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Janus kinase 3

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Target id: 2049

Nomenclature: Janus kinase 3

Abbreviated Name: JAK3

Family: Janus kinase (JakA) family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1124 19p13.11 JAK3 Janus kinase 3
Mouse - 1100 8 34.43 cM Jak3 Janus kinase 3
Rat - 1100 16p14 Jak3 Janus kinase 3
Previous and Unofficial Names Click here for help
JAKL | leukocyte Janus kinase | LJAK
Database Links Click here for help
Alphafold
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  JAK3 kinase domain in complex with 2-Cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid ((S)-1,2,2-trimethyl-propyl)-amide
PDB Id:  4HVD
Resolution:  1.85Å
Species:  Human
References:  47
Image of receptor 3D structure from RCSB PDB
Description:  JAK3 with Cyanamide CP34.
PDB Id:  6DB4
Ligand:  JAK3 inhibitor 34
Resolution:  1.7Å
Species:  Human
References:  11
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of JAK3 in complex with delgocitinib
PDB Id:  7C3N
Ligand:  delgocitinib
Resolution:  1.98Å
Species:  Human
References:  41
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
nezulcitinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 10.2 pKi 37
pKi 10.2 (Ki 6.3x10-11 M) [37]
delgocitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.3 pKi 50
pKi 8.3 (Ki 5.5x10-9 M) [50]
Description: In an assay using the kinase domain of the recombinant human enzyme, a biotinylated peptide substrate, and [33P]ATP.
izencitinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.0 – 9.0 pKi 31
pKi 7.0 – 9.0 (Ki 1x10-7 – 1x10-9 M) [31]
GDC-0214 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.7 pKi 20
pKi 7.7 (Ki 2.08x10-8 M) [20]
abivertinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 10.1 pIC50 59
pIC50 10.1 (IC50 9x10-11 M) [59]
Description: In a biochemical assay.
ritlecitinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 9.5 pIC50
pIC50 9.5 (IC50 3x10-10 M)
Description: At 4 μM ATP (Km).
AT-9283 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.0 pIC50 30
pIC50 9.0 (IC50 1.1x10-9 M) [30]
JAK inhibitor 17b Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.8 pIC50 22
pIC50 8.8 (IC50 1.67x10-9 M) [22]
PF-956980 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.6 pIC50 28
pIC50 8.6 (IC50 2.8x10-9 M) [28]
LASW1393 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.5 pIC50 5
pIC50 8.5 (IC50 3.5x10-9 M) [5]
JAK inhibitor I Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pIC50 52
pIC50 8.3 (IC50 5x10-9 M) [52]
compound 2 [PMID: 15546730] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 16
pIC50 8.2 (IC50 6x10-9 M) [16]
cerdulatinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.1 pIC50 18
pIC50 8.1 (IC50 8x10-9 M) [18]
decernotinib 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 7.1 – 8.9 pIC50 17
pIC50 8.9 (IC50 1.2x10-9 M) [17]
pIC50 7.1 (IC50 7.44x10-8 M) [17]
lepzacitinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition >8.0 pIC50 3
pIC50 >8.0 (IC50 <1x10-8 M) [3]
JAK3 inhibitor 32 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.0 pIC50 11
pIC50 8.0 (IC50 1.1x10-8 M) [11]
delgocitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.9 pIC50 41
pIC50 7.9 (IC50 1.3x10-8 M) [41]
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 6.7 – 9.0 pIC50 14,17,24,42
pIC50 8.2 (IC50 6x10-9 M) [42]
pIC50 6.7 – 9.0 (IC50 2.1x10-7 – 1x10-9 M) [14,24]
pIC50 7.3 (IC50 5.5x10-8 M) [17]
Description: In a biochemical enzyme assay.
compound 1d [PMID: 21493067] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 55
pIC50 7.8 (IC50 1.5x10-8 M) [55]
lazertinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition >7.7 pIC50 49
pIC50 >7.7 (IC50 <2x10-8 M) [49]
Description: In a biochemical enzyme activity assay.
PRN694 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.5 pIC50 63
pIC50 7.5 (IC50 3x10-8 M) [63]
momelotinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.8 – 8.2 pIC50 4,43
pIC50 8.2 (IC50 6.1x10-9 M) [4]
pIC50 6.8 (IC50 1.55x10-7 M) [43]
ibrutinib 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 10
pIC50 7.5 (IC50 3.2x10-8 M) [10]
ilginatinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pIC50 40
pIC50 7.4 (IC50 3.9x10-8 M) [40]
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 7.4 pIC50 61
pIC50 7.4 (IC50 3.9x10-8 M) [61]
ruxolitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.3 – 8.5 pIC50 17,29
pIC50 8.5 (IC50 3.22x10-9 M) [29]
pIC50 6.3 (IC50 4.87x10-7 M) [17]
compound 8l [PMID: 36053746] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 pIC50 36
pIC50 7.3 (IC50 4.62x10-8 M) [36]
gandotinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.3 pIC50 38
pIC50 7.3 (IC50 4.8x10-8 M) [38]
JAK3 inhibitor 34 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 7.3 pIC50 11
pIC50 7.3 (IC50 4.9x10-8 M) [11]
poseltinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition >7.3 pIC50 12
pIC50 >7.3 (IC50 <5x10-8 M) [12]
Description: Biochemical assay result. Binned IC50 value provided in patent.
CEE321 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.2 pIC50 51
pIC50 7.2 (IC50 5.9x10-8 M) [51]
PF-06263276 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.2 pIC50 33
pIC50 7.2 (IC50 5.99x10-8 M) [33]
BMS-911543 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pIC50 45
pIC50 7.1 (IC50 7.3x10-8 M) [45]
JAK3 inhibitor IV Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.1 pIC50 9
pIC50 7.1 (IC50 7.9x10-8 M) [9]
lorpucitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 34
pIC50 7.0 (IC50 9.22x10-8 M) [34]
Description: Determined in a biochemical high-throughput mass spectrometry (HTMS) assay.
compound 25ap [PMID: 37796543] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 62
pIC50 7.0 (IC50 9.1x10-8 M) [62]
compound 13ac [PMID: 33256400] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 60
pIC50 7.0 (IC50 9.4x10-8 M) [60]
oclacitinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.0 pIC50 7
pIC50 7.0 (IC50 9.51x10-8 M) [7]
mivavotinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.9 pIC50 35
pIC50 6.9 (IC50 1.15x10-7 M) [35]
JAK inhibitor 20a Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.9 pIC50 22
pIC50 6.9 (IC50 1.144x10-7 M) [22]
CEP-33779 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 21
pIC50 6.8 (IC50 1.5x10-7 M) [21]
XL019 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 25
pIC50 6.7 (IC50 2.142x10-7 M) [25]
compound 19a [PMID: 24359159] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 48
pIC50 6.7 (IC50 2.2x10-7 M) [48]
filgotinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.5 pIC50 53
pIC50 6.5 (IC50 8.1x10-7 M) [53]
solcitinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.4 pIC50 8
pIC50 6.4 (IC50 4.08x10-7 M) [8]
pacritinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pIC50 56
pIC50 6.3 (IC50 5.2x10-7 M) [56]
baricitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.1 pIC50 17
pIC50 6.1 (IC50 7.87x10-7 M) [17]
NIK inhibitor 12f Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.1 pIC50 64
pIC50 6.1 (IC50 8.92x10-7 M) [64]
Description: Inhibitory concentration determined in a Reaction Biology kinase sreening assay.
compound 30 [PMID: 37057760] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pIC50 46
pIC50 6.0 (IC50 9.54x10-7 M) [46]
fedratinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.0 pIC50 39
pIC50 6.0 (IC50 1x10-6 M) [39]
acalabrutinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition <6.0 pIC50 10
pIC50 <6.0 (IC50 >1x10-6 M) [10]
SAR-20347 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.8 pIC50 58
pIC50 5.8 (IC50 1.437x10-6 M) [58]
Description: In a TR-FRET assay.
JAK3 inhibitor II Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.7 pIC50 15
pIC50 5.7 (IC50 1.8x10-6 M) [15]
upadacitinib Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.6 pIC50 54
pIC50 5.6 (IC50 2.3x10-6 M) [54]
AZD1480 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.4 pIC50 27
pIC50 5.4 (IC50 3.63x10-6 M) [27]
brepocitinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.2 pIC50 23
pIC50 5.2 (IC50 6.494x10-6 M) [23]
peficitinib Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition >- pIC50 32
pIC50 [32]
Inhibitor Comments
The IC50 for filgotinib vs. JAK3 is >10 μM [17].
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 8.9 pKd 13
pKd 8.9 (Kd 1.4x10-9 M) [13]
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: 19,57

Key to terms and symbols Click column headers to sort
Target used in screen: JAK3(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 9.8 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.7 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.6 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.9 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 7.7 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.4 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.4 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 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: 2,26

Key to terms and symbols Click column headers to sort
Target used in screen: JAK3/JAK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
EGFR/ErbB-2/ErbB-4 inhibitor Small molecule or natural product Hs Inhibitor Inhibition -0.2 51.0 59.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.4 1.0 1.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 0.5 0.0 0.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.7 0.0 0.5
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 0.8 1.0 1.0
tofacitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 1.9
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 1.9 8.0 9.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.4 1.0 2.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 4.8 6.0 1.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.2 0.0 2.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
Psoriatic skin samples show elevated JAK3 (and JAK1) expression, with signalling predominantly through STAT3 [1]. JAK3 upregulation is observed in skin cells and dermal inflammatory infiltrate.
Noncoding mutation which creates a dominant splice site and reduces wild-type JAK3 protein expression is the cause of SCID/CID in siblings [44].
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  T cell (activation)
Immuno Process:  B cell (activation)
Immuno Process:  Immune regulation
Immuno Process:  Immune system development
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Combined immunodeficiency
Description: Combined immunodeficiency evolving into predominant CD4+ lymphopenia
Role: 
Disease:  Severe combined immunodeficiency, autosomal recessive, T cell-negative, B cell-positive, NK cell-negative
Synonyms: T-B+ severe combined immunodeficiency due to JAK3 deficiency [Orphanet: ORPHA35078]
Disease Ontology: DOID:0060008
OMIM: 600802
Orphanet: ORPHA35078
Biologically Significant Variants Click here for help
Type:  Missense mutation
Species:  Human
Description:  This mutation causes combined immunodeficiency evolving into predominant CD4+ lymphopenia.
Amino acid change:  Cys1066Arg
Nucleotide change:  T3196C
References:  6
Type:  Naturally occurring SNP
Species:  Human
Description:  An inherited non-coding homozygous mutation creating a dominant splice site and reduced wild-type protein expression causes SCID/CID.
Nucleotide change:  c.2652C>T
References:  44

References

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1. Alves de Medeiros AK, Speeckaert R, Desmet E, Van Gele M, De Schepper S, Lambert J. (2016) JAK3 as an Emerging Target for Topical Treatment of Inflammatory Skin Diseases. PLoS ONE, 11 (10): e0164080. [PMID:27711196]

2. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

3. 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.

4. 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]

5. 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]

6. Ban SA, Salzer E, Eibl MM, Linder A, Geier CB, Santos-Valente E, Garncarz W, Lion T, Ott R, Seelbach C et al.. (2014) Combined immunodeficiency evolving into predominant CD4+ lymphopenia caused by somatic chimerism in JAK3. J Clin Immunol, 34 (8): 941-53. [PMID:25205547]

7. 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.

8. 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.

9. 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]

10. Byrd JC, Harrington B, O'Brien S, Jones JA, Schuh A, Devereux S, Chaves J, Wierda WG, Awan FT, Brown JR et al.. (2016) Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. N Engl J Med, 374 (4): 323-32. [PMID:26641137]

11. 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]

12. Cha MY, Kang SJ, Kim MR, Lee JY, Jeon JY, Jo MG, Kwak EJ, Lee KO, Ha TH, Suh KH, Kim MS. (2011) Novel fused pyrimidine derivatives for inhd3ition of tyrosine kinase activity. Patent number: WO2011162515A2. Assignee: Hanmi Holdings Co. , Ltd.. Priority date: 23/06/2010. Publication date: 29/12/2011.

13. 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]

14. Changelian PS, Flanagan ME, Ball DJ, Kent CR, Magnuson KS, Martin WH, Rizzuti BJ, Sawyer PS, Perry BD, Brissette WH et al.. (2003) Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science, 302 (5646): 875-8. [PMID:14593182]

15. 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]

16. Chen P, Norris D, Das J, Spergel SH, Wityak J, Leith L, Zhao R, Chen BC, Pitt S, Pang S et al.. (2004) Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. Bioorg Med Chem Lett, 14 (24): 6061-6. [PMID:15546730]

17. 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]

18. 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]

19. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

20. Dengler HS, Wu X, Peng I, Rinderknecht CH, Kwon Y, Suto E, Kohli PB, Liimatta M, Barrett K, Lloyd J et al.. (2018) Lung-restricted inhibition of Janus kinase 1 is effective in rodent models of asthma. Sci Transl Med, 10 (468): eaao2151. [PMID:30463918]

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Janus kinase (JakA) family: Janus kinase 3. Last modified on 06/10/2023. Accessed on 23/06/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2049.