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Information on EC 2.7.10.2 - non-specific protein-tyrosine kinase

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EC Tree
IUBMB Comments
Unlike EC 2.7.10.1, receptor protein-tyrosine kinase, this protein-tyrosine kinase does not have a transmembrane domain. In the human genome, 32 non-specific protein-tyrosine kinases have been identified and these can be divided into ten families .
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This record set is specific for:
UNIPROT: P52333
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Word Map
The enzyme appears in viruses and cellular organisms
Synonyms
bcr-abl, focal adhesion kinase, c-abl, zap-70, src kinase, janus kinase, v-src, ephb4, p56lck, bruton's tyrosine kinase, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Janus family kinase JAK3
-
Leukocyte janus kinase
-
tyrosine-protein kinase JAK3
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70 kDa zeta-associated protein
-
-
-
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ACTR-IIB
-
-
-
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ACTRIIA
-
-
-
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Agammaglobulinaemia tyrosine kinase
-
-
-
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Amylovoran biosynthesis membrane-associated protein amsA
-
-
-
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ATK
-
-
-
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B cell progenitor kinase
-
-
-
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B lymphocyte kinase
-
-
-
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B-cell/myeloid kinase
-
-
-
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BCR-ABL tyrosine kinase
-
-
-
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BMK
-
-
-
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BMP type II receptor
-
-
-
-
BMP-2/BMP-4 receptor
-
-
-
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Bone marrow kinase BMX
-
-
-
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BPK
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-
-
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Breast tumor kinase
-
-
-
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Bruton's tyrosine kinase
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-
-
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c-ABL
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-
-
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c-FER
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-
-
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C-FES
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-
-
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C-SRC
-
-
-
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C-SRC kinase
-
-
-
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C-YES
-
-
-
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CADTK
-
-
-
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CAK beta
-
-
-
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Calcium-dependent tyrosine kinase
-
-
-
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Cell adhesion kinase beta
-
-
-
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D-ash
-
-
-
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DFer
-
-
-
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Dsrc28C
-
-
-
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ectoprotein kinase
-
-
-
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Epithelial and endothelial tyrosine kinase
-
-
-
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EPS I polysaccharide export protein epsB
-
-
-
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focal adhesion kinase 1
-
-
-
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gene lck protein kinase
-
-
-
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gene lck tyrosine kinase
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-
-
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Hematopoietic consensus tyrosine-lacking kinase
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-
-
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Hemopoietic cell kinase
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-
-
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IL-2-inducible T-cell kinase
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-
-
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Itk
-
-
-
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JAK protein tyrosine kinase
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-
-
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Kinase EMB
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-
-
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Kinase EMT
-
-
-
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Kinase TLK
-
-
-
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kinase, protein (phosphorylating tyrosine)
-
-
-
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kinase, protein p56lck (phosphorylating)
-
-
-
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L-JAK
-
-
-
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Lck Tyrosine kinase
-
-
-
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Leukocyte janus kinase
-
-
-
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LSK
-
-
-
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nonreceptor protein tyrosine kinase
-
-
-
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NTK38
-
-
-
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Nuclear tyrosine protein kinase RAK
-
-
-
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ORF6
-
-
-
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p150
-
-
-
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p55-BLK
-
-
-
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P55-FGR
-
-
-
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p56-HCK
-
-
-
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p56-HCK/p59-HCK
-
-
-
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P56-LCK
-
-
-
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p56lck kinase
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-
-
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p56lck protein kinase
-
-
-
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p56lck protein tyrosine kinase
-
-
-
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p56lck tyrosine kinase
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-
-
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P57-STK
-
-
-
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P59-FYN
-
-
-
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p59-HCK/p60-HCK
-
-
-
-
P60-SRC
-
-
-
-
p60-YRK
-
-
-
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P61-YES
-
-
-
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p94-FER
-
-
-
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phosphotyrosyl-protein kinase
-
-
-
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PP125FAK
-
-
-
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Protein kinase (tyrosine-phosphorylating)
-
-
-
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protein kinase A
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-
-
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Protein kinase BATK
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-
-
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Protein kinase HYL
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-
-
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Protein kinase Lck
-
-
-
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Protein kinase NTK
-
-
-
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Protein kinase p56-LCK
-
-
-
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Protein kinase p56lck
-
-
-
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Protein p56c-lck kinase
-
-
-
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Protein p56lck tyrosine kinase
-
-
-
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Protein tyrosine kinase
-
-
-
-
protein tyrosine kinase 2beta
-
-
-
-
Protein tyrosine kinase lck
-
-
-
-
Protein tyrosine kinase p56lck
-
-
-
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Protein tyrosine kinase pp56lck
-
-
-
-
Protein-tyrosine kinase C-TKL
-
-
-
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Protein-tyrosine kinase CYL
-
-
-
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PTK
-
-
-
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PTK-RL-18
-
-
-
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PTK70
-
-
-
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Quek1
-
-
-
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Related adhesion focal tyrosine kinase
-
-
-
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Resting lymphocyte kinase
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-
-
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Rlk/Txk
-
-
-
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S-domain receptor-like protein kinase
-
-
-
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SLK
-
-
-
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Spleen tyrosine kinase
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-
-
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src-kinase
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-
-
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SRC-related intestinal kinase
-
-
-
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Syk-related tyrosine kinase
-
-
-
-
SYN
-
-
-
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T cell-specific protein-tyrosine kinase
-
-
-
-
T-cell-specific kinase
-
-
-
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Tyrosine kinase
-
-
-
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Tyrosine kinase ARG
-
-
-
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Tyrosine kinase lck
-
-
-
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Tyrosine kinase p56lck
-
-
-
-
Tyrosine phosphokinase
-
-
-
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Tyrosine protein kinase
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-
-
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Tyrosine protein kinase p56lck
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-
-
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Tyrosine-protein kinase brk
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-
-
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Tyrosine-protein kinase CTK
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-
-
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Tyrosine-protein kinase Lyk
-
-
-
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Tyrosine-protein kinase TYRO 10
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-
-
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Tyrosine-specific protein kinase
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-
-
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Tyrosylprotein kinase
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-
-
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v-fps Protein-tyrosine kinase
-
-
-
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WEE1hu
-
-
-
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YES related kinase
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:[protein]-L-tyrosine O-phosphotransferase (non-specific)
Unlike EC 2.7.10.1, receptor protein-tyrosine kinase, this protein-tyrosine kinase does not have a transmembrane domain. In the human genome, 32 non-specific protein-tyrosine kinases have been identified and these can be divided into ten families [1].
CAS REGISTRY NUMBER
COMMENTARY hide
114051-78-4
p56lck protein kinase
80449-02-1
protein-tyrosine kinase
9026-43-1
this CAS Reg. No. encompasses a great variety of protein kinases including the serine/threonine specific kinases
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + [Signal Transducer and Activation of Transcription (STAT) protein]-L-tyrosine
ADP + [Signal Transducer and Activation of Transcription (STAT) protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
additional information
?
-
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
-
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000085
3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000064
3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000028
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000046
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000023
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000092
3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000032
3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000053
3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000012
3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000052
3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000046
3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.0000033
3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
Homo sapiens
37°C, pH not specified in the publication
0.000025
baricitinib
Homo sapiens
37°C, pH not specified in the publication
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
hematopoietic cancer cells
Manually annotated by BRENDA team
hematopoietic and epithelial cancer cells
Manually annotated by BRENDA team
epithelial cancer cells
Manually annotated by BRENDA team
expressed in primary human vascular cells, as well as other non-lymphoid and non-myeloid cell types
Manually annotated by BRENDA team
additional information
three splice variants are isolated from different mRNA sources: breast, spleen, and activated monocytes. JAK3 splice isoforms are functional in JAK3 signaling and may enrich the complexity of the intracellular responses functional in IL-2 or cytokine signaling
Manually annotated by BRENDA team
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
JAK3_HUMAN
1124
0
125099
Swiss-Prot
other Location (Reliability: 3)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Bozzi, F.; Lefranc, G.; Villa, A.; Badolato, R.; Schumacher, R.F.; Khalil, G.; Loiselet, J.; Bresciani, S.; O'Shea, J.J.; Vezzoni, P.; Notarangelo, L.D.; Candotti, F.
Molecular and biochemical characterization of JAK3 deficiency in a patient with severe combined immunodeficiency over 20 years after bone marrow transplantation: implications for treatment
Br. J. Haematol.
102
1363-1366
1998
Homo sapiens (P52333)
Manually annotated by BRENDA team
Candotti, F.; Oakes, S.A.; Johnston, J.A.; Giliani, S.; Schumacher, R.F.; Mella, P.; Fiorini, M.; Ugazio, A.G.; Badolato, R.; Notarangelo, L.D.; Bozzi, F.; Macchi, P.; Strina, D.; Vezzoni, P.; Blaese, R.M.; O'Shea, J.J.; Villa, A.
Structural and functional basis for JAK3-deficient severe combined immunodeficiency
Blood
90
3996-4003
1997
Homo sapiens (P52333), Homo sapiens
Manually annotated by BRENDA team
Kawamura, M.; McVicar, D.W.; Johnston, J.A.; Blake, T.B.; Chen, Y.Q.; Lal, B.K.; Lloyd, A.R.; Kelvin, D.J.; Staples, J.E.; Ortaldo, J.R.; et al.
Molecular cloning of L-JAK, a Janus family protein-tyrosine kinase expressed in natural killer cells and activated leukocytes
Proc. Natl. Acad. Sci. USA
91
6374-6378
1994
Homo sapiens (P52333)
Manually annotated by BRENDA team
Lai, K.S.; Jin, Y.; Graham, D.K.; Witthuhn, B.A.; Ihle, J.N.; Liu, E.T.
A kinase-deficient splice variant of the human JAK3 is expressed in hematopoietic and epithelial cancer cells
J. Biol. Chem.
270
25028-25036
1995
Homo sapiens (P52333)
Manually annotated by BRENDA team
Macchi, P.; Villa, A.; Giliani, S.; Sacco, M.G.; Frattini, A.; Porta, F.; Ugazio, A.G.; Johnston, J.A.; Candotti, F.; O'Shea, J.J.; et al.
Mutations of Jak-3 gene in patients with autosomal severe combined immune deficiency (SCID)
Nature
377
65-68
1995
Homo sapiens (P52333)
Manually annotated by BRENDA team
Schumacher, R.F.; Mella, P.; Badolato, R.; Fiorini, M.; Savoldi, G.; Giliani, S.; Villa, A.; Candotti, F.; Tampalini, A.; O'Shea, J.J.; Notarangelo, L.D.
Complete genomic organization of the human JAK3 gene and mutation analysis in severe combined immunodeficiency by single-strand conformation polymorphism
Hum. Genet.
106
73-79
2000
Homo sapiens (P52333)
Manually annotated by BRENDA team
Verbsky, J.W.; Bach, E.A.; Fang, Y.F.; Yang, L.; Randolph, D.A.; Fields, L.E.
Expression of Janus kinase 3 in human endothelial and other non-lymphoid and non-myeloid cells
J. Biol. Chem.
271
13976-13980
1996
Homo sapiens (P52333), Homo sapiens
Manually annotated by BRENDA team
Yogo, T.; Nagamiya, H.; Seto, M.; Sasaki, S.; Shih-Chung, H.; Ohba, Y.; Tokunaga, N.; Lee, G.N.; Rhim, C.Y.; Yoon, C.H.; Cho, S.Y.; Skene, R.; Yamamoto, S.; Satou, Y.; Kuno, M.; Miyazaki, T.; Nakagawa, H.; Okabe, A.; Marui, S.; Aso, K.; Yoshida, M.
Structure-based design and synthesis of 3-amino-1,5-dihydro-4H-pyrazolopyridin-4-one derivatives as tyrosine kinase 2 inhibitors
J. Med. Chem.
59
733-749
2016
Homo sapiens (O60674), Homo sapiens (P23458), Homo sapiens (P29597), Homo sapiens (P52333), Homo sapiens
Manually annotated by BRENDA team