General Information of the Protein
Protein ID
PT06037
Protein Name
Aryl hydrocarbon receptor
Gene Name
AHR
Sequence
MSSGANITYASRKRRKPVQKTVKPIPAEGIKSNPSKRHRDRLNTELDRLASLLPFPQDVINKLDKLSVLRLSVSYLRAKSFFDVALKSTPADRNGGQDQCRAQIRDWQDLQEGEFLLQALNGFVLVVTADALVFYASSTIQDYLGFQQSDVIHQSVYELIHTEDRAEFQRQLHWALNPDSAQGVDEAHGPPQAAVYYTPDQLPPENASFMERCFRCRLRCLLDNSSGFLAMNFQGRLKYLHGQNKKGKDGALLPPQLALFAIATPLQPPSILEIRTKNFIFRTKHKLDFTPIGCDAKGQLILGYTEVELCTRGSGYQFIHAADMLHCAESHIRMIKTGESGMTVFRLFAKHSRWRWVQSNARLIYRNGRPDYIIATQRPLTDEEGREHLQKRSTSLPFMFATGEAVLYEISSPFSPIMDPLPIRTKSNTSRKDWAPQSTPSKDSFHPSSLMSALIQQDESIYLCPPSSPAPLDSHFLMGSVSKCGSWQDSFAAAGSEAALKHEQIGHAQDVNLALSGGPSELFPDNKNNDLYNIMRNLGIDFEDIRSMQNEEFFRTDSTAAGEVDFKDIDITDEILTYVQDSLNNSTLMNSACQQQPVTQHLSCMLQERLQLEQQQQLQQPPPQALEPQQQLCQMVCPQQDLGPKHTQINGTFASWNPTPPVSFNCPQQELKHYQLFSSLQGTAQEFPYKPEVDSVPYTQNFAPCNQPLLPEHSKSVQLDFPGRDFEPSLHPTTSNLDFVSCLQVPENQSHGINSQSTMVSPQAYYAGAMSMYQCQPGPQRTPVDQTQYSSEIPGSQAFLSKVQSRGIFNETYSSDLSSIGHAAQTTGHLHHLAEARPLPDITPGGFL
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Organism
Mus musculus, Mouse
Protein Classification
Transcription factor
Function
Ligand-activated transcription factor that enables cells to adapt to changing conditions by sensing compounds from the environment, diet, microbiome and cellular metabolism, and which plays important roles in development, immunity and cancer (PubMed:10639156, PubMed:10973493, PubMed:1314586, PubMed:7961644, PubMed:7969080, PubMed:8806883, PubMed:9427285, PubMed:33436590). Upon ligand binding, translocates into the nucleus, where it heterodimerizes with ARNT and induces transcription by binding to xenobiotic response elements (XRE) (By similarity). Regulates a variety of biological processes, including angiogenesis, hematopoiesis, drug and lipid metabolism, cell motility and immune modulation (PubMed:20106950, PubMed:28396409). Xenobiotics can act as ligands: upon xenobiotic-binding, activates the expression of multiple phase I and II xenobiotic chemical metabolizing enzyme genes (such as the CYP1A1 gene) (PubMed:10639156, PubMed:10973493, PubMed:1314586, PubMed:7961644, PubMed:7969080, PubMed:8806883, PubMed:9427285). Mediates biochemical and toxic effects of halogenated aromatic hydrocarbons (By similarity). Next to xenobiotics, natural ligands derived from plants, microbiota, and endogenous metabolism are potent AHR agonists (By similarity). Tryptophan (Trp) derivatives constitute an important class of endogenous AHR ligands (By similarity). Acts as a negative regulator of anti-tumor immunity: indoles and kynurenic acid generated by Trp catabolism act as ligand and activate AHR, thereby promoting AHR-driven cancer cell motility and suppressing adaptive immunity (By similarity). Regulates the circadian clock by inhibiting the basal and circadian expression of the core circadian component PER1 (By similarity). Inhibits PER1 by repressing the CLOCK-BMAL1 heterodimer mediated transcriptional activation of PER1 (PubMed:20106950). The heterodimer ARNT:AHR binds to core DNA sequence 5'-TGCGTG-3' within the dioxin response element (DRE) of target gene promoters and activates their transcription (PubMed:28396409).
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Uniprot ID
Primary ID:
P30561

Secondarily ID:
Q8QZX6
Q8R4S3
Q99P79
Q9QVY1
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Ensembl ID
ENSG00000106546
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: CL000827 , HC11
Compound ID Compound Name Compound Formula
CP0469141
5-(2,4-dichlorophenyl)-3-phenyl-1,2,4-oxadiazole
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C14H8Cl2N2O
 1
1
EC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0535863
5-chloro-2-(3-phenyl-1,2,4-oxadiazol-5-yl)aniline
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C14H10ClN3O
 1
1
EC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0382725
5-(4-fluoro-2-nitrophenyl)-3-phenyl-1,2,4-oxadiazole
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C14H8FN3O3
 1
1
EC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0463644
2-(3-phenyl-1,2,4-oxadiazol-5-yl)-5-(trifluoromethyl)aniline
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C15H10F3N3O
 1
1
EC50 = 3200 nM
   TI
   LI
   LO
   TS
CP0491010
3-phenyl-5-(2,3,4-trichlorophenyl)-1,2,4-oxadiazole
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C14H7Cl3N2O
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0569777
methyl 2-(1H-indole-3-carbonyl)-1,3-thiazole-4-carboxylate
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C14H10N2O3S
 1
1 Kd = 3 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02265 Aryl hydrocarbon receptor Homo sapiens, Human