General Information of the Protein
Protein ID
PT01577
Protein Name
Androgen receptor
Secondarily
Protein Name
Dihydrotestosterone receptor
Nuclear receptor subfamily 3 group C member 4
Gene Name
AR
Secondarily
Gene Name
Nr3c4
Sequence
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREAIQNPGPRHPEAANIAPPGACLQQRQETSPRRRRRQQHTEDGSPQAHIRGPTGYLALEEEQQPSQQQAASEGHPESSCLPEPGAATAPGKGLPQQPPAPPDQDDSAAPSTLSLLGPTFPGLSSCSADIKDILNEAGTMQLLQQQQQQQQHQQQHQQHQQQQEVISEGSSARAREATGAPSSSKDSYLGGNSTISDSAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYASLLGGPPAVRPTPCAPLPECKGLPLDEGPGKSTEETAEYSSFKGGYAKGLEGESLGCSGSSEAGSSGTLEIPSSLSLYKSGALDEAAAYQNRDYYNFPLALSGPPHPPPPTHPHARIKLENPLDYGSAWAAAAAQCRYGDLGSLHGGSVAGPSTGSPPATTSSSWHTLFTAEEGQLYGPGGGGGSSSPSDAGPVAPYGYTRPPQGLTSQESDYSASEVWYPGGVVNRVPYPSPNCVKSEMGPWMENYSGPYGDMRLDSTRDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRNDCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGENSNAGSPTEDPSQKMTVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAKALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRMYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDRIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIISVQVPKILSGKVKPIYFHTQ
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Organism
Mus musculus, Mouse
Protein Classification
Transcription factor
>
Nuclear receptor
>
Nuclear hormone receptor subfamily 3
>
Nuclear hormone receptor subfamily 3 group C
>
Nuclear hormone receptor subfamily 3 group C member 4
Function
Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins like ZBTB7A that recruits NCOR1 and NCOR2 to the androgen response elements/ARE on target genes, negatively regulating androgen receptor signaling and androgen-induced cell proliferation. Transcription activation is also down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3.
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Uniprot ID
P19091
Ensembl ID
ENSG00000169083
Subcellular Location
Nucleus
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: CL000361 , C2C12
Compound ID Compound Name Compound Formula
CP0255862
BMS-564929
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C14H12ClN3O3
 1
1
EC50 = 0.44 nM
   TI
   LI
   LO
   TS
CP0645750
(7R,7aS)-4-(tetrahydro-7-hydroxy-1,3-dioxo-1H-pyrrolo[1,2-c]imidazol-2(3H)-yl)-1-naphthalenecarbonitrile
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C17H13N3O3
 1
1
EC50 = 2.3 nM
   TI
   LI
   LO
   TS
CP0087810
[(8R,9S,10R,13S,14S,17S)-10,13-dimethyl-3-oxo-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl] propanoate
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C22H32O3
 1
1
EC50 = 2.8 nM
   TI
   LI
   LO
   TS
CP0505476
(2S,3R)-1-(3-chloro-4-cyano-2-methyl-phenylsulfamoyl)-3-hydroxy-pyrrolidine-2-carboxylic acid
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C13H14ClN3O5S
 1
1
EC50 = 2.8 nM
   TI
   LI
   LO
   TS
CP0462960
2-Chloro-4-((3aS,4R)-4-hydroxy-1,1,3-trioxo-tetrahydro-1lambda*6*-thia-2,6a-diaza-pentalen-2-yl)-3-methyl-benzonitrile
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C13H12ClN3O4S
 1
1
EC50 = 11.9 nM
   TI
   LI
   LO
   TS
CP0501696
2-chloro-4-((3aS,4R)-4-hydroxy-3a-methyl-1,1,3-trioxo-tetrahydro-1lambda6-thia-2,6a-diaza-pentalen-2-yl)-3-methyl-benzonitrile
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C14H14ClN3O4S
 1
1
EC50 = 1251 nM
   TI
   LI
   LO
   TS
CP0505479
2-chloro-4-((3aS,4S)-4-hydroxy-1,1,3-trioxo-tetrahydro-1lambda6-thia-2,6a-diaza-pentalen-2-yl)-3-methyl-benzonitrile
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C13H12ClN3O4S
 1
1
EC50 = 2959 nM
   TI
   LI
   LO
   TS
CP0434434
2-chloro-4-((3aS,5S)-5-hydroxy-1,1,3-trioxo-tetrahydro-1lambda6-thia-2,6a-diaza-pentalen-2-yl)-3-methyl-benzonitrile
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C13H12ClN3O4S
 1
1
EC50 = 3517 nM
   TI
   LI
   LO
   TS
CP0490931
(2S,3R)-1-(3-chloro-4-cyano-2-methyl-phenylsulfamoyl)-3-hydroxy-pyrrolidine-2-carboxylic acid methyl ester
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C14H16ClN3O5S
 1
1
EC50 = 7459 nM
   TI
   LI
   LO
   TS
CP0536440
2-chloro-4-((3aR,4R)-4-hydroxy-1,1-dioxo-tetrahydro-1lambda6-thia-2,6a-diaza-pentalen-2-yl)-3-methyl-benzonitrile
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C13H14ClN3O3S
 1
1
EC50 = 7729 nM
   TI
   LI
   LO
   TS
CP0530871
2-chloro-4-((3aR,4S)-4-hydroxy-3-methyl-1,1-dioxo-tetrahydro-1lambda6-thia-2,6a-diaza-pentalen-2-yl)-3-methyl-benzonitrile
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C14H16ClN3O3S
 1
1
EC50 = 8962 nM
   TI
   LI
   LO
   TS
CP0539652
(2S,3R)-methyl 1-(3-chloro-4-cyano-2-methylphenylsulfonyl)-3-hydroxypyrrolidine-2-carboxylate
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C14H15ClN2O5S
 2
1
EC50 > 3000 nM
   TI
   LI
   LO
   TS
2
IC50 = 278 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0041416
(6alpha)-17-(Acetyloxy)-6-methylpreg-4-ene-3,20-dione
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C24H34O4
 1
1 EC50 = 6.1 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01486 Androgen receptor Rattus norvegicus, Rat
50% Identity
Protein ID Protein Name Protein Organism
PT00894 Androgen receptor Homo sapiens, Human