General Information of the Protein
Protein ID
PT02212
Protein Name
Signal transducer and activator of transcription 1-alpha/beta
Secondarily
Protein Name
Transcription factor ISGF-3 components p91/p84
Gene Name
STAT1
Sequence
MSQWYELQQLDSKFLEQVHQLYDDSFPMEIRQYLAQWLEKQDWEHAANDVSFATIRFHDLLSQLDDQYSRFSLENNFLLQHNIRKSKRNLQDNFQEDPIQMSMIIYSCLKEERKILENAQRFNQAQSGNIQSTVMLDKQKELDSKVRNVKDKVMCIEHEIKSLEDLQDEYDFKCKTLQNREHETNGVAKSDQKQEQLLLKKMYLMLDNKRKEVVHKIIELLNVTELTQNALINDELVEWKRRQQSACIGGPPNACLDQLQNWFTIVAESLQQVRQQLKKLEELEQKYTYEHDPITKNKQVLWDRTFSLFQQLIQSSFVVERQPCMPTHPQRPLVLKTGVQFTVKLRLLVKLQELNYNLKVKVLFDKDVNERNTVKGFRKFNILGTHTKVMNMEESTNGSLAAEFRHLQLKEQKNAGTRTNEGPLIVTEELHSLSFETQLCQPGLVIDLETTSLPVVVISNVSQLPSGWASILWYNMLVAEPRNLSFFLTPPCARWAQLSEVLSWQFSSVTKRGLNVDQLNMLGEKLLGPNASPDGLIPWTRFCKENINDKNFPFWLWIESILELIKKHLLPLWNDGCIMGFISKERERALLKDQQPGTFLLRFSESSREGAITFTWVERSQNGGEPDFHAVEPYTKKELSAVTFPDIIRNYKVMAAENIPENPLKYLYPNIDKDHAFGKYYSRPKEAPEPMELDGPKGTGYIKTELISVSEVHPSRLQTTDNLLPMSPEEFDEVSRIVGSVEFDSMMNTV
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Organism
Homo sapiens, Human
Protein Classification
Transcription factor
Function
Signal transducer and transcription activator that mediates cellular responses to interferons (IFNs), cytokine KITLG/SCF and other cytokines and other growth factors (PubMed:9724754, PubMed:12855578, PubMed:12764129, PubMed:15322115, PubMed:34508746, PubMed:35568036, PubMed:23940278). Following type I IFN (IFN-alpha and IFN-beta) binding to cell surface receptors, signaling via protein kinases leads to activation of Jak kinases (TYK2 and JAK1) and to tyrosine phosphorylation of STAT1 and STAT2. The phosphorylated STATs dimerize and associate with ISGF3G/IRF-9 to form a complex termed ISGF3 transcription factor, that enters the nucleus (PubMed:28753426, PubMed:35568036). ISGF3 binds to the IFN stimulated response element (ISRE) to activate the transcription of IFN-stimulated genes (ISG), which drive the cell in an antiviral state (PubMed:28753426, PubMed:35568036). In response to type II IFN (IFN-gamma), STAT1 is tyrosine- and serine-phosphorylated (PubMed:26479788). It then forms a homodimer termed IFN-gamma-activated factor (GAF), migrates into the nucleus and binds to the IFN gamma activated sequence (GAS) to drive the expression of the target genes, inducing a cellular antiviral state (PubMed:8156998). Becomes activated in response to KITLG/SCF and KIT signaling (PubMed:15526160). May mediate cellular responses to activated FGFR1, FGFR2, FGFR3 and FGFR4 (PubMed:19088846). Involved in food tolerance in small intestine: associates with the Gasdermin-D, p13 cleavage product (13 kDa GSDMD) and promotes transcription of CIITA, inducing type 1 regulatory T (Tr1) cells in upper small intestine (By similarity).
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Uniprot ID
Primary ID:
P42224

Secondarily ID:
A8K989
B2RCA0
D2KFR8
D3DPI7
Q53S88
Q53XW4
Q68D00
Q9UDL5
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Ensembl ID
ENSG00000115415
HGNC ID
HGNC:11362
Subcellular Location
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: CL000403 , CAL-33
Compound ID Compound Name Compound Formula
CP0163405
US9211296, Table 7, Compd: 9
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C18H23N5
 1
1
IC50 = 5900 nM
   TI
   LI
   LO
   TS
CP0413418
4-methyl-2-[(4,6,8-trimethylquinazolin-2-yl)amino]-1H-pyrimidin-6-one
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C16H17N5O
 1
1
IC50 = 12100 nM
   TI
   LI
   LO
   TS
CP0379139
4-methyl-N-phenylquinazolin-2-amine
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C15H13N3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0379140
N-[2-(1H-indol-3-yl)ethyl]-4-methylquinazolin-2-amine
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C19H18N4
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0379142
4-methyl-N-(2-morpholin-4-ylethyl)quinazolin-2-amine
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C15H20N4O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0379143
N-cyclohexyl-4-methylquinazolin-2-amine
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C15H19N3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0379467
N-benzyl-4-methylquinazolin-2-amine
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C16H15N3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0413417
4-methyl-N-(naphthalen-1-ylmethyl)quinazolin-2-amine
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C20H17N3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0413420
4-methyl-N-[(5-methylfuran-2-yl)methyl]quinazolin-2-amine
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C15H15N3O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0413421
4-methyl-N-pyridin-2-ylquinazolin-2-amine
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C14H12N4
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0553419
N-(1,3-benzodioxol-5-ylmethyl)-4-methylquinazolin-2-amine
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C17H15N3O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0379145
2-[(4,7-dimethylquinazolin-2-yl)amino]-4,5-dimethyl-1H-pyrimidin-6-one
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C16H17N5O
 1
1
IC50 = 35200 nM
   TI
   LI
   LO
   TS
CP0520594
2-[(4,7-dimethylquinazolin-2-yl)amino]-4-methyl-1H-pyrimidin-6-one
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C15H15N5O
 1
1
IC50 = 39700 nM
   TI
   LI
   LO
   TS
CP0147464
4,5-dimethyl-2-[(4,6,8-trimethylquinazolin-2-yl)amino]-1H-pyrimidin-6-one
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C17H19N5O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0152343
6-ethoxy-4-methyl-N-(4,4,6-trimethyl-1H-pyrimidin-2-yl)quinazolin-2-amine
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C18H23N5O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0232354
7-ethoxy-4-methyl-N-(4,4,6-trimethyl-1H-pyrimidin-2-yl)quinazolin-2-amine
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C18H23N5O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0379141
2-[(8-methyl-[1,3]dioxolo[4,5-g]quinazolin-6-yl)amino]-4-phenyl-1H-pyrimidin-6-one
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C20H15N5O3
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0379144
5-benzyl-2-[(6-methoxy-4-methylquinazolin-2-yl)amino]-4-methyl-1H-pyrimidin-6-one
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C22H21N5O2
 1
1
IC50 = 50000 nM
   TI
   LI
   LO
   TS
CP0379146
4,5-dimethyl-2-[(4,6,7-trimethylquinazolin-2-yl)amino]-1H-pyrimidin-6-one
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C17H19N5O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0379468
CS115
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C15H15N5O2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0380897
2-[(6-ethoxy-4-methylquinazolin-2-yl)amino]-4-methyl-1H-pyrimidin-6-one
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C16H17N5O2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0380898
2-[(6-methoxy-4-methylquinazolin-2-yl)amino]-4-methyl-1H-pyrimidin-6-one
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C15H15N5O2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0406147
2-[(6-ethoxy-4-methylquinazolin-2-yl)amino]-4-phenyl-1H-pyrimidin-6-one
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C21H19N5O2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0406148
4-methyl-2-[(4,6,7-trimethylquinazolin-2-yl)amino]-1H-pyrimidin-6-one
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C16H17N5O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0406149
4-methyl-2-[(8-methyl-[1,3]dioxolo[4,5-g]quinazolin-6-yl)amino]-1H-pyrimidin-6-one
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C15H13N5O3
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0413419
5-benzyl-4-methyl-2-[(8-methyl-[1,3]dioxolo[4,5-g]quinazolin-6-yl)amino]-1H-pyrimidin-6-one
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C22H19N5O3
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0515356
1,4-dioxane;6-phenyl-2-[(4,6,8-trimethyl-2-quinazolinyl)amino]-1H-pyrimidin-4-one
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C21H19N5O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0537674
4,6-dimethyl-N-(4,4,6-trimethyl-1H-pyrimidin-2-yl)quinazolin-2-amine
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C17H21N5
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0537688
2-[(6-ethoxy-4-methylquinazolin-2-yl)amino]-4,5-dimethyl-1H-pyrimidin-6-one
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C17H19N5O2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0551483
4-methyl-5-prop-2-enyl-2-[(4,6,8-trimethylquinazolin-2-yl)amino]-1H-pyrimidin-6-one
   Show/Hide
C19H21N5O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0551484
5-benzyl-2-[(6-ethoxy-4-methylquinazolin-2-yl)amino]-4-methyl-1H-pyrimidin-6-one
   Show/Hide
C23H23N5O2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0553659
4,5-dimethyl-2-[(8-methyl-[1,3]dioxolo[4,5-g]quinazolin-6-yl)amino]-1H-pyrimidin-6-one
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C16H15N5O3
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Signal transducer and activator of transcription 1 (STAT1) )
Target Type Patented-recorded Target