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Found 30 Enz. Inhib. hit(s) for PDB: 3LXN
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataKi:  4.39nMAssay Description:Inhibition of human recombinant GST-tagged TYK2 using 5-FAM-KKSRGDYMTMQIG as substrate by peptide mobility shift assayMore data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataKi:  7.80nMAssay Description:Inhibition of TYK2More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataKi:  6.20E+5nMAssay 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
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  8.90nMAssay Description:A commercial assay by Reaction Biology Corp.More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  9nMAssay Description:Inhibition of human TYK2 using KKSRGDYMTMQIG as substrate in presence of 10 uM [gamma33P]ATP by radiometric methodMore data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  10nMAssay Description:Inhibition of TYK2 (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
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  10.4nMAssay 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
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  12nMAssay Description:Inhibition of N-terminal GST-tagged recombinant human TYK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 ...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  13nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  34nMAssay Description:Inhibition of Tyk2 by solution phase kinase assayMore data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  34nMAssay Description:Inhibition of recombinant GST-fused TYK2 kinase domain (870 to 1187) (unknown origin) harboring C1187S modification using 5-FAM-KKSRGDYMTMQIG as subs...More data for this Ligand-Target Pair
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  35nMAssay 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
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  35nMAssay 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
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  36nMAssay Description:Inhibition of recombinant human GST-tagged TYK2 catalytic domain expressed in baculovirus expression system using TK-substrate-biotin preincubated fo...More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  41nMpH: 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(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  52nMAssay Description:Inhibition of human recombinant N-terminal GST-tagged TYK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FR...More data for this Ligand-Target Pair
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
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
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  176nMAssay Description:Inhibition of GST-tagged Tyk2 expressed in insect cells using 35 uM ATPMore data for this Ligand-Target Pair
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
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
TargetNon-receptor tyrosine-protein kinase TYK2 [888-1187](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  230nMpH: 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
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  409nMAssay 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
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  472nMpH: 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(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  489nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  1.20E+3nMAssay Description:Inhibition of TEL-fused TYK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assayMore data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
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
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataKd:  4.80nMAssay Description:Binding constant for TYK2(JH1domain-catalytic) kinase domainMore data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for TYK2(JH2domain-pseudokinase) kinase domainMore data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataKd:  250nMAssay Description:Binding affinity to TYK2More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataKd:  620nMAssay Description:Binding affinity to TYK2More data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Argenta Discovery

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataKd:  620nMAssay Description:Binding constant for TYK2(Kin.Dom.2/JH1 - catalytic) kinase domainMore data for this Ligand-Target Pair