Compile Data Set for Download or QSAR
Report error Found 21 Enz. Inhib. hit(s) for PDB: 5USY
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataIC50: 1nMAssay Description:Inhibition of JAK2 JH2 V617F mutant in human HEL cells assessed as reduction in STAT5 phosphorylation at 0.5 to 25 uM measured after 1 hrs by Western...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  31nMAssay Description:Binding affinity to N-terminal TEV-cleavable hexa-histidine tagged human JAK2 JH1 domain (840 to 1132 residues) expressed in baculovirus-infected Sf9...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/18/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  94nMAssay Description:Binding affinity to human C-terminal His8-tagged JAK2 pseudokinase (513 to 827 residues) expressed in baculovirus infected Hi-5 cells by intrinsic tr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  220nMAssay Description:Binding affinity to JAK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/3/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  220nMAssay Description:Binding affinity to JAK2 JH1 domain (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/18/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  220nMAssay Description:Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  220nMAssay Description:Binding affinity to human JAK2 (kinase domain 2/JH1 catalytic domain) by competitive binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  456nMAssay Description:Binding affinity to JAK2 JH2 (unknown origin) expressed in baculovirus infected Sf9 cells assessed as dissociation constant measured upto 30 mins in ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  456nMAssay Description:Binding affinity to wild type human C-terminal thrombin cleavage site-fused/ 6xHis-tagged JAK2 JH2 pseudokinase domain (536 to 812 residues) expresse...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  460nMAssay Description:Binding affinity to wild type JAK2 JH2 pseudokinase domain (unknown origin) expressed in Sf9 cells and measured upto 30 mins by competitive fluoresce...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  460nMAssay Description:Binding affinity to wild type full length JAK2 JH2 (unknown origin) expressed in HEK293 cells assessed as dissociation constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  490nMAssay Description:Binding affinity to wild type human C-terminal thrombin cleavage site-fused/ 6xHis-tagged JAK2 JH2 pseudokinase domain (536 to 812 residues) expresse...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  600nMAssay Description:Binding affinity to human C-terminal thrombin cleavage site-fused/ 6xHis-tagged JAK2 JH2 pseudokinase domain V617F mutant (536 to 812 residues) expre...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  600nMAssay Description:Binding affinity to JAK2 V617F mutant (unknown origin) assessed as dissociation constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2 [808-1132](Human)
Yale University

US Patent
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  670nMAssay Description:In a flat black bottom 96 well plate (Corning), the buffer (20 mM Tris-HCl pH 8.0, 150 mM NaCl, 20% Glycerol, 0.5 mM TCEP, 0.01% Tween 20) is added&#...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2025
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  670nMAssay Description:Binding affinity to JAK2 JH1 (unknown origin) assessed as dissociation constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  670nMAssay Description:Binding affinity to wild type human N-terminal TEV cleavage site-fused/His6-tagged JAK2 JH1 domain (840 to 1132 residues) expressed in baculovirus in...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  800nMAssay Description:Binding affinity to wild type JAK2 JH2 domain (unknown origin) by competitive fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/18/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataIC50: 2.96E+3nMAssay Description:Inhibition of wild type full length human JAK2 (1 to 1132 residues) autophosphorylation expressed in HEK293T cells incubated in buffer with compound ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataIC50: 1.11E+4nMAssay Description:Inhibition of full length human C-terminal FLAG-tagged JAK2 V617F mutant (1 to 1132 residues) autophosphorylation expressed in HEK293T cells incubate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Yale University

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKi:  2.20E+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
In Depth
Date in BDB:
4/22/2011
Entry Details
PCBioAssayPDB3D3D Structure (crystal)