General Information of the Protein
Protein ID
PT01486
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
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREAIQNPGPRHPEAASIAPPGACLQQRQETSPRRRRRQQHPEDGSPQAHIRGTTGYLALEEEQQPSQQQSASEGHPESGCLPEPGAATAPGKGLPQQPPAPPDQDDSAAPSTLSLLGPTFPGLSSCSADIKDILSEAGTMQLLQQQQQQQQQQQQQQQQQQQQQQEVISEGSSSVRAREATGAPSSSKDSYLGGNSTISDSAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYASLLGGPPAVRPTPCAPLAECKGLSLDEGPGKGTEETAEYSSFKGGYAKGLEGESLGCSGSSEAGSSGTLEIPSSLSLYKSGAVDEAAAYQNRDYYNFPLALSGPPHPPPPTHPHARIKLENPSDYGSAWAAAAAQCRYGDLASLHGGSVAGPSTGSPPATASSSWHTLFTAEEGQLYGPGGGGGSSSPSDAGPVAPYGYTRPPQGLASQEGDFSASEVWYPGGVVNRVPYPSPSCVKSEMGPWMENYSGPYGDMRLDSTRDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRNDCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGENSSAGSPTEDPSQKMTVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAKALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRMYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDRIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIISVQVPKILSGKVKPIYFHTQ
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Organism
Rattus norvegicus, Rat
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 (By similarity).
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Uniprot ID
Primary ID:
P15207

Secondarily ID:
Q63049
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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
CP0434850
BMS-665139
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C15H13ClF3N3O2
 1
1
EC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0443499
oxazolidin-2-imine, 6e
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C15H13ClF3N3O2
 1
1
EC50 = 1.1 nM
   TI
   LI
   LO
   TS
CP0498559
oxazolidin-2-imine, 6f
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C15H13ClF3N3O2
 1
1
EC50 = 1.4 nM
   TI
   LI
   LO
   TS
CP0036395
4-[(1S,7S,7aR)-1-ethyl-7-hydroxy-3-oxo-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile
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C16H18ClN3O2
 1
1
EC50 = 1.8 nM
   TI
   LI
   LO
   TS
CP0044960
(1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-5-one
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C19H30O2
 1
1
EC50 = 2.8 nM
   TI
   LI
   LO
   TS
CP0877320
Z-4-[(1R,7R,7aS)-7-hydroxy-1-isopropyltetrahydropyrrolo[1,2-c]oxazol-3-ylideneamino]-2-chloro-3-methylbenzonitrile
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C17H20ClN3O2
 1
1
EC50 = 3.7 nM
   TI
   LI
   LO
   TS
CP0847834
tetrahydro-7-hydroxy-2-(4-nitro-1-naphthalenyl)-1H-pyrrolo[1,2-c]imidazole-1,3(2H)-dione
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C16H13N3O5
 1
1
EC50 = 4.4 nM
   TI
   LI
   LO
   TS
CP0498560
oxazolidin-2-imine, 6a
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C14H14ClN3O2
 1
1
EC50 = 4.8 nM
   TI
   LI
   LO
   TS
CP0474737
4-[(1S,7S,7aR)-7-hydroxy-1-methyl-3-oxo-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile
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C15H16ClN3O2
 1
1
EC50 = 5.4 nM
   TI
   LI
   LO
   TS
CP0878549
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 = 6.3 nM
   TI
   LI
   LO
   TS
CP0474544
4-[(7R,7aR)-7-hydroxy-3-oxo-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile
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C14H14ClN3O2
 1
1
EC50 = 6.4 nM
   TI
   LI
   LO
   TS
CP0255862
BMS-564929
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C14H12ClN3O3
 1
1
EC50 = 7.8 nM
   TI
   LI
   LO
   TS
CP0434910
oxazolidin-2-imine, 6b
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C14H14ClN3O2
 1
1
EC50 = 14 nM
   TI
   LI
   LO
   TS
CP0381822
oxazolidin-2-imine, 6d
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C15H13ClF3N3O2
 1
1
EC50 = 19 nM
   TI
   LI
   LO
   TS
CP0443500
guanidine derivative, 12
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C15H17ClN4O
 1
1
EC50 = 44 nM
   TI
   LI
   LO
   TS
CP0918726
(6S)-tetrahydro-6-hydroxy-2-(4-nitro-1-naphthalenyl)-1H-pyrrolo[1,2-c]imidazole-1,3(2H)-dione
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C16H13N3O5
 1
1
EC50 = 265 nM
   TI
   LI
   LO
   TS
CP0873296
tetrahydro-2-(4-nitro-1-naphthalenyl)-1H-pyrrolo[1,2-c]imidazole-1,3(2H)-dione
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C16H13N3O4
 1
1
EC50 = 270 nM
   TI
   LI
   LO
   TS
CP0849428
(6R)-tetrahydro-6-hydroxy-2-(4-nitro-1-naphthalenyl)-1H-pyrrolo[1,2-c]imidazole-1,3(2H)-dione
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C16H13N3O5
 1
1
EC50 = 320 nM
   TI
   LI
   LO
   TS
CP0847835
(1S,6R,7R)-4-(4-nitro-1-naphthyl)-2,4-diazatricyclo[5.2.1.0~2,6~]decane-3,5-dione
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C18H15N3O4
 1
1
EC50 = 385 nM
   TI
   LI
   LO
   TS
CP0877321
(1S,7S,7aR)-2-(3-chloro-4-cyano-2-methylphenyl)-7-hydroxy-1-methyl-hexahydropyrrolo[1,2-c]imidazol-3-ylidenecyanamide
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C16H18ClN5O
 1
1
EC50 = 1109 nM
   TI
   LI
   LO
   TS
CP0474545
guanidine derivative, 11
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C14H15ClN4O
 1
1
EC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0847884
(5alpha,8alpha,8aalpha)-4-(octahydro-1,3-dioxo-5,8-methanoimidazo[1,5-a]pyridine-2yl)-1-naphthalenecarbonitrile
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C19H15N3O2
 2
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
2
IC50 = 260 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
IC50 = 60 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0044960
(1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-5-one
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C19H30O2
 8
1 IC50 = 1 nM
2 IC50 = 2 nM
3 IC50 = 3.1 nM
4 IC50 = 18.5 nM
5 IC50 = 3200 nM
6 Ki = 0.27 nM
7 Ki = 0.2818 nM
8 Ki = 0.69 nM
CP0146696
Bicalutamide
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C18H14F4N2O4S
 5
1 IC50 = 25 nM
2 IC50 = 54 nM
3 IC50 = 1300 nM
4 Ki = 14 nM
5 Ki = 509 nM
CP0095953
ENZALUTAMIDE
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C21H16F4N4O2S
 2
1 IC50 = 294 nM
2 Ki = 3641 nM
CP0037412
(2R)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorobenzene)sulfonyl]-2-hydroxy-2-methylpropanamide
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C18H14F4N2O4S
 2
1 Ki = 10.96 nM
2 Ki = 11 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01577 Androgen receptor Mus musculus, Mouse
50% Identity
Protein ID Protein Name Protein Organism
PT00894 Androgen receptor Homo sapiens, Human