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Janus kinase 1

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 2047

Nomenclature: Janus kinase 1

Abbreviated Name: JAK1

Family: Janus kinase (JakA) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1154 1p31.3 JAK1 Janus kinase 1
Mouse - 1153 4 2.05 cM Jak1 Janus kinase 1
Rat - 1153 5 q31.3-q35 Jak1 Janus kinase 1
Previous and Unofficial Names Click here for help
JAK1A | JAK1B | JTK3
Database Links Click here for help
Alphafold P23458 (Hs), P52332 (Mm)
BRENDA 2.7.10.2
CATH/Gene3D 3.30.505.10, 1.20.80.10
ChEMBL Target CHEMBL2835 (Hs), CHEMBL2968 (Mm)
DrugBank Target P23458 (Hs)
Ensembl Gene ENSG00000162434 (Hs), ENSMUSG00000028530 (Mm), ENSRNOG00000011157 (Rn)
Entrez Gene 3716 (Hs), 16451 (Mm), 84598 (Rn)
Human Protein Atlas ENSG00000162434 (Hs)
KEGG Enzyme 2.7.10.2
KEGG Gene hsa:3716 (Hs), mmu:16451 (Mm), rno:84598 (Rn)
OMIM 147795 (Hs)
Pharos P23458 (Hs)
RefSeq Nucleotide NM_002227 (Hs), NM_146145 (Mm), NM_053466 (Rn)
RefSeq Protein NP_002218 (Hs), NP_666257 (Mm), NP_445918 (Rn)
UniProtKB P23458 (Hs), P52332 (Mm)
Wikipedia JAK1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  JAK1 kinase (JH1 domain) in complex with compound 26
PDB Id:  4E5W
Resolution:  1.86Å
Species:  Human
References:  30
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of JAK1 in complex with compound 25
PDB Id:  6BBU
Ligand:  abrocitinib
Resolution:  2.08Å
Species:  Human
References:  50
Image of receptor 3D structure from RCSB PDB
Description:  Human JAK1 in complex with LASW1393
PDB Id:  6HZU
Ligand:  LASW1393
Resolution:  2.2Å
Species:  Human
References:  4
Image of receptor 3D structure from RCSB PDB
Description:  Jak1 with compound 23
PDB Id:  6DBN
Ligand:  brepocitinib
Resolution:  2.48Å
Species:  Human
References:  16
Enzyme Reaction Click here for help
EC Number: 2.7.10.2

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 5e [PMID: 28580438] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.6 pKd 27
⤷ pKd 7.6 (Kd 2.8x10-8 M) [27]
Description: Measured using the JAK1 JH2 domain-pseudokinase.
nezulcitinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 10.2 pKi 34
⤷ pKi 10.2 (Ki 6.3x10-11 M) [34]
izencitinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition >10.0 pKi 24
⤷ pKi >10.0 (Ki <1x10-10 M) [24]
GDC-0214 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 9.6 pKi 14
⤷ pKi 9.6 (Ki 2.6x10-10 M) [14]
Description: Biochemical assay determination
delgocitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.7 pKi 46
⤷ pKi 8.7 (Ki 2.1x10-9 M) [46]
Description: In an assay using the kinase domain of the recombinant human enzyme, a biotinylated peptide substrate, and [33P]ATP.
lorpucitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.4 pIC50 29
⤷ pIC50 9.4 (IC50 4x10-10 M) [29]
Description: Determined in a biochemical high-throughput mass spectrometry (HTMS) assay.
ruxolitinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.2 – 10.1 pIC50 11,22,42
⤷ pIC50 8.5 – 10.1 (IC50 3.3x10-9 – 9x10-11 M) [22,42]
pIC50 8.2 (IC50 6x10-9 M) [11]
ivarmacitinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.7 pIC50 61
⤷ pIC50 8.7 (IC50 2x10-9 M) [61]
PF-06263276 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.7 pIC50 28
⤷ pIC50 8.7 (IC50 2.2x10-9 M) [28]
delgocitinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.6 pIC50 38
⤷ pIC50 8.6 (IC50 2.8x10-9 M) [38]
AZD1480 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition >8.5 pIC50 25
⤷ pIC50 >8.5 (IC50 <3x10-9 M) [25]
compound 19a [PMID: 24359159] Small molecule or natural product Click here for species-specific activity table Hs Inhibition >8.5 pIC50 45
⤷ pIC50 >8.5 (IC50 <3x10-9 M) [45]
londamocitinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition >8.5 pIC50 37
⤷ pIC50 >8.5 (IC50 <3x10-9 M) [37]
JAK inhibitor 20a Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.5 pIC50 15
⤷ pIC50 8.5 (IC50 3.37x10-9 M) [15]
peficitinib Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.4 pIC50 26
⤷ pIC50 8.4 (IC50 4x10-9 M) [26]
baricitinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.2 – 8.4 pIC50 11,18
⤷ pIC50 8.4 (IC50 4x10-9 M) [11]
pIC50 8.2 (IC50 5.9x10-9 M) [18]
itacitinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition >8.3 pIC50 23
⤷ pIC50 >8.3 (IC50 <5x10-9 M) [23]
LASW1393 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.3 pIC50 4
⤷ pIC50 8.3 (IC50 5.5x10-9 M) [4]
compound 25ap [PMID: 37796543] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 62
⤷ pIC50 8.2 (IC50 5.7x10-9 M) [62]
zemprocitinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.2 pIC50 53
⤷ pIC50 8.2 (IC50 5.95x10-9 M) [53]
solcitinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.2 pIC50 6
⤷ pIC50 8.2 (IC50 6.6x10-9 M) [6]
PF-956980 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 21
⤷ pIC50 8.1 (IC50 7.5x10-9 M) [21]
compound 8l [PMID: 36053746] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 33
⤷ pIC50 8.1 (IC50 8.9x10-9 M) [33]
oclacitinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.0 pIC50 5
⤷ pIC50 8.0 (IC50 9.53x10-9 M) [5]
WXFL10203614 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition >8.0 pIC50 58
⤷ pIC50 >8.0 (IC50 <1x10-8 M) [58]
lepzacitinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition >8.0 pIC50 2
⤷ pIC50 >8.0 (IC50 <1x10-8 M) [2]
girocitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition >8.0 pIC50 32
⤷ pIC50 >8.0 (IC50 <1x10-8 M) [32]
upadacitinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.4 – 8.5 pIC50 51
⤷ pIC50 8.5 (IC50 3x10-9 M) [51]
Description: at 1uM ATP in a biochemical assay
pIC50 7.4 (IC50 4.3x10-8 M) [51]
cerdulatinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.9 pIC50 12
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [12]
tofacitinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.8 pIC50 11
⤷ pIC50 7.8 (IC50 1.5x10-8 M) [11]
Description: In a biochemical enzyme assay.
brepocitinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.8 pIC50 16
⤷ pIC50 7.8 (IC50 1.7x10-8 M) [16]
momelotinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 – 8.0 pIC50 3,39
⤷ pIC50 8.0 (IC50 1.1x10-8 M) [39]
pIC50 7.6 (IC50 2.69x10-8 M) [3]
compound 18e [PMID: 31670517] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.6 pIC50 60
⤷ pIC50 7.6 (IC50 2.6x10-8 M) [60]
abrocitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.5 pIC50 50
⤷ pIC50 7.5 (IC50 2.9x10-8 M) [50]
ilginatinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 36
⤷ pIC50 7.5 (IC50 3.3x10-8 M) [36]
SAR-20347 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.2 – 7.6 pIC50 56
⤷ pIC50 7.6 (IC50 2.3x10-8 M) [56]
Description: In a 33P-ATP assay.
pIC50 7.2 (IC50 5.9x10-8 M) [56]
Description: In a TR-FRET assay.
decernotinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.9 – 7.9 pIC50 11
⤷ pIC50 7.9 (IC50 1.32x10-8 M) [11]
pIC50 6.9 (IC50 1.12x10-7 M) [11]
compound 30 [PMID: 37057760] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 41
⤷ pIC50 7.4 (IC50 4.102x10-8 M) [41]
compound 13ac [PMID: 33256400] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 59
⤷ pIC50 7.4 (IC50 4.2x10-8 M) [59]
CEE321 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.3 pIC50 47
⤷ pIC50 7.3 (IC50 5x10-8 M) [47]
zotiraciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 20
⤷ pIC50 7.2 (IC50 5.9x10-8 M) [20]
filgotinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.4 – 8.0 pIC50 11,49
⤷ pIC50 8.0 (IC50 1x10-8 M) [49]
pIC50 6.4 (IC50 3.63x10-7 M) [11]
golidocitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 44
⤷ pIC50 7.2 (IC50 7x10-8 M) [44]
Description: Inhbition of JAK1 enzymatic activity.
fedratinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.0 pIC50 35
⤷ pIC50 7.0 (IC50 1x10-7 M) [35]
JAK inhibitor 17b Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.9 pIC50 15
⤷ pIC50 6.9 (IC50 1.25x10-7 M) [15]
XL019 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.9 pIC50 17
⤷ pIC50 6.9 (IC50 1.343x10-7 M) [17]
NIK inhibitor 12f Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.7 pIC50 63
⤷ pIC50 6.7 (IC50 1.826x10-7 M) [63]
Description: Inhibitory concentration determined in a Reaction Biology kinase sreening assay.
povorcitinib Small molecule or natural product Hs Inhibition >6.5 pIC50 31
⤷ pIC50 >6.5 (IC50 <3x10-7 M) [31]
BMS-911543 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.4 pIC50 40
⤷ pIC50 6.4 (IC50 3.56x10-7 M) [40]
ropsacitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 19
⤷ pIC50 6.4 (IC50 3.83x10-7 M) [19]
pacritinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.9 pIC50 54
⤷ pIC50 5.9 (IC50 1.28x10-6 M) [54]
ritlecitinib Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.8 pIC50 48
⤷ pIC50 5.8 (IC50 1.64x10-6 M) [48]
Description: At 1 mM ATP.
JAK3 inhibitor 32 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.6 pIC50 8
⤷ pIC50 5.6 (IC50 2.703x10-6 M) [8]
JAK3 inhibitor 34 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.5 pIC50 8
⤷ pIC50 5.5 (IC50 3.345x10-6 M) [8]
JAK3 inhibitor II Small molecule or natural product Click here for species-specific activity table Hs Inhibition <5.0 pIC50 10
⤷ pIC50 <5.0 (IC50 >1x10-5 M) [10]
JAK3 inhibitor IV Small molecule or natural product Click here for species-specific activity table Hs Inhibition 4.4 pIC50 7
⤷ pIC50 4.4 (IC50 3.981x10-5 M) [7]
deuruxolitinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition - - 52
⤷ [52]
Inhibitor Comments
Binding to JAK1 pseudokinase domain, although potent, produces low functional activity in a JAK1/JAK3 dependent IL-2 stimulated cellular assay [57].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
deucravacitinib Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 9.0 pIC50 57
⤷ pIC50 9.0 (IC50 1x10-9 M) [57]
Description: Binding to JAK1 JH2 pseudokinase domain.
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
SJ988497 Small molecule or natural product Click here for species-specific activity table Hs Binding 8.0 pKd 9
⤷ pKd 8.0 (Kd 9.3x10-9 M) [9]
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 13,55
Key to terms and symbols Click column headers to sort
Target used in screen: JAK1(JH1domain-catalytic)
Ligand Sp. Type Action Value Parameter
tofacitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.8 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.2 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.1 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.7 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.1 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
Target used in screen: JAK1(JH2domain-pseudokinase)
Ligand Sp. Type Action Value Parameter
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: ...1
Key to terms and symbols Click column headers to sort
Target used in screen: nd/JAK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Small molecule or natural product Hs Inhibitor Inhibition 1.8
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.1
tofacitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 2.3
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.5
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 4.9
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.2
IKK-2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.4
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 16.3
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.2
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 22.2
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
The JAK1 tyrosine kinase is crucial for signaling of certain type I and type II cytokines, via receptors belonging to the IL-2, IL-4 and IL-6 receptor families as well as neurotrophin-1 and leptin receptors (all type I cytokine receptors). JAK1 is also involved in signalling via type II IL-10 family receptors, and receptors for type I and type II interferons (IFN-α/β and IFN-γ respectively).
Immuno Process Associations
Immuno Process:  Inflammation
Comment:  JAK1 is crucial for mediating the intracellular signals for a range of type I and type II cytokines, and for type I and type II interferons (IFN-α/β and IFN-γ respectively) following ligand-receptor interaction.
Immuno Process:  Immune regulation
Comment:  JAK1 is crucial for mediating the intracellular signals for a range of type I and type II cytokines, and for type I and type II interferons (IFN-α/β and IFN-γ respectively) following ligand-receptor interaction.
Immuno Process:  Cytokine production & signalling
Comment:  JAK1 is crucial for mediating the intracellular signals for a range of type I and type II cytokines, and for type I and type II interferons (IFN-α/β and IFN-γ respectively) following ligand-receptor interaction.
Physiological Consequences of Altering Gene Expression Click here for help
Disruption of the Jak1 gene demonstrates obligatory and nonredundant roles of the Jaks in cytokine-induced biologic responses. Jak1-/- cells fail to generate biologic responses to all class II cytokine receptors, cytokine receptors using the γc subunit or the IL6ST (gp130) subunits for signaling.
Species:  Mouse
Tissue: 
Technique:  Gene knockout.
References:  43

References

Show »

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2. Anderson DR, Hockerman SL, Blinn JR, Jacobsen EJ. (2019) Substituted pyrrolopyrimidine jak inhibitors and methods of making and using the same. Patent number: WO2019090158A1. Assignee: Aclaris Therapeutics, Inc.. Priority date: 02/10/2029. Publication date: 02/08/2029.

3. Asshoff M, Petzer V, Warr MR, Haschka D, Tymoszuk P, Demetz E, Seifert M, Posch W, Nairz M, Maciejewski P et al.. (2017) Momelotinib inhibits ACVR1/ALK2, decreases hepcidin production, and ameliorates anemia of chronic disease in rodents. Blood, 129 (13): 1823-1830. [PMID:28188131]

4. Bach J, Eastwood P, González J, Gómez E, Alonso JA, Fonquerna S, Lozoya E, Orellana A, Maldonado M, Calaf E et al.. (2019) Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases. J Med Chem, 62 (20): 9045-9060. [PMID:31609613]

5. Berlinski PJ, Birchmeier MJ, Bowman JW, Gonzales AJ, Kamerling SG, Mann DW, Mitton-Fry MJ. (2010) Pyrrolo[2,3-d]pyrimidine compounds. Patent number: WO2010020905. Assignee: Pfizer Inc.. Priority date: 20/08/2008. Publication date: 25/02/2010.

6. Blanc J. (2010) Novel compound useful for the treatment of degenerative and inflammatory diseases. Patent number: WO2010149771. Assignee: Galapagos Nv, Menet, Christel Jeanne Marie. Priority date: 26/06/2009. Publication date: 29/12/2010.

7. Brown GR, Bamford AM, Bowyer J, James DS, Rankine N, Tang E, Torr V, Culbert EJ. (2000) Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett, 10 (6): 575-9. [PMID:10741557]

8. Casimiro-Garcia A, Trujillo JI, Vajdos F, Juba B, Banker ME, Aulabaugh A, Balbo P, Bauman J, Chrencik J, Coe JW et al.. (2018) Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors. J Med Chem, 61 (23): 10665-10699. [PMID:30423248]

9. Chang Y, Min J, Jarusiewicz JA, Actis M, Yu-Chen Bradford S, Mayasundari A, Yang L, Chepyala D, Alcock LJ, Roberts KG et al.. (2021) Degradation of Janus kinases in CRLF2-rearranged acute lymphoblastic leukemia. Blood, 138 (23): 2313-2326. [PMID:34110416]

10. Changelian PS, Moshinsky D, Kuhn CF, Flanagan ME, Munchhof MJ, Harris TM, Whipple DA, Doty JL, Sun J, Kent CR et al.. (2008) The specificity of JAK3 kinase inhibitors. Blood, 111 (4): 2155-7. [PMID:18094329]

11. Clark JD, Flanagan ME, Telliez JB. (2014) Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases. J Med Chem, 57 (12): 5023-38. [PMID:24417533]

12. Coffey G, Betz A, DeGuzman F, Pak Y, Inagaki M, Baker DC, Hollenbach SJ, Pandey A, Sinha U. (2014) The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J Pharmacol Exp Ther, 351 (3): 538-48. [PMID:25253883]

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How to cite this page

Janus kinase (JakA) family: Janus kinase 1. Last modified on 06/03/2024. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2047.