General Information of the Protein
Protein ID
PT01066
Protein Name
Tyrosine-protein kinase Yes
Secondarily
Protein Name
Proto-oncogene c-Yes
p61-Yes
Gene Name
YES1
Secondarily
Gene Name
YES
Sequence
MGCIKSKENKSPAIKYRPENTPEPVSTSVSHYGAEPTTVSPCPSSSAKGTAVNFSSLSMTPFGGSSGVTPFGGASSSFSVVPSSYPAGLTGGVTIFVALYDYEARTTEDLSFKKGERFQIINNTEGDWWEARSIATGKNGYIPSNYVAPADSIQAEEWYFGKMGRKDAERLLLNPGNQRGIFLVRESETTKGAYSLSIRDWDEIRGDNVKHYKIRKLDNGGYYITTRAQFDTLQKLVKHYTEHADGLCHKLTTVCPTVKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTKVAIKTLKPGTMMPEAFLQEAQIMKKLRHDKLVPLYAVVSEEPIYIVTEFMSKGSLLDFLKEGDGKYLKLPQLVDMAAQIADGMAYIERMNYIHRDLRAANILVGENLVCKIADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILQTELVTKGRVPYPGMVNREVLEQVERGYRMPCPQGCPESLHELMNLCWKKDPDERPTFEYIQSFLEDYFTATEPQYQPGENL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Src family
Function
Non-receptor protein tyrosine kinase that is involved in the regulation of cell growth and survival, apoptosis, cell-cell adhesion, cytoskeleton remodeling, and differentiation. Stimulation by receptor tyrosine kinases (RTKs) including EGFR, PDGFR, CSF1R and FGFR leads to recruitment of YES1 to the phosphorylated receptor, and activation and phosphorylation of downstream substrates. Upon EGFR activation, promotes the phosphorylation of PARD3 to favor epithelial tight junction assembly. Participates in the phosphorylation of specific junctional components such as CTNND1 by stimulating the FYN and FER tyrosine kinases at cell-cell contacts. Upon T-cell stimulation by CXCL12, phosphorylates collapsin response mediator protein 2/DPYSL2 and induces T-cell migration. Participates in CD95L/FASLG signaling pathway and mediates AKT-mediated cell migration. Plays a role in cell cycle progression by phosphorylating the cyclin-dependent kinase 4/CDK4 thus regulating the G1 phase. Also involved in G2/M progression and cytokinesis. Catalyzes phosphorylation of organic cation transporter OCT2 which induces its transport activity (PubMed:26979622).
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Uniprot ID
Primary ID:
P07947

Secondarily ID:
A6NLB3
D3DUH1
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Ensembl ID
ENSG00000176105
HGNC ID
HGNC:12841
Subcellular Location
Cell membrane
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Cytoplasm
Cytosol
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: CL000012 , Sf21
Compound ID Compound Name Compound Formula
CP0072678
5-(1,3-benzodioxol-5-yl)-7-[[(2R)-1-ethenylsulfonylpyrrolidin-2-yl]methyl]pyrrolo[2,3-d]pyrimidin-4-amine
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C20H21N5O4S
 1
1
IC50 = 57.3 nM
   TI
   LI
   LO
   TS
CP0717983
2-(4-Methoxyphenyl)-N-(4-piperidin-1-ylphenyl)pyrido[3,4-b]pyrazin-5-amine
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C25H25N5O
 1
1
IC50 = 1020 nM
   TI
   LI
   LO
   TS
CP0841521
N-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl)pyrido[3,4-b]pyrazin-8-amine
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C22H20N4O3
 1
1
IC50 = 2010 nM
   TI
   LI
   LO
   TS
CP0747495
2-(4-methoxyphenyl)-N-(4-morpholinophenyl)pyrido[3,4-b]pyrazin-8-amine
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C24H23N5O2
 1
1
IC50 = 2410 nM
   TI
   LI
   LO
   TS
CP0747494
N-(4-morpholinophenyl)-2-phenylpyrido[3,4-b]pyrazin-8-amine
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C23H21N5O
 1
1
IC50 = 5110 nM
   TI
   LI
   LO
   TS
CP0670159
2-(4-methoxyphenyl)-N-(4-(piperidin-1-yl)phenyl)pyrido[3,4-b]pyrazin-8-amine
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C25H25N5O
 1
1
IC50 = 5340 nM
   TI
   LI
   LO
   TS
CP0726868
2-phenyl-N-(4-(piperidin-1-yl)phenyl)pyrido[3,4-b]pyrazin-8-amine
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C24H23N5
 1
1
IC50 = 5560 nM
   TI
   LI
   LO
   TS
CP0761937
3-Phenyl-N-(4-piperidin-1-ylphenyl)pyrido[3,4-b]pyrazin-8-amine
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C24H23N5
 1
1
IC50 = 6210 nM
   TI
   LI
   LO
   TS
CP0726601
2-(4-Methoxyphenyl)-N-(4-morpholin-4-ylphenyl)pyrido[3,4-b]pyrazin-5-amine
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C24H23N5O2
 1
1
IC50 = 7070 nM
   TI
   LI
   LO
   TS
CP0717984
2-Phenyl-N-(4-piperidin-1-ylphenyl)pyrido[3,4-b]pyrazin-5-amine
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C24H23N5
 1
1
IC50 = 8100 nM
   TI
   LI
   LO
   TS
CP0674969
N-phenyl-2-(4-(piperidin-1-yl)phenyl)pyrido[3,4-b]pyrazin-8-amine
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C24H23N5
 1
1
IC50 = 8820 nM
   TI
   LI
   LO
   TS
CP0670157
N-(3-methoxyphenyl)-2-(4-(piperidin-1-yl)phenyl)pyrido[3,4-b]pyrazin-8-amine
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C25H25N5O
 1
1
IC50 = 11100 nM
   TI
   LI
   LO
   TS
CP0726600
N-(4-Morpholin-4-ylphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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C23H21N5O
 1
1
IC50 = 12630 nM
   TI
   LI
   LO
   TS
CP0680579
N-(2-Methoxyphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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C20H16N4O
 1
1
IC50 = 20430 nM
   TI
   LI
   LO
   TS
CP0674998
N-(4-Methoxyphenyl)-N'-(3-phenylpyrido[3,4-b]pyrazin-8-yl)urea
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C21H17N5O2
 1
1
IC50 = 22060 nM
   TI
   LI
   LO
   TS
CP0663577
2-Phenyl-N-(4-piperidin-1-ylphenyl)pyrido[3,4-b]pyrazin-7-amine
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C24H23N5
 1
1
IC50 = 23110 nM
   TI
   LI
   LO
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CP0691196
3-Phenyl-N-(4-piperidin-1-ylphenyl)pyrido[3,4-b]pyrazin-7-amine
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C24H23N5
 1
1
IC50 = 27210 nM
   TI
   LI
   LO
   TS
CP0674971
N-(4-Methoxyphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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C20H16N4O
 1
1
IC50 = 31510 nM
   TI
   LI
   LO
   TS
CP0717884
N-Phenyl-3-(4-piperidin-1-ylphenyl)pyrido[3,4-b]pyrazin-8-amine
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C24H23N5
 1
1
IC50 > 31600 nM
   TI
   LI
   LO
   TS
CP0717985
N-(3-Methoxyphenyl)-3-(4-piperidin-1-ylphenyl)pyrido[3,4-b]pyrazin-8-amine
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C25H25N5O
 1
1
IC50 > 31600 nM
   TI
   LI
   LO
   TS
CP0726598
N-(3-Methoxyphenyl)-N'-(3-phenylpyrido[3,4-b]pyrazin-8-yl)urea
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C21H17N5O2
 1
1
IC50 > 31600 nM
   TI
   LI
   LO
   TS
CP0726599
N-(3-Chloro-4-fluorophenyl)-3-phenylpyrido[3,4-b]pyrazin-8-amine
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C19H12ClFN4
 1
1
IC50 > 31600 nM
   TI
   LI
   LO
   TS
CP0726602
N-(3-Methoxyphenyl)-2-phenylpyrido[3,4-b]pyrazin-7-amine
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C20H16N4O
 1
1
IC50 > 31600 nM
   TI
   LI
   LO
   TS
CP0761933
N-(3-Methoxyphenyl)-N'-(2-phenylpyrido[3,4-b]pyrazin-5-yl)urea
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C21H17N5O2
 1
1
IC50 > 31600 nM
   TI
   LI
   LO
   TS
CP0660964
N-(3-Methoxyphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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C20H16N4O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0691194
N-Allyl-N'-(3-phenylpyrido[3,4-b]pyrazin-8-yl)urea
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C17H15N5O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0691195
N-(3-Ethynylphenyl)-2-phenylpyrido[3,4-b]pyrazin-5-amine
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C21H14N4
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0726603
N-(4-Morpholin-4-ylphenyl)-2-phenylpyrido[3,4-b]pyrazin-7-amine
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C23H21N5O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0731455
N-Ethyl-N'-(2-phenylpyrido[3,4-b]pyrazin-5-yl)urea
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C16H15N5O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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Clinical Information about the Protein
Target 1 ( Yes tyrosine kinase (YES) )
Target Type Clinical trial Target
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00879 Proto-oncogene tyrosine-protein kinase Src Homo sapiens, Human
PT01342 Tyrosine-protein kinase Fgr Homo sapiens, Human
PT02255 Proto-oncogene tyrosine-protein kinase Src Mus musculus, Mouse
PT06144 Proto-oncogene tyrosine-protein kinase Src Rattus norvegicus, Rat