General Information of the Protein
Protein ID
PT04205
Protein Name
Transcription factor Jun
Secondarily
Protein Name
Activator protein 1
Proto-oncogene c-Jun
Transcription factor AP-1 subunit Jun
V-jun avian sarcoma virus 17 oncogene homolog
p39
Gene Name
JUN
Sequence
MTAKMETTFYDDALNASFLPSESGPYGYSNPKILKQSMTLNLADPVGSLKPHLRAKNSDLLTSPDVGLLKLASPELERLIIQSSNGHITTTPTPTQFLCPKNVTDEQEGFAEGFVRALAELHSQNTLPSVTSAAQPVNGAGMVAPAVASVAGGSGSGGFSASLHSEPPVYANLSNFNPGALSSGGGAPSYGAAGLAFPAQPQQQQQPPHHLPQQMPVQHPRLQALKEEPQTVPEMPGETPPLSPIDMESQERIKAERKRMRNRIAASKCRKRKLERIARLEEKVKTLKAQNSELASTANMLREQVAQLKQKVMNHVNSGCQLMLTQQLQTF
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Organism
Homo sapiens, Human
Protein Classification
Transcription factor
Function
Transcription factor that recognizes and binds to the AP-1 consensus motif 5'-TGA[GC]TCA-3' (PubMed:10995748, PubMed:22083952). Heterodimerizes with proteins of the FOS family to form an AP-1 transcription complex, thereby enhancing its DNA binding activity to the AP-1 consensus sequence 5'-TGA[GC]TCA-3' and enhancing its transcriptional activity (By similarity). Together with FOSB, plays a role in activation-induced cell death of T cells by binding to the AP-1 promoter site of FASLG/CD95L, and inducing its transcription in response to activation of the TCR/CD3 signaling pathway (PubMed:12618758). Promotes activity of NR5A1 when phosphorylated by HIPK3 leading to increased steroidogenic gene expression upon cAMP signaling pathway stimulation (PubMed:17210646). Involved in activated KRAS-mediated transcriptional activation of USP28 in colorectal cancer (CRC) cells (PubMed:24623306). Binds to the USP28 promoter in colorectal cancer (CRC) cells (PubMed:24623306).
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Uniprot ID
Primary ID:
P05412

Secondarily ID:
Q6FHM7
Q96G93
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Ensembl ID
ENSG00000177606
HGNC ID
HGNC:6204
Subcellular Location
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: CL000068 , A-549
Compound ID Compound Name Compound Formula
CP0177092
4-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)-N-ethylpiperidine-1-carboxamide
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C20H23ClN6O
 1
1
IC50 = 704 nM
   TI
   LI
   LO
   TS
CP0344192
4-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)-N,N-dimethylpiperidine-1-carboxamide
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C20H23ClN6O
 1
1
IC50 = 741 nM
   TI
   LI
   LO
   TS
CP0288707
4-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)-N-(4-methylpiperidin-1-yl)piperidine-1-carboxamide
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C24H30ClN7O
 1
1
IC50 = 807 nM
   TI
   LI
   LO
   TS
CP0254044
(4-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)piperidin-1-yl)(4-methylpiperidin-1-yl)methanone
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C24H29ClN6O
 1
1
IC50 = 813 nM
   TI
   LI
   LO
   TS
CP0203188
2-(4-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)piperidin-1-yl)-N-methylacetamide
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C20H23ClN6O
 1
1
IC50 = 1769 nM
   TI
   LI
   LO
   TS
CP0210136
N-[2-[4-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]piperidin-1-yl]-2-oxoethyl]acetamide
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C21H23ClN6O2
 1
1
IC50 = 1938 nM
   TI
   LI
   LO
   TS
CP0157438
1-(4-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)piperidin-1-yl)-2-(methylamino)ethanone
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C20H23ClN6O
 1
1
IC50 = 2028 nM
   TI
   LI
   LO
   TS
CP0201741
1-(4-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)piperidin-1-yl)-2-(dimethylamino)ethanone
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C21H25ClN6O
 1
1
IC50 = 2497 nM
   TI
   LI
   LO
   TS
CP0293001
(4-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)piperidin-1-yl)(4-methylpiperazin-1-yl)methanone
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C23H28ClN7O
 1
1
IC50 = 2770 nM
   TI
   LI
   LO
   TS
CP0229050
2-((R)-3-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)piperidin-1-yl)-N-methylacetamide
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C20H23ClN6O
 1
1
IC50 = 2807 nM
   TI
   LI
   LO
   TS
CP0157416
4-(5-cyano-4-(6-fluoro-1H-indol-3-yl)pyrimidin-2-ylamino)-N-ethylpiperidine-1-carboxamide
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C21H22FN7O
 1
1
IC50 = 3700 nM
   TI
   LI
   LO
   TS
CP0194893
N-ethyl-4-[[4-(2-phenyl-1H-indol-3-yl)pyrimidin-2-yl]amino]piperidine-1-carboxamide
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C26H28N6O
 1
1
IC50 = 3845 nM
   TI
   LI
   LO
   TS
CP0192116
(3R)-3-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)-N-ethylpiperidine-1-carboxamide
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C20H23ClN6O
 1
1
IC50 = 3883 nM
   TI
   LI
   LO
   TS
CP0177069
3-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)-N-ethylazetidine-1-carboxamide
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C18H19ClN6O
 1
1
IC50 = 4272 nM
   TI
   LI
   LO
   TS
CP0177090
3-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)-N-ethylpyrrolidine-1-carboxamide
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C19H21ClN6O
 1
1
IC50 = 6268 nM
   TI
   LI
   LO
   TS
CP0203027
(3S)-3-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)-N-ethylpiperidine-1-carboxamide
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C20H23ClN6O
 1
1
IC50 = 6995 nM
   TI
   LI
   LO
   TS
CP0194894
4-(5-chloro-4-(H-imidazo[1,2-a]pyridin-3-yl)pyrimidin-2-ylamino)-N-ethylpiperidine-1-carboxamide
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C19H22ClN7O
 1
1
IC50 = 7723 nM
   TI
   LI
   LO
   TS
CP0293000
4-(4-(1H-indol-3-yl)pyrimidin-2-ylamino)-N-ethylpiperidine-1-carboxamide
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C20H24N6O
 1
1
IC50 = 8091 nM
   TI
   LI
   LO
   TS
CP0177091
4-(5-chloro-4-(1H-indol-1-yl)pyrimidin-2-ylamino)-N-ethylpiperidine-1-carboxamide
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C20H23ClN6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0221444
4-(4-(1H-indol-3-yl)-5-methylpyrimidin-2-ylamino)-N-ethylpiperidine-1-carboxamide
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C21H26N6O
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0203042
2-((S)-3-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)piperidin-1-yl)-N-methylacetamide
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C20H23ClN6O
 1
1
IC50 = 14667 nM
   TI
   LI
   LO
   TS
CP0194896
4-(4-(H-imidazo[1,2-a]pyridin-3-yl)pyrimidin-2-ylamino)-N-ethylpiperidine-1-carboxamide
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C19H23N7O
 1
1
IC50 = 19331 nM
   TI
   LI
   LO
   TS
CP0254416
N-ethyl-4-[[4-(2-propan-2-yl-1H-indol-3-yl)pyrimidin-2-yl]amino]piperidine-1-carboxamide
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C23H30N6O
 1
1
IC50 = 21160 nM
   TI
   LI
   LO
   TS
CP0203189
4-(4-(1H-indol-1-yl)pyrimidin-2-ylamino)-N-ethylpiperidine-1-carboxamide
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C20H24N6O
 1
1
IC50 = 29891 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0131137
(1S,2S,4S,5R,6S,7S,9R,13R,17S)-4,5-dihydroxy-15-methoxy-2,6,14,17-tetramethyl-10-oxatetracyclo[7.7.1.02,7.013,17]heptadec-14-ene-3,11,16-trione
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C21H28O7
 1
1 EC50 = 130 nM
CP0666523
Glaucarubinone
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C25H34O10
 1
1 EC50 = 1490 nM
CP0022497
3-[5-(4-cyclopentyloxy-2-hydroxybenzoyl)-2-[(3-oxo-1,2-benzoxazol-6-yl)methoxy]phenyl]propanoic acid
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C29H27NO8
 1
1 IC50 = 10000 nM
Clinical Information about the Protein
Target 1 ( Transcription factor AP-1 (JUN) )
Target Type Discontinued Target
Disease 1 Target-related Disease  1
1 Rheumatoid arthritis [ICD-11: FA20]
Discontinued Drug(s) 1 Discontinued Drug  1
1 T-5224 Discontinued in Phase 2
Rheumatoid arthritis
Target 2 ( c-Jun messenger RNA (c-Jun mRNA) )
Target Type Literature-reported Target