General Information of the Protein
Protein ID
PT02265
Protein Name
Aryl hydrocarbon receptor
Secondarily
Protein Name
Class E basic helix-loop-helix protein 76
Gene Name
AHR
Secondarily
Gene Name
BHLHE76
Sequence
MNSSSANITYASRKRRKPVQKTVKPIPAEGIKSNPSKRHRDRLNTELDRLASLLPFPQDVINKLDKLSVLRLSVSYLRAKSFFDVALKSSPTERNGGQDNCRAANFREGLNLQEGEFLLQALNGFVLVVTTDALVFYASSTIQDYLGFQQSDVIHQSVYELIHTEDRAEFQRQLHWALNPSQCTESGQGIEEATGLPQTVVCYNPDQIPPENSPLMERCFICRLRCLLDNSSGFLAMNFQGKLKYLHGQKKKGKDGSILPPQLALFAIATPLQPPSILEIRTKNFIFRTKHKLDFTPIGCDAKGRIVLGYTEAELCTRGSGYQFIHAADMLYCAESHIRMIKTGESGMIVFRLLTKNNRWTWVQSNARLLYKNGRPDYIIVTQRPLTDEEGTEHLRKRNTKLPFMFTTGEAVLYEATNPFPAIMDPLPLRTKNGTSGKDSATTSTLSKDSLNPSSLLAAMMQQDESIYLYPASSTSSTAPFENNFFNESMNECRNWQDNTAPMGNDTILKHEQIDQPQDVNSFAGGHPGLFQDSKNSDLYSIMKNLGIDFEDIRHMQNEKFFRNDFSGEVDFRDIDLTDEILTYVQDSLSKSPFIPSDYQQQQSLALNSSCMVQEHLHLEQQQQHHQKQVVVEPQQQLCQKMKHMQVNGMFENWNSNQFVPFNCPQQDPQQYNVFTDLHGISQEFPYKSEMDSMPYTQNFISCNQPVLPQHSKCTELDYPMGSFEPSPYPTTSSLEDFVTCLQLPENQKHGLNPQSAIITPQTCYAGAVSMYQCQPEPQHTHVGQMQYNPVLPGQQAFLNKFQNGVLNETYPAELNNINNTQTTTHLQPLHHPSEARPFPDLTSSGFL
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Organism
Homo sapiens, Human
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:30373764, PubMed:23275542, PubMed:7961644, PubMed:32818467). Upon ligand binding, translocates into the nucleus, where it heterodimerizes with ARNT and induces transcription by binding to xenobiotic response elements (XRE) (PubMed:30373764, PubMed:23275542, PubMed:7961644). Regulates a variety of biological processes, including angiogenesis, hematopoiesis, drug and lipid metabolism, cell motility and immune modulation (PubMed:12213388). 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:7961644). Mediates biochemical and toxic effects of halogenated aromatic hydrocarbons (PubMed:7961644, PubMed:34521881). Next to xenobiotics, natural ligands derived from plants, microbiota, and endogenous metabolism are potent AHR agonists (PubMed:18076143). Tryptophan (Trp) derivatives constitute an important class of endogenous AHR ligands (PubMed:32866000, PubMed:32818467). 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 (PubMed:32818467). Regulates the circadian clock by inhibiting the basal and circadian expression of the core circadian component PER1 (PubMed:28602820). Inhibits PER1 by repressing the CLOCK-BMAL1 heterodimer mediated transcriptional activation of PER1 (PubMed:28602820). 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:28602820).
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Uniprot ID
Primary ID:
P35869

Secondarily ID:
A4D130
Q13728
Q13803
Q13804
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Ensembl ID
ENSG00000106546
HGNC ID
HGNC:348
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: CL000063 , Hep-G2
Compound ID Compound Name Compound Formula
CP0410654
2-[(1-methylindol-3-yl)methyl]-1H-indole-3-carbaldehyde
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C19H16N2O
 1
1
EC50 = 55 nM
   TI
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CP0542236
3-(1H-indol-2-ylmethyl)-1-methylindole
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C18H16N2
 1
1
EC50 = 86 nM
   TI
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CP0515417
2-[(5-chloro-1H-indol-3-yl)methyl]-1H-indole-3-carbaldehyde
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C18H13ClN2O
 1
1
EC50 = 93 nM
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   LI
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CP0379259
3-(1H-indol-2-ylmethyl)-5-methoxy-1H-indole
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C18H16N2O
 1
1
EC50 = 94 nM
   TI
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CP0515420
2-(1H-indol-3-ylmethyl)-1H-indole
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C17H14N2
 1
1
EC50 = 215 nM
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CP0410665
2-[(5-methoxy-1H-indol-3-yl)methyl]-1H-indole-3-carbaldehyde
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C19H16N2O2
 1
1
EC50 = 230 nM
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CP0379260
2-(1H-indol-3-ylmethyl)-1H-indole-3-carbaldehyde
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C18H14N2O
 1
1
EC50 = 270 nM
   TI
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CP0400161
2-[(7-chloro-1H-indol-3-yl)methyl]-1H-indole-3-carbaldehyde
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C18H13ClN2O
 1
1
EC50 = 320 nM
   TI
   LI
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   TS
CP0065937
US9138393, Methyl- cholanthrene
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C21H16
 1
1
EC50 = 490 nM
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CP0046495
2-(3-methoxyphenyl)-1H-quinazoline-4-thione
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C15H12N2OS
 1
1
EC50 = 630 nM
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CP0180452
2-(3-methoxyphenyl)-4-methylsulfanylquinazoline
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C16H14N2OS
 1
1
EC50 = 2300 nM
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CP0059925
4-methoxy-2-(3-methoxyphenyl)quinazoline
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C16H14N2O2
 1
1
EC50 = 7300 nM
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CP0135474
6-Formylindolo[3,2-B]Carbazole
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C19H12N2O
 1
1
EC50 = 9060 nM
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CP0421506
4-[pyridin-2-yl(thiophen-2-yl)methyl]phenol
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C16H13NOS
 1
1
EC50 = 13160 nM
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CP0554484
(4-methoxyphenyl)-pyridin-2-yl-quinolin-2-ylmethanol
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C22H18N2O2
 1
1
EC50 = 19880 nM
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CP0941325
3-((4-methoxyphenyl)(pyridin-2-yl)methyl)-1H-indole
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C21H18N2O
 1
1
EC50 = 21720 nM
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CP0928202
4-((1H-indol-3-yl)(pyridin-2-yl)methyl)phenyl acetate
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C22H18N2O2
 1
1
EC50 = 27860 nM
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CP0483674
1-[(4-hydroxyphenyl)-pyridin-2-ylmethyl]naphthalen-2-ol
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C22H17NO2
 1
1
EC50 > 50000 nM
   TI
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CP0528355
2-[(4-methoxyphenyl)-thiophen-2-ylmethyl]pyridine
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C17H15NOS
 1
1
EC50 > 50000 nM
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CP0516985
(4-methoxyphenyl)-pyridin-2-yl-[4-(trifluoromethyl)phenyl]methanol
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C20H16F3NO2
 1
1
EC50 = 52030 nM
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CP0490675
1-[(4-methoxyphenyl)-pyridin-2-ylmethyl]naphthalen-2-ol
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C23H19NO2
 1
1
EC50 = 53620 nM
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CP0424668
4-[(4-bromophenyl)-pyridin-2-ylmethyl]phenol
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C18H14BrNO
 1
1
EC50 > 100000 nM
   TI
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CP0424669
[4-[(4-fluorophenyl)-pyridin-2-ylmethyl]phenyl] acetate
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C20H16FNO2
 1
1
EC50 > 100000 nM
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CP0424782
[4-[(4-bromophenyl)-(1-oxidopyridin-1-ium-2-yl)methyl]phenyl] acetate
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C20H16BrNO3
 1
1
EC50 > 100000 nM
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CP0451012
[4-[benzotriazol-1-yl(pyridin-2-yl)methyl]phenyl] acetate
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C20H16N4O2
 1
1
EC50 > 100000 nM
   TI
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CP0477819
[4-[(4-methylphenyl)-pyridin-2-ylmethyl]phenyl] acetate
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C21H19NO2
 1
1
EC50 > 100000 nM
   TI
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CP0490645
2-[(4-methylphenyl)-pyridin-2-ylmethyl]phenol
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C19H17NO
 1
1
EC50 > 100000 nM
   TI
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CP0495569
4-[(4-chlorophenyl)-pyridin-2-ylmethyl]phenol
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C18H14ClNO
 1
1
EC50 > 100000 nM
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CP0528354
1-[(4-methoxyphenyl)-pyridin-2-ylmethyl]benzotriazole
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C19H16N4O
 1
1
EC50 > 100000 nM
   TI
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CP0554485
4-[(4-methylphenyl)-pyridin-2-ylmethyl]phenol
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C19H17NO
 1
1
EC50 > 100000 nM
   TI
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CP0515418
5-chloro-3-(1H-indol-2-ylmethyl)-1H-indole
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C17H13ClN2
 1
1
EC50 > 6700 nM
   TI
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CP0272403
CH-223191
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C19H19N5O
 1
1
IC50 = 2430 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0129110
3-Phenyl-1H-naphtho[2,1-b]pyran-1-one
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C19H12O2
 2
1 EC50 = 8.4 nM
2 EC50 = 1400 nM
CP0456268
3-(2',6'-Difluorophenyl)-1H-naphtho[2,1-b]pyran-1-one
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C19H10F2O2
 1
1 EC50 = 200 nM
Clinical Information about the Protein
Target 1 ( Aryl hydrocarbon receptor (AHR) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Thrombocytopenia [ICD-11: 3B64]
2 Plaque psoriasis [ICD-11: EA90.0]
Approved Drug(s) 2 Approved Drugs  2
1 Romiplostim Approved
Thrombocytopenia
2 Tapinarof Approved
Plaque psoriasis
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06037 Aryl hydrocarbon receptor Mus musculus, Mouse