General Information of the Protein
Protein ID
PT00892
Protein Name
Tyrosine-protein kinase JAK3
Secondarily
Protein Name
Janus kinase 3
Leukocyte janus kinase
Gene Name
JAK3
Sequence
MAPPSEETPLIPQRSCSLLSTEAGALHVLLPARGPGPPQRLSFSFGDHLAEDLCVQAAKASGILPVYHSLFALATEDLSCWFPPSHIFSVEDASTQVLLYRIRFYFPNWFGLEKCHRFGLRKDLASAILDLPVLEHLFAQHRSDLVSGRLPVGLSLKEQGECLSLAVLDLARMAREQAQRPGELLKTVSYKACLPPSLRDLIQGLSFVTRRRIRRTVRRALRRVAACQADRHSLMAKYIMDLERLDPAGAAETFHVGLPGALGGHDGLGLLRVAGDGGIAWTQGEQEVLQPFCDFPEIVDISIKQAPRVGPAGEHRLVTVTRTDNQILEAEFPGLPEALSFVALVDGYFRLTTDSQHFFCKEVAPPRLLEEVAEQCHGPITLDFAINKLKTGGSRPGSYVLRRSPQDFDSFLLTVCVQNPLGPDYKGCLIRRSPTGTFLLVGLSRPHSSLRELLATCWDGGLHVDGVAVTLTSCCIPRPKEKSNLIVVQRGHSPPTSSLVQPQSQYQLSQMTFHKIPADSLEWHENLGHGSFTKIYRGCRHEVVDGEARKTEVLLKVMDAKHKNCMESFLEAASLMSQVSYRHLVLLHGVCMAGDSTMVQEFVHLGAIDMYLRKRGHLVPASWKLQVVKQLAYALNYLEDKGLPHGNVSARKVLLAREGADGSPPFIKLSDPGVSPAVLSLEMLTDRIPWVAPECLREAQTLSLEADKWGFGATVWEVFSGVTMPISALDPAKKLQFYEDRQQLPAPKWTELALLIQQCMAYEPVQRPSFRAVIRDLNSLISSDYELLSDPTPGALAPRDGLWNGAQLYACQDPTIFEERHLKYISQLGKGNFGSVELCRYDPLGDNTGALVAVKQLQHSGPDQQRDFQREIQILKALHSDFIVKYRGVSYGPGRQSLRLVMEYLPSGCLRDFLQRHRARLDASRLLLYSSQICKGMEYLGSRRCVHRDLAARNILVESEAHVKIADFGLAKLLPLDKDYYVVREPGQSPIFWYAPESLSDNIFSRQSDVWSFGVVLYELFTYCDKSCSPSAEFLRMMGCERDVPALCRLLELLEEGQRLPAPPACPAEVHELMKLCWAPSPQDRPSFSALGPQLDMLWSGSRGCETHAFTAHPEGKHHSLSFS
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Organism
Homo sapiens, Human
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, or differentiation. Mediates essential signaling events in both innate and adaptive immunity and plays a crucial role in hematopoiesis during T-cells development. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors sharing the common subunit gamma such as IL2R, IL4R, IL7R, IL9R, IL15R and IL21R. 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, upon IL2R activation by IL2, JAK1 and JAK3 molecules bind to IL2R beta (IL2RB) and gamma chain (IL2RG) subunits inducing the tyrosine phosphorylation of both receptor subunits on their cytoplasmic domain. Then, STAT5A and STAT5B are recruited, phosphorylated and activated by JAK1 and JAK3. Once activated, dimerized STAT5 translocates to the nucleus and promotes the transcription of specific target genes in a cytokine-specific fashion.
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Uniprot ID
Primary ID:
P52333

Secondarily ID:
Q13259
Q13260
Q13611
Q8N1E8
Q99699
Q9Y6S2
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Ensembl ID
ENSG00000105639
HGNC ID
HGNC:6193
Subcellular Location
Endomembrane system
Cytoplasm
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
CP0957903
5-(6-acetamidopyrimidin-4-yloxy)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)indoline-1-carboxamide
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C28H30F3N7O3
 1
1
GI50 = 451 nM
   TI
   LI
   LO
   TS
CP0002393
3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile
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C16H20N6O
 2
1
GI50 = 503 nM
   TI
   LI
   LO
   TS
2
IC50 = 54 nM
   TI
   LI
   LO
   TS
CP0807417
4-(((2S,4S)-1-(4-Chlorobenzyl)-2-methylpiperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
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C22H26ClN5O
 1
1
GI50 = 1141 nM
   TI
   LI
   LO
   TS
CP0065873
1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]-2-(dimethylamino)ethanone
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C26H29N7O2
 1
1
GI50 = 2500 nM
   TI
   LI
   LO
   TS
CP0807413
4-((8-(4-Chlorobenzyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
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C23H26ClN5O
 1
1
GI50 = 3895 nM
   TI
   LI
   LO
   TS
CP0387299
4-(methylamino)-2-[4-methyl-3-(propanoylamino)anilino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]pyrimidine-5-carboxamide
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C31H30F3N7O3
 1
1
GI50 = 8300 nM
   TI
   LI
   LO
   TS
CP0224766
4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]-N-[2-methyl-5-[(3,4,5-trimethoxybenzoyl)amino]phenyl]pyrimidine-5-carboxamide
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C33H35N7O6
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0387298
4-(methylamino)-2-[4-methyl-3-(propanoylamino)anilino]-N-[2-methyl-5-[(3,4,5-trimethoxybenzoyl)amino]phenyl]pyrimidine-5-carboxamide
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C33H37N7O6
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0389976
4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]pyrimidine-5-carboxamide
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C31H28F3N7O3
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0008628
US10112907, Example 00033
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C21H23N5O3S
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0807416
4-((cis-3-Fluoro-1-(3-methoxybenzyl)piperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
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C22H26FN5O2
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0952685
4-((trans-1-(3-Chlorobenzyl)-2-methylpiperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
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C22H26ClN5O
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0952760
4-((1-(3-Chlorobenzyl)azepan-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
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C22H26ClN5O
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0001071
4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-[2-(dimethylamino)ethyl]thieno[3,2-c]pyridine-7-carboxamide
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C22H29N5O3S2
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0001781
4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-methoxyethyl)thieno[3,2-c]pyridine-7-carboxamide
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C21H26N4O4S2
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0001805
4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-morpholin-4-ylethyl)thieno[3,2-c]pyridine-7-carboxamide
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C24H31N5O4S2
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0008918
4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-methylthieno[3,2-c]pyridine-7-carboxamide
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C19H22N4O3S2
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0009734
4-amino-2-(4-morpholin-4-ylphenyl)thieno[3,2-c]pyridine-7-carboxamide
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C18H18N4O2S
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0388710
4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-hydroxyethyl)thieno[3,2-c]pyridine-7-carboxamide
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C20H24N4O4S2
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0392929
4-amino-2-[4-(2-cyanopropan-2-yl)phenyl]-N-methylthieno[3,2-c]pyridine-7-carboxamide
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C19H18N4OS
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0392977
4-amino-N-methyl-2-phenylthieno[3,2-c]pyridine-7-carboxamide
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C15H13N3OS
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0392981
4-amino-N-methyl-2-(4-methylphenyl)thieno[3,2-c]pyridine-7-carboxamide
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C16H15N3OS
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0393021
4-amino-2-(4-tert-butylphenyl)-N-methylthieno[3,2-c]pyridine-7-carboxamide
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C19H21N3OS
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0417017
4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-piperidin-1-ylethyl)thieno[3,2-c]pyridine-7-carboxamide
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C25H33N5O3S2
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0417018
4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(3-morpholin-4-ylpropyl)thieno[3,2-c]pyridine-7-carboxamide
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C25H33N5O4S2
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0441323
4-amino-N-methyl-2-(4-morpholin-4-ylphenyl)thieno[3,2-c]pyridine-7-carboxamide
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C19H20N4O2S
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0441325
4-amino-N-methyl-2-[4-(trifluoromethoxy)phenyl]thieno[3,2-c]pyridine-7-carboxamide
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C16H12F3N3O2S
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0002393
3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile
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C16H20N6O
 30
1 EC50 < 5 nM
2 IC50 = 0.24 nM
3 IC50 = 0.29 nM
4 IC50 = 0.35 nM
5 IC50 = 0.7 nM
6 IC50 = 0.8 nM
7 IC50 = 0.98 nM
8 IC50 = 1 nM
9 IC50 = 1.1 nM
10 IC50 = 1.4 nM
11 IC50 = 1.5 nM
12 IC50 = 1.6 nM
13 IC50 = 2 nM
14 IC50 = 2.2 nM
15 IC50 = 3.2 nM
16 IC50 = 5 nM
17 IC50 = 8.5 nM
18 IC50 = 10.9 nM
19 IC50 = 13 nM
20 IC50 = 55 nM
21 IC50 = 76 nM
22 IC50 = 93.5 nM
23 IC50 >= 8000 nM
24 Kd = 0.16 nM
25 Kd = 0.7 nM
26 Kd = 2.2 nM
27 Ki = 0.2 nM
28 Ki = 0.24 nM
29 Ki = 0.4 nM
30 Ki = 1 nM
CP0004106
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
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C28H26N4O3
 13
1 IC50 = 0.0913 nM
2 IC50 = 0.1 nM
3 IC50 = 0.12 nM
4 IC50 = 0.138 nM
5 IC50 = 0.15 nM
6 IC50 = 0.184 nM
7 IC50 = 0.5 nM
8 IC50 < 1 nM
9 IC50 = 1 nM
10 IC50 = 8 nM
11 IC50 < 100 nM
12 Kd = 10 nM
13 Kd = 12 nM
CP0633840
(E/Z)-2-Cyano-3-(5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]-pyrrolo[2,3-b]pyridin-2-yl)furan-2-yl)-N,N-dimethylacrylamide
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C24H24N6O2
 3
1 IC50 = 0.13 nM
2 IC50 = 2 nM
3 IC50 = 9 nM
CP0013024
(E)-3-[5-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)furan-2-yl]prop-2-enenitrile
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C21H19N5O
 1
1 IC50 = 0.21 nM
CP0014161
2-[[5-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)furan-2-yl]methylidene]propanedinitrile
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C22H18N6O
 1
1 IC50 = 0.39 nM
CP0013026
3-{5-[4-(2-Hydroxy-2-methyl-propionyl)-piperazin-1-yl]-2-trifluoromethyl-phenyl}-4-(1H-indol-3-yl)-pyrrole-2,5-dione
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C27H25F3N4O4
 2
1 IC50 = 0.5 nM
2 IC50 = 1 nM
CP0014520
[(1S)-6-[5-[3-(hydroxymethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2,3-dihydro-1H-inden-1-yl]cyanamide
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C23H19N5O
 3
1 IC50 = 0.5 nM
2 IC50 = 78 nM
3 IC50 > 10000 nM
CP0014853
N-[3-[5-(2-methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]prop-2-enamide
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C18H18N4O2
 3
1 IC50 = 0.5 nM
2 IC50 = 31 nM
3 IC50 = 953 nM
CP0001797
[(1S)-6-(5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamide
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C22H17N5
 3
1 IC50 = 0.7 nM
2 IC50 = 49 nM
3 IC50 > 10000 nM
CP0008733
[(1S)-1-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydroinden-1-yl]cyanamide
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C17H15N5
 3
1 IC50 = 0.7 nM
2 IC50 = 56 nM
3 IC50 = 5480 nM
CP0637281
(E/Z)-3-(5-(1-Cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]-pyridin-2-yl)furan-2-yl)-2-(4-methylpiperazine-1-carbonyl)-acrylonitrile
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C27H29N7O2
 1
1 IC50 = 0.74 nM
CP0013445
N-[(1R,3S)-3-(cyanoamino)-5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]methanesulfonamide
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C17H16N6O2S
 2
1 IC50 = 0.9 nM
2 IC50 = 38 nM
CP0004519
[(1S,3R)-3-hydroxy-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamide
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C16H13N5O
 2
1 IC50 = 1 nM
2 IC50 = 163 nM
CP0104423
US10399979, Compound 17d
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C24H27N3O3
 1
1 IC50 = 1.01 nM
CP0230502
US10399979, Compound 17c
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C23H25N3O3
 1
1 IC50 = 1.09 nM
CP0238761
US10399979, Compound 17b
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C23H25N3O3
 1
1 IC50 = 1.65 nM
CP0807417
4-(((2S,4S)-1-(4-Chlorobenzyl)-2-methylpiperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
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C22H26ClN5O
 1
1 IC50 = 2.31 nM
CP0756820
(R)-3-(3-(7,8-Dimethoxy-5-oxo-1,5-dihydro-4H-benzo[c]-pyrrolo[2,3-h][1,6]naphthyridin-4-yl)piperidin-1-yl)-3-oxopropanenitrile
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C24H23N5O4
 1
1 IC50 = 2.55 nM
CP0012129
INCB-018424
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C17H18N6
 14
1 IC50 = 2.8 nM
2 IC50 = 10.7 nM
3 IC50 = 14.6 nM
4 IC50 = 20.7 nM
5 IC50 = 428 nM
6 IC50 = 430 nM
7 IC50 = 487 nM
8 IC50 = 1940 nM
9 IC50 > 300 nM
10 IC50 > 400 nM
11 IC50 >= 8000 nM
12 Kd = 2 nM
13 Ki = 3.2 nM
14 Ki = 3.22 nM
CP0083241
US10399979, Compound 17a
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C22H23N3O3
 1
1 IC50 = 2.92 nM
CP0001795
2,2-difluoro-6-[5-(2-methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-3H-1,4-benzoxazine-4-carbonitrile
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C18H15F2N5O2
 3
1 IC50 = 3 nM
2 IC50 = 456 nM
3 IC50 = 7252 nM
CP0004518
[(1S)-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamide
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C16H13N5
 3
1 IC50 = 3 nM
2 IC50 = 256 nM
3 IC50 > 10000 nM
CP0308346
(R)-3-(6-(1-(4-fluorophenyl)ethylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine
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C18H16FN7
 1
1 IC50 = 7 nM
CP0015934
(S)-5-fluoro-2-(1-(5-fluoropyridin-2-yl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile
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C17H15F2N7
 2
1 IC50 = 7 nM
2 IC50 = 15 nM
CP0145368
3-[2-[5-methyl-2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-6,7-dihydro-4H-furo[3,2-c]pyridin-5-yl]-3-oxopropanenitrile
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C25H26N6O3
 1
1 IC50 = 7.6 nM
CP0153918
4-N-[(1S)-1-(3,5-difluoropyridin-2-yl)ethyl]-5-fluoro-2-N-(5-methyl-1H-pyrazol-3-yl)-6-morpholin-4-ylpyrimidine-2,4-diamine
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C19H21F3N8O
 1
1 IC50 = 8 nM
CP0035351
(S)-5-fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile
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C18H16F2N6
 1
1 IC50 = 9 nM
CP0207126
(R)-3-(6-(1-(4-fluorophenyl)butylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine
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C20H20FN7
 1
1 IC50 = 10 nM
CP0007430
IBRUTINIB
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C25H24N6O2
 6
1 IC50 = 10 nM
2 IC50 = 16.1 nM
3 IC50 = 22 nM
4 IC50 = 32 nM
5 Kd = 21 nM
6 Kd = 37 nM
CP0001796
N-[(1R,3S)-3-(cyanoamino)-5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-3-fluorobenzenesulfonamide
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C22H17FN6O2S
 2
1 IC50 = 11 nM
2 IC50 > 10000 nM
CP0089651
(R)-3-(6-(1-(4-fluorophenyl)propylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine
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C19H18FN7
 1
1 IC50 = 12 nM
CP0252996
(R)-3-(6-(1-(4-fluorophenyl)-2-methylpropylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine
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C20H20FN7
 1
1 IC50 = 12 nM
CP0165499
3-[2-[5-methyl-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]-6,7-dihydro-4H-furo[3,2-c]pyridin-5-yl]-3-oxopropanenitrile
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C24H25N5O5
 1
1 IC50 = 12 nM
CP0636232
DELGOCITINIB
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C16H18N6O
 1
1 IC50 = 13 nM
CP0014854
3-cyano-N-[(1R,3S)-3-(cyanoamino)-5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]benzenesulfonamide
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C23H17N7O2S
 1
1 IC50 = 14 nM
CP0001779
N-[(1R,3S)-3-(cyanoamino)-5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-4-methoxybenzenesulfonamide
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C23H20N6O3S
 1
1 IC50 = 16 nM
CP0952685
4-((trans-1-(3-Chlorobenzyl)-2-methylpiperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
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C22H26ClN5O
 1
1 IC50 = 19.6 nM
CP0271843
(S)-5-chloro-2-(1-(5-fluoropyridin-2-yl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile
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C17H15ClFN7
 1
1 IC50 = 21 nM
CP0807413
4-((8-(4-Chlorobenzyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
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C23H26ClN5O
 1
1 IC50 = 47.5 nM
CP0952760
4-((1-(3-Chlorobenzyl)azepan-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
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C22H26ClN5O
 1
1 IC50 = 62.5 nM
CP0280668
(R)-3-(6-(1-(4-chlorophenyl)ethylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine
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C18H16ClN7
 1
1 IC50 = 81 nM
CP0291008
3-(6-(2-(4-fluorophenyl)pyrrolidin-1-yl)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine
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C20H18FN7
 1
1 IC50 = 86 nM
CP0326425
3-[2-[2-(3,5-difluoro-4-morpholin-4-ylanilino)-5-methylpyrimidin-4-yl]-6,7-dihydro-4H-furo[3,2-c]pyridin-5-yl]-3-oxopropanenitrile
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C25H24F2N6O3
 1
1 IC50 = 88.1 nM
CP0807416
4-((cis-3-Fluoro-1-(3-methoxybenzyl)piperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
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C22H26FN5O2
 1
1 IC50 = 88.7 nM
CP0104421
US10399979, Compound 17e
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C22H24N4O3
 1
1 IC50 = 124.1 nM
CP0242999
(S)-6-(5-cyclopropyl-1H-pyrazol-3-ylamino)-5-fluoro-2-(1-(4-fluorophenyl)ethylamino)nicotinonitrile
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C20H18F2N6
 1
1 IC50 = 183 nM
CP0306526
N-(3,5-difluoro-4-morpholin-4-ylphenyl)-5-methyl-4-(5-methylsulfonyl-6,7-dihydro-4H-furo[3,2-c]pyridin-2-yl)pyrimidin-2-amine
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C23H25F2N5O4S
 1
1 IC50 = 195.1 nM
CP0283874
(R)-3-(6-(2,3-dihydro-1H-inden-1-ylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine
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C19H17N7
 1
1 IC50 = 200 nM
CP0232448
N-[5-[4-(2-cyano-1-hydroxyprop-2-enyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide
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C20H17N5O2
 1
1 IC50 = 285 nM
CP0070994
(S)-3-(6-(1-phenylethylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine
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C18H17N7
 1
1 IC50 = 290 nM
CP0008628
US10112907, Example 00033
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C21H23N5O3S
 6
1 IC50 = 623 nM
2 IC50 = 810 nM
3 IC50 = 932 nM
4 IC50 = 3083 nM
5 IC50 > 10000 nM
6 Kd = 300 nM
CP0351745
Cyclopropanecarboxylic acid {5-[4-(3-cyano-azetidine-1- carbonyl)-phenyl]- [1,2,4]triazolo[1,5-a]pyridin-2- yl)-amide
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C21H18N6O2
 1
1 IC50 = 659 nM
CP0054852
1-(2-aminoethyl)-2-piperidin-4-ylbenzimidazole-5-carboxamide
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C15H21N5O
 1
1 IC50 = 1260 nM
CP0233890
ABT-494
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C17H19F3N6O
 1
1 IC50 = 2300 nM
CP0113747
2-methyl-N-[2-[3-(prop-2-enoylamino)anilino]pyrimidin-5-yl]-5-[[3-(trifluoromethyl)benzoyl]amino]benzamide
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C29H23F3N6O3
 1
1 IC50 = 2680 nM
CP0035025
4-anilinoquinazoline deriv. 2
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C17H13BrN4O
 1
1 IC50 = 3140 nM
CP0036058
N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide
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C24H25ClFN5O3
 2
1 IC50 = 3880 nM
2 Kd = 630 nM
CP0163785
3-((3S,4S)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile
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C16H20N6O
 1
1 Kd = 180 nM
CP0031719
(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
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C21H22Cl2FN5O
 1
1 Kd = 200 nM
CP0036082
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
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C22H24ClFN4O3
 1
1 Kd > 10000 nM
Clinical Information about the Protein
Target 1 ( Janus kinase 3 (JAK-3) )
Target Type Successful Target
Disease 9 Target-related Diseases  9
1 Rheumatoid arthritis [ICD-11: FA20]
2 Myelofibrosis [ICD-11: 2A20.2]
3 Atopic dermatitis [ICD-11: EA80]
4 Alopecia areata [ICD-11: ED70.2]
5 B-cell lymphoma [ICD-11: 2A86]
6 Asthma [ICD-11: CA23]
7 Multiple myeloma [ICD-11: 2A83]
8 Inflammation [ICD-11: 1A00-CA43.1]
9 Diffuse large B-cell lymphoma [ICD-11: 2A81]
Approved Drug(s) 4 Approved Drugs  4
1 Tofacitinib Approved
Rheumatoid arthritis
2 Pacritinib Approved
Myelofibrosis
3 Abrocitinib Approved
Atopic dermatitis
4 Ritlecitinib Approved
Alopecia areata
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 VX-509 Phase 2/3
Rheumatoid arthritis
2 ATI-502 Phase 2
Atopic dermatitis
3 Cerdulatinib Phase 2
B-cell lymphoma
4 GDC-0214 Phase 1
Asthma
Discontinued Drug(s) 1 Discontinued Drug  1
1 AG490 Terminated
Multiple myeloma
Investigative Drug(s) 2 Investigative Drugs  2
1 PF-956980 Investigative
Inflammation
2 WHI-P154 Investigative
Diffuse large B-cell lymphoma
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT05132 Tyrosine-protein kinase JAK3 Mus musculus, Mouse