General Information of the Protein
Protein ID
PT04886
Protein Name
Tyrosine-protein kinase JAK2
Secondarily
Protein Name
Janus kinase 2
Gene Name
JAK2
Sequence
MGMACLTMTEMEATSTSPVHQNGDIPGSANSVKQIEPVLQVYLYHSLGQAEGEYLKFPSGEYVAEEICVAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHDILYRIRFYFPHWYCSGSSRTYRYGVSRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKEKDQTPLAVYNSVSYKTFLPKCVRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEQFEVKESARGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDVQLYCDFPDIIDVSIKQANQECSNESRIVTVHKQDGKVLEIELSSLKEALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIHSNCHGPISMDFAISKLKKAGNQTGLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENGEYNLSGTKRNFSNLKDLLNCYQMETVRSDSIIFQFTKCCPPKPKDKSNLLVFRTNGISDVQISPTLQRHNNVNQMVFHKIRNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHKTEVLLKVLDKAHRNYSESFFEAASMMSQLSHKHLVLNYGVCVCGEENILVQEFVKFGSLDTYLKKNKNSINILWKLGVAKQLAWAMHFLEEKSLIHGNVCAKNILLIREEDRRTGNPPFIKLSDPGISITVLPKDILQERIPWVPPECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDKHQLPAPKWTELANLINNCMDYEPDFRPAFRAVIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLRLIMEYLPYGSLRDYLQKHKERIDHKKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPVEFMRMIGNDKQGQMIVFHLIELLKSNGRLPRPEGCPDEIYVIMTECWNNNVSQRPSFRDLSLRVDQIRDSIAA
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Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase JakB family
Function
Non-receptor tyrosine kinase involved in various processes such as cell growth, development, differentiation or histone modifications. Mediates essential signaling events in both innate and adaptive immunity. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors such as growth hormone (GHR), prolactin (PRLR), leptin (LEPR), erythropoietin (EPOR), thrombopoietin (THPO); or type II receptors including IFN-alpha, IFN-beta, IFN-gamma and multiple interleukins. Following ligand-binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins. Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor. Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, cell stimulation with erythropoietin (EPO) during erythropoiesis leads to JAK2 autophosphorylation, activation, and its association with erythropoietin receptor (EPOR) that becomes phosphorylated in its cytoplasmic domain. Then, STAT5 (STAT5A or STAT5B) is recruited, phosphorylated and activated by JAK2. Once activated, dimerized STAT5 translocates into the nucleus and promotes the transcription of several essential genes involved in the modulation of erythropoiesis. Part of a signaling cascade that is activated by increased cellular retinol and that leads to the activation of STAT5 (STAT5A or STAT5B). In addition, JAK2 mediates angiotensin-2-induced ARHGEF1 phosphorylation. Plays a role in cell cycle by phosphorylating CDKN1B. Cooperates with TEC through reciprocal phosphorylation to mediate cytokine-driven activation of FOS transcription. In the nucleus, plays a key role in chromatin by specifically mediating phosphorylation of 'Tyr-41' of histone H3 (H3Y41ph), a specific tag that promotes exclusion of CBX5 (HP1 alpha) from chromatin.
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Uniprot ID
Primary ID:
Q62120

Secondarily ID:
G5E852
Q62124
Q7TQD0
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Ensembl ID
ENSG00000096968
Subcellular Location
Endomembrane system
Cytoplasm
Nucleus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0012129
INCB-018424
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C17H18N6
 1
1
EC50 = 186 nM
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CP0357998
(E)-1-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]-4-phenylbut-2-ene-1,4-dione
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C30H30N6O2
 1
1
IC50 = 10 nM
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CP0219569
methyl (E)-4-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-enoate
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C25H30N6O2
 1
1
IC50 = 10.3 nM
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CP0136525
(E)-1-(4-methylphenyl)-4-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-ene-1,4-dione
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C31H32N6O2
 1
1
IC50 = 12.8 nM
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CP0143654
(E)-4-(dimethylamino)-1-[7-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-en-1-one
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C26H33N7O
 1
1
IC50 = 24.5 nM
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CP0466385
(E)-4-(dimethylamino)-1-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-en-1-one
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C26H33N7O
 1
1
IC50 = 41 nM
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CP0561585
(E)-1-(4-methylphenyl)-4-[7-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-ene-1,4-dione
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C31H32N6O2
 1
1
IC50 = 50.5 nM
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CP0142408
2-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]acetonitrile
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C22H25N7
 1
1
IC50 = 57.8 nM
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CP0357574
(E)-1-[7-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]-4-phenylbut-2-ene-1,4-dione
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C30H30N6O2
 1
1
IC50 = 61.2 nM
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CP0466322
2-[7-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]acetonitrile
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C22H25N7
 1
1
IC50 = 75.5 nM
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CP0466326
methyl (E)-4-[7-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-enoate
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C25H30N6O2
 1
1
IC50 = 120 nM
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CP0466323
(E)-4-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-enoic acid
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C24H28N6O2
 1
1
IC50 = 128 nM
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CP0007710
2-[[1-[2-fluoro-4-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]phenyl]piperidin-4-yl]-methylamino]ethanol
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C25H34FN7O
 1
1
IC50 = 145 nM
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CP0553266
(E)-N-tert-butyl-4-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-enamide
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C28H37N7O
 1
1
IC50 = 145 nM
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CP0422139
3-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]propanenitrile
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C23H27N7
 1
1
IC50 = 177 nM
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CP0422129
4-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]butan-1-ol
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C24H32N6O
 1
1
IC50 = 234 nM
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CP0549513
(E)-N,N-diethyl-4-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-enamide
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C28H37N7O
 1
1
IC50 = 287 nM
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CP0426514
2-(2-ethoxyethyl)-N-[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]-3,4-dihydro-1H-isoquinolin-6-amine
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C24H32N6O
 1
1
IC50 = 302 nM
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CP0549517
5-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]pentan-1-ol
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C25H34N6O
 1
1
IC50 = 354 nM
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CP0571801
3-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]propan-1-ol
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C23H30N6O
 1
1
IC50 = 365 nM
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CP0466331
3-[6-[[5-fluoro-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]propan-1-ol
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C22H27FN6O
 1
1
IC50 = 392 nM
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CP0563063
5-[6-[[5-fluoro-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]pentan-1-ol
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C24H31FN6O
 1
1
IC50 = 420 nM
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CP0565768
2-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]ethanol
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C22H28N6O
 1
1
IC50 = 431 nM
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CP0549518
4-[6-[[5-fluoro-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]butan-1-ol
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C23H29FN6O
 1
1
IC50 = 445 nM
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CP0533189
N-[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]-2-prop-2-enyl-3,4-dihydro-1H-isoquinolin-6-amine
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C23H28N6
 1
1
IC50 = 452 nM
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CP0466328
2-butyl-N-[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]-3,4-dihydro-1H-isoquinolin-6-amine
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C24H32N6
 1
1
IC50 = 640 nM
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CP0565878
1-[6-[[5-fluoro-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]-2-hydroxyethanone
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C21H23FN6O2
 1
1
IC50 = 679 nM
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CP0422131
N-[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]-2-prop-2-ynyl-3,4-dihydro-1H-isoquinolin-6-amine
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C23H26N6
 1
1
IC50 = 695 nM
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CP0466324
2-[6-[[5-fluoro-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]ethanol
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C21H25FN6O
 1
1
IC50 = 760 nM
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CP0507670
1-(4-methylphenyl)-4-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]butane-1,4-dione
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C31H34N6O2
 1
1
IC50 = 784 nM
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CP0549512
2-but-2-ynyl-N-[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]-3,4-dihydro-1H-isoquinolin-6-amine
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C24H28N6
 1
1
IC50 = 908 nM
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CP0466377
methyl 4-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]butanoate
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C25H32N6O2
 1
1
IC50 = 938 nM
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CP0426511
(E)-4-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]-N-(2-piperidin-1-ylethyl)but-2-enamide
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C31H42N8O
 1
1
IC50 = 1200 nM
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CP0426508
6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-N-propyl-3,4-dihydro-1H-isoquinoline-2-carboxamide
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C24H31N7O
 1
1
IC50 = 1210 nM
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CP0425707
3-[2-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-7,8-dihydro-5H-1,6-naphthyridin-6-yl]propan-1-ol
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C22H29N7O
 1
1
IC50 = 1430 nM
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CP0139390
N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide
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C23H22N6O2
 1
1
IC50 = 1500 nM
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CP0422128
N-ethyl-6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinoline-2-carboxamide
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C23H29N7O
 1
1
IC50 = 1890 nM
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CP0553269
N-(3-chlorophenyl)-6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinoline-2-carboxamide
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C27H28ClN7O
 1
1
IC50 = 2180 nM
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CP0565766
2-[5-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-1,3-dihydroisoindol-2-yl]ethanol
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C21H26N6O
 1
1
IC50 = 2330 nM
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CP0466327
4-(dimethylamino)-1-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]butan-1-one
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C26H35N7O
 1
1
IC50 = 2480 nM
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CP0466383
2-[7-fluoro-6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]ethanol
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C22H27FN6O
 1
1
IC50 = 2570 nM
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CP0532772
2-[5-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-2,3-dihydroindol-1-yl]ethanol
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C21H26N6O
 1
1
IC50 = 4390 nM
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Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01214 Tyrosine-protein kinase JAK2 Homo sapiens, Human