAssay Description:Inhibition of recombinant JAK2 (unknown origin) in presence of 0.1 mM ATP by alpha-screen assayMore data for this Ligand-Target Pair
Affinity DataIC50: 8nMAssay Description:Inhibition of JAK1 (unknown origin) by cell based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 8nMAssay Description:Inhibition of recombinant human JAK2 expressed in Sf9 insect cells by HTRF analysisMore data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
AbbVie Bioresearch Center
Curated by ChEMBL
AbbVie Bioresearch Center
Curated by ChEMBL
Affinity DataIC50: 10nMAssay Description:Inhibition of JAK1/JAK3 in human T cell assessed as reduction in IL-2-induced STAT5 phosphorylation by flow cytometry analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of JAK1 in human TF-1 cells assessed as reduction in IL-6-induced STAT3 phosphorylation by flow cytometry analysisMore data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
AbbVie Bioresearch Center
Curated by ChEMBL
AbbVie Bioresearch Center
Curated by ChEMBL
Affinity DataIC50: 13nMAssay 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
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
AbbVie Bioresearch Center
Curated by ChEMBL
AbbVie Bioresearch Center
Curated by ChEMBL
Affinity DataIC50: 13nMAssay 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: 14nMAssay Description:Inhibition of JAK1 in mouse BaF3 cellsMore data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
AbbVie Bioresearch Center
Curated by ChEMBL
AbbVie Bioresearch Center
Curated by ChEMBL
Affinity DataIC50: 19nMAssay Description:Inhibition of JAK1/JAK2 in human CD14-positive cell assessed as reduction in IFNgamma-induced STAT1 phosphorylation by flow cytometry analysisMore data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
AbbVie Bioresearch Center
Curated by ChEMBL
AbbVie Bioresearch Center
Curated by ChEMBL
Affinity DataIC50: 22nMAssay Description:Inhibition of JAK1/JAK3 in human T cell assessed as reduction in IL-15-induced STAT5 phosphorylation by flow cytometry analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 26nMAssay 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: 30nMAssay Description:Inhibition of TYK2 (unknown origin) by caliper technologyMore data for this Ligand-Target Pair
Affinity DataIC50: 43nMAssay Description:Inhibition of recombinant human JAK1 (845 to 1142 residues) expressed in Sf9 insect cells in presence of 0.1 mM of ATP by HTRF analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 43nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 43nMAssay Description:Inhibition of recombinant JAK1 (unknown origin) by alpha-screen assayMore data for this Ligand-Target Pair
Affinity DataIC50: 43nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 43nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 43nMAssay Description:Inhibition of JAK 1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 45nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 45nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2/Tyrosine-protein kinase JAK1/Tyrosine-protein kinase JAK2/Tyrosine-protein kinase JAK3(Human)
Genentech
Curated by ChEMBL
Genentech
Curated by ChEMBL
Affinity DataIC50: 45nMAssay Description:Inhibition of JAK in human BEAS-2B cells assessed as reduction in IL13-induced STAT6 phosphorylation incubated for 1 hr followed by IL13 addition and...More data for this Ligand-Target Pair
Affinity DataIC50: 47nMAssay Description:Inhibition of recombinant human GST-fused JAK1 (845 to 1142 residues) expressed in Sf9 cells at varying concentrations of ATP by competitive binding ...More data for this Ligand-Target Pair
Affinity DataIC50: 47nMAssay Description:Inhibition of recombinant human GST-tagged JAK1 catalytic domain (845 to 1142 residues) expressed in Sf9 cells in presence of ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 47nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 47nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 47nMAssay Description:Inhibition of GST-fused recombinant human JAK1 catalytic domain (845-1142 residues) expressed in Sf9 cells in presence of 0.1 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 47nMAssay Description:Inhibition of recombinant human JAK1 (845 to 1142 residues) expressed in Sf9 insect cells by Cheng-Prusoff equation analysisMore data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
AbbVie Bioresearch Center
Curated by ChEMBL
AbbVie Bioresearch Center
Curated by ChEMBL
Affinity DataIC50: 48nMAssay 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: 54nMAssay Description:Inhibition of recombinant human JAK3 (811 to 1103 residues) expressed in Sf9 insect cells in presence of 0.001 mM ATP by HTRF analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 55nMAssay Description:Inhibition of N-terminal/C-terminal his-tagged recombinant human TYK2 (880 to 1185 residues) expressed in Sf9 insect cells in presence of 0.1 mM by H...More data for this Ligand-Target Pair
Affinity DataIC50: 64nMAssay Description:Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino aci...More data for this Ligand-Target Pair
Affinity DataIC50: 68nMAssay Description:Inhibition of recombinant human JAK3 (811 to 1103 residues) expressed in Sf9 insect cells by TR-FRET analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 78nMAssay Description:Inhibition of JAK1 in human CD14-positive cell assessed as reduction in IL-6-induced STAT3 phosphorylation by flow cytometry analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 109nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 120nMAssay Description:Inhibition of recombinant JAK2 (unknown origin) by alpha-screen assayMore data for this Ligand-Target Pair
Affinity DataIC50: 120nMAssay Description:Inhibition of recombinant human C-terminal His6-tagged JAK2 (808 to end residues) expressed in baculovirus infected Sf21 cells at varying concentrati...More data for this Ligand-Target Pair
Affinity DataIC50: 120nMAssay Description:Inhibition of recombinant human JAK2 in presence of ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 120nMAssay Description:Inhibition of recombinant human JAK2 expressed in Sf9 insect cells in presence of 0.1 mM ATP by HTRF analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 120nMAssay Description:Inhibition of recombinant C-terminal His6-tagged human JAK2 kinase domain (808 to end residues) expressed in baculovirus-infected Sf21 cells in prese...More data for this Ligand-Target Pair
Affinity DataIC50: 120nMAssay Description:Inhibition of recombinant human JAK2 expressed in Sf9 insect cells by Cheng-Prusoff equation analysisMore data for this Ligand-Target Pair