AHR

Summary

AHR (aryl hydrocarbon receptor, HGNC:348) is a protein-coding gene on chromosome 7p21.1, encoding Aryl hydrocarbon receptor (P35869). 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.

The protein encoded by this gene is a ligand-activated helix-loop-helix transcription factor involved in the regulation of biological responses to planar aromatic hydrocarbons. This receptor has been shown to regulate xenobiotic-metabolizing enzymes such as cytochrome P450. Before ligand binding, the encoded protein is sequestered in the cytoplasm; upon ligand binding, this protein moves to the nucleus and stimulates transcription of target genes.

Source: NCBI Gene 196 — RefSeq curated summary.

At a glance

• Gene–disease (curated): retinitis pigmentosa 85 (Strong, GenCC) — +3 more curated relationships
• GWAS associations: 58
• Clinical variants (ClinVar): 547 total — 6 pathogenic, 2 likely-pathogenic
• Phenotypes (HPO): 49
• Druggable target: yes — 9 molecules with ChEMBL bioactivity
• Transcription factor: yes — 207 downstream targets (CollecTRI)
• MANE Select transcript: NM_001621

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:348
Approved symbol	AHR
Name	aryl hydrocarbon receptor
Location	7p21.1
Locus type	gene with protein product
Status	Approved
Aliases	bHLHe76
Ensembl gene	ENSG00000106546
Ensembl biotype	protein_coding
OMIM	600253
Entrez	196

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 4 protein_coding_CDS_not_defined, 3 protein_coding, 1 nonsense_mediated_decay

ENST00000242057, ENST00000463496, ENST00000475440, ENST00000481944, ENST00000492120, ENST00000642825, ENST00000645559, ENST00000964518

RefSeq mRNA: 1 — MANE Select: NM_001621 NM_001621

CCDS: CCDS5366

Canonical transcript exons

ENST00000242057 — 11 exons

Exon	Start	End
ENSE00000672355	17333912	17334114
ENSE00000672361	17327759	17327848
ENSE00000672363	17322501	17322607
ENSE00000831833	17329952	17330075
ENSE00000831836	17334887	17334996
ENSE00001086356	17338986	17340228
ENSE00001180187	17309936	17310123
ENSE00001855259	17298652	17299329
ENSE00003626083	17335645	17335786
ENSE00003647464	17330756	17330886
ENSE00003844503	17342921	17346147

Expression profiles

Bgee: expression breadth ubiquitous, 275 present calls, max score 97.96.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 26.9405 / max 647.4582, expressed in 1697 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
77347	14.0726	1569
77346	6.9954	1555
77348	4.3939	1133
77349	0.4582	214
77355	0.4557	245
77331	0.3470	121
77359	0.2177	81

Top tissues by expression

293 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
visceral pleura	UBERON:0002401	97.96	gold quality
parietal pleura	UBERON:0002400	96.93	gold quality
pleura	UBERON:0000977	96.88	gold quality
superficial temporal artery	UBERON:0001614	96.77	gold quality
mucosa of paranasal sinus	UBERON:0005030	96.35	gold quality
calcaneal tendon	UBERON:0003701	96.28	gold quality
lower lobe of lung	UBERON:0008949	96.25	gold quality
gall bladder	UBERON:0002110	95.55	gold quality
skin of hip	UBERON:0001554	95.45	gold quality
mammalian vulva	UBERON:0000997	95.30	gold quality
tibial nerve	UBERON:0001323	95.04	gold quality
mucosa of urinary bladder	UBERON:0001259	95.02	gold quality
upper leg skin	UBERON:0004262	94.80	gold quality
mammary duct	UBERON:0001765	94.55	gold quality
cauda epididymis	UBERON:0004360	94.35	gold quality
seminal vesicle	UBERON:0000998	94.23	gold quality
monocyte	CL:0000576	94.03	gold quality
mononuclear cell	CL:0000842	93.75	gold quality
epithelium of mammary gland	UBERON:0003244	93.54	gold quality
urinary bladder	UBERON:0001255	93.32	gold quality
leukocyte	CL:0000738	93.17	gold quality
jejunal mucosa	UBERON:0000399	93.08	gold quality
bronchial epithelial cell	CL:0002328	92.96	gold quality
nasal cavity epithelium	UBERON:0005384	92.85	gold quality
vermiform appendix	UBERON:0001154	92.81	gold quality
epithelium of nasopharynx	UBERON:0001951	92.81	gold quality
sural nerve	UBERON:0015488	92.78	gold quality
penis	UBERON:0000989	92.64	gold quality
synovial joint	UBERON:0002217	92.37	gold quality
nasal cavity mucosa	UBERON:0001826	92.31	gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 4.

Experiment	Marker?	Max mean expression
E-GEOD-135922	yes	22.03
E-CURD-122	yes	9.29
E-GEOD-81608	yes	7.87
E-MTAB-6142	no	37.08
E-CURD-112	no	3.62
E-ANND-3	no	0.00

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

207 targets.

Target	Regulation
ABCA4
ABCB1	Unknown
ABCB6
ABCC2	Activation
ABCC3	Activation
ABCC4	Activation
ABCC5	Activation
ABCG2	Unknown
ACHE
ADAM2
AFMID
AGR2
AHR
AHRR	Activation
AIP
ALB
ALDH3A1
APAF1
APOA1
APP
AREG	Activation
ARNT	Unknown
ATM
BAX
BDNF	Repression
BRCA1	Unknown
BTK
CA3	Repression
CA9	Repression
CAD

Upstream regulators (CollecTRI, top): AHR, AHRR, AIP, AR, ARNT, E2F2, EPAS1, ESR1, ESR2, ESRRA, NANOG, NFE2L2, NFIC, NFKB, NFKBID, NKX3-1, NR0B2, NR1H3, NR3C1, OSM, PAX3, PITX2, POU5F1, PPARA, RELB, SIM1, SMAD2, SMAD3, SMAD4, SOX2, SP1, STAT3, TCF3, TP63, VSX2

miRNA regulators (miRDB)

245 targeting AHR, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-3163	100.00	77.23	8605
HSA-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-126-5P	100.00	72.71	3180
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-656-3P	100.00	72.15	2788
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-6740-5P	100.00	65.64	932
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-188-3P	100.00	68.76	1240
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-3185	99.99	68.12	1959
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-6077	99.99	68.04	2299
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-433-3P	99.98	69.37	1203
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-3692-3P	99.98	70.27	2139
HSA-MIR-373-5P	99.98	75.36	4753

Literature-anchored findings (GeneRIF, showing 40)

• polymorphisms that result in loss of CYP1A1 induction (PMID:11689007)
• Phylogenetic analysis shows that AHRR, AHR1, and AHR2 are distinct genes, members of an AHR gene family; these three vertebrate AHR-like genes descended from a single invertebrate AHR (PMID:11742002)
• The female reproductive tract expresses AHR and ARNT mRNA, and changes in expression at target sites in conditions such as endometriosis and uterine leiomyomas suggest a potential role for these factors in the pathogenesis of these conditions. (PMID:11756572)
• Aryl hydrocarbon receptor/dioxin receptor in human monocytes and macrophages (PMID:11768231)
• Functional involvement of the Brahma/SWI2-related gene 1 protein in cytochrome P4501A1 transcription mediated by the aryl hydrocarbon receptor complex (PMID:11805098)
• Arg554Lys was investigated and no association with micropenis was found. (PMID:11835227)
• SRC-1, NCoA-2, and p/CIP are capable of independently enhancing TCDD-dependent induction of a luciferase reporter gene by the AHR/ARNT dimer. (PMID:12024042)
• Two parallel pathways mediate cytoplasmic localization (PMID:12065584)
• The silencing mediator of retinoic acid and thyroid hormone receptors can interact with the aryl hydrocarbon (Ah) receptor but fails to repress Ah receptor-dependent gene expression. (PMID:12139968)
• functional AhR are present in endometrial and endometriotic stromal cells and that TCDD up-regulates the expression of RANTES, providing a possible mechanistic link between dioxin exposure and chemokine expression in endometriosis. (PMID:12200463)
• Polymorphisms that regulate the phenotype of AHR-mediated responses, especially differences among ethnic groups. (PMID:12213390)
• Possible involvement of aryl hydrocarbon receptor (AhR) in adult T-cell leukemia (ATL) leukemogenesis: constitutive activation of AhR in ATL. (PMID:12480531)
• AhR gene expression associates with individual variation of CYP1A1 inducibility and CYP1B1 expression in cultivated lymphocytes (PMID:12520072)
• Binding of ligands such as TCDD, beta-naphthoflavone, and benzopyrene metabolites to the Ah receptor is involved in human UGT1A1 induction. (PMID:12566446)
• experiments revealed a complex distribution of aryl hydrocarbon receptor and aryl hydrocarbon receptor nuclear translocator mRNAs and proteins in rat and human testis (PMID:12586752)
• DNA damage and cell cycle arrest induced by 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203, NSC 703786) is attenuated in aryl hydrocarbon receptor deficient MCF-7 cells (PMID:12592376)
• Inhibitory AhR-ERalpha cross talk is linked to a new pathway for degrading ERalpha in which TCDD initially induces formation of a nuclear AhR complex which coordinately recruits ERalpha & the proteasome complex, resulting in degradation of both receptors. (PMID:12612060)
• results confirm that the Ah receptor plays a critical role in B[a]P-7,8-dihydrodiol-induced apoptosis (PMID:12637498)
• In mice transgenic to this receptor, there is a lessened susceptibility to dioxin-induced toxicity. (PMID:12730383)
• estrogen receptor-mediated estrogen signalling is modulated by a co-regulatory-like function of activated AhR/Arnt, giving rise to adverse oestrogen-related actions of dioxin-type environmental contaminants (PMID:12774124)
• the dioxin receptor is stabilized by XAP2 (PMID:12837759)
• Results describe the recruitment of aryl hydrocarbon receptor and associated proteins to the human cytochrome P4501A1 gene promoter in vivo. (PMID:14560034)
• interactions between the aryl hydrocarbon receptor and estrogen receptor have a role in development of breast neoplasms [review] (PMID:14973392)
• AhR tyrosine 9, which is not a phosphorylated residue itself but is required for DNA binding, appears to play a crucial role in AhR activity by permitting proper phosphorylation of the AhR. (PMID:14978034)
• cell density regulates the intracellular localization and function of AhR, because of modulation of nuclear export activity (PMID:14985336)
• Inhibitory AHR-androgen receptor crosstalk was studied in the LNCaP prostatic tumor cell line. (PMID:15026081)
• AhR activation causes apoptosis and cell cycle arrest, especially through expression changes in genes related to apoptosis and cell cycle arrest. (PMID:15069065)
• Results describe a mechanism whereby the aryl hydrocarbon receptor, a known transcriptional activator, mediates gene repression through interactions at E2F-responsive promoters, leading to the repression of E2F-dependent, S phase-specific genes. (PMID:15123621)
• nucleotide preference of the heterodimers of AHR and Arnt (PMID:15190133)
• Promoters and long-distance regulatory regions of AhR-responsive genes were analyzed by the genetic algorithm and a variety of other computational methods. (PMID:15342792)
• Thirty-two single nucleotide variations have been identified in the aryl hydrocarbon receptor gene, including 25 novel ones and a GGGGC repeat polymorphism in the promoter region. (PMID:15499202)
• MEK1 facilitates ligand-initiated transcriptional activation while targeting the Ah receptor for degradation (PMID:15572374)
• Folding of the aryl hydrocarbon receptor transactivation domain modulates protein-protein interactions, such as the binding of transcription factor TATA-binding protein (TBP). (PMID:15641800)
• AhR activation in the T-lineage cells is directly involved in thymocyte loss and skewed differentiation; AhR activation in T cells and not in B cells suppresses the immunization-induced increase in both T cells and B cells. (PMID:15728486)
• ER alpha-AHR-ARNT protein-protein interactions mediate estradiol-dependent transrepression of dioxin-inducible gene transcription (PMID:15837795)
• AHR pathway plays important role in cigarette smoke-mediated COX-2 and prostaglandin production in human lung fibroblasts and may contribute to tobacco-associated inflammation and lung disease. (PMID:15863442)
• Induction of c-jun depends on activation of p38-mitogen-activated protein kinase (MAPK) by an AhR-dependent mechanism. (PMID:15897893)
• Expression of BCRP is most likely aryl hydrocarbon receptor (AhR) dependent in Caco-2 cells. (PMID:15917307)
• AHR-mediated transcription: ligand-dependent recruitment of Era to TCDD-responsive promoters was studied. (PMID:15964790)
• AhR influences the expression of c-Myc, a protein critical to malignant transformation (PMID:16091746)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	ahr1a	ENSDARG00000020046
mus_musculus	Ahr	ENSMUSG00000019256
rattus_norvegicus	Ahr	ENSRNOG00000004342
drosophila_melanogaster	ss	FBGN0003513
caenorhabditis_elegans	ahr-1	WBGENE00000096

Paralogs (1): AHRR (ENSG00000063438)

Protein

Protein identifiers

Aryl hydrocarbon receptor — P35869 (reviewed: P35869)

Alternative names: Class E basic helix-loop-helix protein 76

All UniProt accessions (2): P35869, A0A2R8Y7G1

UniProt curated annotations — full annotation on UniProt →

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. Upon ligand binding, translocates into the nucleus, where it heterodimerizes with ARNT and induces transcription by binding to xenobiotic response elements (XRE). Regulates a variety of biological processes, including angiogenesis, hematopoiesis, drug and lipid metabolism, cell motility and immune modulation. 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). Mediates biochemical and toxic effects of halogenated aromatic hydrocarbons. Next to xenobiotics, natural ligands derived from plants, microbiota, and endogenous metabolism are potent AHR agonists. Tryptophan (Trp) derivatives constitute an important class of endogenous AHR ligands. 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. Regulates the circadian clock by inhibiting the basal and circadian expression of the core circadian component PER1. Inhibits PER1 by repressing the CLOCK-BMAL1 heterodimer mediated transcriptional activation of PER1. 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.

Subunit / interactions. Homodimer. Heterodimer; efficient DNA binding requires dimerization with another bHLH protein. Interacts with ARNT; 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. Binds MYBBP1A. Interacts with coactivators including SRC-1, RIP140 and NOCA7, and with the corepressor SMRT. Interacts with NEDD8 and IVNS1ABP. Interacts with BMAL1. Interacts with HSP90AB1. Interacts with TIPARP; leading to mono-ADP-ribosylation of AHR and subsequent inhibition of AHR.

Subcellular location. Cytoplasm. Nucleus.

Tissue specificity. Expressed in all tissues tested including blood, brain, heart, kidney, liver, lung, pancreas and skeletal muscle. Expressed in retinal photoreceptors.

Post-translational modifications. Mono-ADP-ribosylated, leading to inhibit transcription activator activity of AHR.

Disease relevance. Retinitis pigmentosa 85 (RP85) [MIM:618345] A form of retinitis pigmentosa, a retinal dystrophy belonging to the group of pigmentary retinopathies. Retinitis pigmentosa is characterized by retinal pigment deposits visible on fundus examination and primary loss of rod photoreceptor cells followed by secondary loss of cone photoreceptors. Patients typically have night vision blindness and loss of midperipheral visual field. As their condition progresses, they lose their far peripheral visual field and eventually central vision as well. RP85 is an autosomal recessive form manifesting as early-onset progressive difficulty to adapt in dim light and gradually decreasing visual acuity in both eyes. The disease is caused by variants affecting the gene represented in this entry. Foveal hypoplasia 3 (FVH3) [MIM:620958] An autosomal recessive form of foveal hypoplasia, a developmental defect of the eye defined as the lack of foveal depression with continuity of all neurosensory retinal layers in the presumed foveal area. Clinical features include absence of foveal pit on optical coherence tomography, absence of foveal hyperpigmentation, absence of foveal avascularity, absence of foveal and macular reflexes, decreased visual acuity, and nystagmus. The disease is caused by variants affecting the gene represented in this entry.

Domain organisation. The PAS 1 domain is essential for dimerization and also required for AHR:ARNT heterodimerization.

Induction. Induced or repressed by TGFB1 and dioxin in a cell-type specific fashion. Repressed by cAMP, retinoic acid, and 12-O-tetradecanoyl phorbol-13 acetate (TPA).

RefSeq proteins (1): NP_001612* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000014	PAS	Domain
IPR001610	PAC	Repeat
IPR011598	bHLH_dom	Domain
IPR013655	PAS_fold_3	Domain
IPR013767	PAS_fold	Domain
IPR033348	AHR_bHLH	Domain
IPR035965	PAS-like_dom_sf	Homologous_superfamily
IPR036638	HLH_DNA-bd_sf	Homologous_superfamily
IPR039091	AHR/AHRR	Family

Pfam: PF00010, PF00989, PF08447

UniProt features (68 total): mutagenesis site 15, helix 15, strand 11, region of interest 6, sequence variant 5, domain 4, short sequence motif 3, sequence conflict 3, turn 2, propeptide 1, chain 1, compositionally biased region 1, modified residue 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
8QMO	ELECTRON MICROSCOPY	2.76
7ZUB	ELECTRON MICROSCOPY	2.85
5NJ8	X-RAY DIFFRACTION	3.3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P35869-F1	56.88	0.22

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (1): 1

Mutagenesis-validated functional residues (15):

Position	Phenotype
36	strongly reduces transcription factor activity.
39	almost abolishes transcription factor activity. no effect on nuclear translocation upon ligand binding.
40	abolishes transcription factor activity. alters on nuclear translocation upon ligand binding.
50	abolishes transcription factor activity; when associated with d-79 and d-82.
74	interferes with transcription factor activity.
79	abolishes transcription factor activity; when associated with d-50 and d-82.
82	abolishes transcription factor activity; when associated with d-50 and d-79.
118–122	strongly reduces transcription factor activity.
118	interferes with transcription factor activity.
122	interferes with transcription factor activity.
136	interferes with transcription factor activity.
154	interferes with transcription factor activity.
381	increases specific ligand binding.
381	abolishes specific ligand binding.
381	no effect on specific ligand binding.

Function

Pathways and Gene Ontology

Reactome pathways

10 pathways

ID	Pathway
R-HSA-1989781	PPARA activates gene expression
R-HSA-211945	Phase I - Functionalization of compounds
R-HSA-211976	Endogenous sterols
R-HSA-211981	Xenobiotics
R-HSA-8937144	Aryl hydrocarbon receptor signalling
R-HSA-1430728	Metabolism
R-HSA-211859	Biological oxidations
R-HSA-211897	Cytochrome P450 - arranged by substrate type
R-HSA-400206	Regulation of lipid metabolism by PPARalpha
R-HSA-556833	Metabolism of lipids

MSigDB gene sets: 615 (showing top): GOBP_CIRCADIAN_RHYTHM, TGGTGCT_MIR29A_MIR29B_MIR29C, GOBP_REGULATION_OF_CELL_ACTIVATION, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_REGULATION_OF_LEUKOCYTE_PROLIFERATION, REACTOME_BIOLOGICAL_OXIDATIONS, GOBP_NEGATIVE_REGULATION_OF_ADAPTIVE_IMMUNE_RESPONSE, MODULE_169, GOBP_INFLAMMATORY_RESPONSE, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_B_CELL_ACTIVATION, GOBP_REGULATION_OF_ADAPTIVE_IMMUNE_RESPONSE, GOBP_CELLULAR_RESPONSE_TO_BIOTIC_STIMULUS, GOBP_NEGATIVE_REGULATION_OF_LEUKOCYTE_MEDIATED_IMMUNITY, MODULE_64

GO Biological Process (23): blood vessel development (GO:0001568), regulation of adaptive immune response (GO:0002819), negative regulation of T cell mediated immune response to tumor cell (GO:0002841), regulation of DNA-templated transcription (GO:0006355), regulation of transcription by RNA polymerase II (GO:0006357), xenobiotic metabolic process (GO:0006805), apoptotic process (GO:0006915), response to xenobiotic stimulus (GO:0009410), response to toxic substance (GO:0009636), regulation of gene expression (GO:0010468), regulation of B cell proliferation (GO:0030888), circadian regulation of gene expression (GO:0032922), negative regulation of DNA-templated transcription (GO:0045892), positive regulation of DNA-templated transcription (GO:0045893), positive regulation of transcription by RNA polymerase II (GO:0045944), negative regulation of inflammatory response (GO:0050728), cellular response to molecule of bacterial origin (GO:0071219), cellular response to cAMP (GO:0071320), cellular response to forskolin (GO:1904322), cellular response to 2,3,7,8-tetrachlorodibenzodioxine (GO:1904613), intracellular receptor signaling pathway (GO:0030522), rhythmic process (GO:0048511), intestinal epithelial structure maintenance (GO:0060729)

GO Molecular Function (17): transcription cis-regulatory region binding (GO:0000976), DNA-binding transcription factor activity, RNA polymerase II-specific (GO:0000981), cis-regulatory region sequence-specific DNA binding (GO:0000987), TFIID-class transcription factor complex binding (GO:0001094), transcription coactivator binding (GO:0001223), DNA binding (GO:0003677), DNA-binding transcription factor activity (GO:0003700), nuclear receptor activity (GO:0004879), TBP-class protein binding (GO:0017025), protein homodimerization activity (GO:0042803), protein heterodimerization activity (GO:0046982), Hsp90 protein binding (GO:0051879), RNA polymerase II-specific DNA-binding transcription factor binding (GO:0061629), E-box binding (GO:0070888), sequence-specific double-stranded DNA binding (GO:1990837), protein binding (GO:0005515), protein dimerization activity (GO:0046983)

GO Cellular Component (10): chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), transcription regulator complex (GO:0005667), cytoplasm (GO:0005737), cytosol (GO:0005829), protein-containing complex (GO:0032991), aryl hydrocarbon receptor complex (GO:0034751), cytosolic aryl hydrocarbon receptor complex (GO:0034752), nuclear aryl hydrocarbon receptor complex (GO:0034753)

Reactome top-level categories

Rollup of top-6 pathways:

Category	Pathways
Cytochrome P450 - arranged by substrate type	2
Phase I - Functionalization of compounds	2
Metabolism	2
Regulation of lipid metabolism by PPARalpha	1
Biological oxidations	1
Metabolism of lipids	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
regulation of DNA-templated transcription	4
cellular anatomical structure	4
DNA-templated transcription	3
regulation of gene expression	2
transcription by RNA polymerase II	2
response to chemical	2
regulation of transcription by RNA polymerase II	2
transcription cis-regulatory region binding	2
protein dimerization activity	2
aryl hydrocarbon receptor complex	2
vasculature development	1
anatomical structure development	1
adaptive immune response	1
regulation of immune response	1
T cell mediated immune response to tumor cell	1
negative regulation of T cell mediated immunity	1
negative regulation of immune response to tumor cell	1
regulation of T cell mediated immune response to tumor cell	1
regulation of RNA biosynthetic process	1
metabolic process	1
cellular response to xenobiotic stimulus	1
programmed cell death	1
apoptotic signaling pathway	1
execution phase of apoptosis	1
gene expression	1
regulation of macromolecule biosynthetic process	1
B cell proliferation	1
regulation of lymphocyte proliferation	1
regulation of B cell activation	1
circadian rhythm	1
negative regulation of RNA biosynthetic process	1
positive regulation of RNA biosynthetic process	1
positive regulation of DNA-templated transcription	1
inflammatory response	1
negative regulation of defense response	1
negative regulation of response to external stimulus	1
regulation of inflammatory response	1
response to molecule of bacterial origin	1
cellular response to biotic stimulus	1
response to cAMP	1

Protein interactions and networks

STRING

684 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
AHR	CYP1A1	P04798	957
AHR	CYP1A2	P05177	865
AHR	HSP90AB1	P08238	736
AHR	HSP90AA1	P07900	717
AHR	CYP1B1	Q16678	690
AHR	AIP	O00170	663
AHR	TSPO	P30536	642
AHR	CYP2B6	P20813	605
AHR	PPIG	Q13427	526
AHR	UGT1A6	P19224	518
AHR	ALDH3A1	P30838	507
AHR	ARNT	P27540	496
AHR	ESR2	Q92731	496
AHR	RELB	Q01201	484
AHR	NR1I2	O75469	476

IntAct

54 interactions, top by confidence:

A	B	Type	Score
AHR	ARNT	psi-mi:“MI:0914”(association)	0.740
ARNT	AHR	psi-mi:“MI:0914”(association)	0.740
AHR	EBNA3	psi-mi:“MI:0407”(direct interaction)	0.620
AHR	EBNA3	psi-mi:“MI:0915”(physical association)	0.620
EBNA3	AHR	psi-mi:“MI:0915”(physical association)	0.620
TSPYL6	NME4	psi-mi:“MI:0914”(association)	0.530
ARNT	HSPA8	psi-mi:“MI:0914”(association)	0.530
HSPB8	VWA8	psi-mi:“MI:0914”(association)	0.530
CLEC11A	VWA8	psi-mi:“MI:0914”(association)	0.530
PTGES3	AIP	psi-mi:“MI:0914”(association)	0.530
NCOA7	AHR	psi-mi:“MI:0915”(physical association)	0.500
NCOR2	AHR	psi-mi:“MI:0915”(physical association)	0.500
AIP	AHR	psi-mi:“MI:0403”(colocalization)	0.460
AHR	AIP	psi-mi:“MI:0403”(colocalization)	0.460
AIP	AHR	psi-mi:“MI:0915”(physical association)	0.460
AHR	CTNNB1	psi-mi:“MI:0915”(physical association)	0.400
AHR	RAB14	psi-mi:“MI:0915”(physical association)	0.400
MAF	AHR	psi-mi:“MI:0915”(physical association)	0.400
AHR	RB1	psi-mi:“MI:0915”(physical association)	0.370
RB1	AHR	psi-mi:“MI:0915”(physical association)	0.370
EP300	AHR	psi-mi:“MI:0915”(physical association)	0.370
Xpo1	IFT56	psi-mi:“MI:0914”(association)	0.350
DDB1	CTNNB1	psi-mi:“MI:0914”(association)	0.350
IQCN	TARSL2	psi-mi:“MI:0914”(association)	0.350
SIRT6	HDAC3	psi-mi:“MI:0914”(association)	0.350
M		psi-mi:“MI:0914”(association)	0.350

BioGRID (241): GNA13 (Affinity Capture-Western), NCOA1 (Affinity Capture-Western), NCOA1 (Two-hybrid), AHR (Reconstituted Complex), XPO1 (Affinity Capture-Western), AIP (Affinity Capture-Western), AHR (Reconstituted Complex), AIP (Reconstituted Complex), AHR (Reconstituted Complex), AHR (Affinity Capture-MS), AHR (Affinity Capture-Western), ARNT (Affinity Capture-Western), ARNT (Reconstituted Complex), AHR (Reconstituted Complex), ARNT (Reconstituted Complex)

ESM2 similar proteins: A0MLS5, G5EGD2, O00327, O02219, O02747, O02748, O15945, O35800, O44712, O88529, P27540, P30561, P35869, P41738, P41739, P53762, P56645, P79832, P97481, Q0PGG7, Q16665, Q17062, Q2VPD4, Q309Z6, Q5R4T2, Q61221, Q61324, Q6YGZ5, Q78E60, Q8K3T2, Q8QGQ7, Q8QGQ8, Q8R4S2, Q8R4S4, Q8R4S5, Q8R4S6, Q8R4S7, Q8WYA1, Q91YA9, Q95LD9

Diamond homologs: A1YFY6, A2T6X9, A9YTQ3, E7FFX1, O02747, O09000, O44712, O57539, O61734, P30561, P35869, P41738, P70365, P81133, P90953, P97459, Q0VBL6, Q14190, Q15788, Q24119, Q2VPD4, Q3U1U7, Q4PJW2, Q61045, Q61079, Q75NT5, Q8R4S2, Q8R4S4, Q8R4S5, Q8R4S6, Q8R4S7, Q95LD9, Q98SJ5, Q99742, Q9JHS2, Q9WVS9, Q9Y2N7, B5DE09, O15945, Q15596

SIGNOR signaling

22 interactions.

A	Effect	B	Mechanism
OSM	“up-regulates quantity by expression”	AHR	“transcriptional regulation”
AHR	“up-regulates quantity by expression”	CYP1B1	“transcriptional regulation”
AHR	“up-regulates quantity by expression”	UGT1A1	“transcriptional regulation”
AHR	“up-regulates quantity by expression”	CYP1A1	“transcriptional regulation”
GSK3B	“up-regulates activity”	AHR	phosphorylation
AHR	“form complex”	AHR-ARNT	binding
resveratrol	“down-regulates activity”	AHR	“chemical inhibition”
“bisphenol A”	“up-regulates activity”	AHR	“chemical activation”
4,4’-sulfonyldiphenol	“up-regulates activity”	AHR	“chemical activation”
“bisphenol F”	“up-regulates activity”	AHR	“chemical activation”
Monobutylphthalate	“up-regulates activity”	AHR	“chemical activation”
PLK1	“down-regulates activity”	AHR	phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

547 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	6
Likely pathogenic	2
Uncertain significance	309
Likely benign	198
Benign	15

Top pathogenic / likely-pathogenic (8)

Variant ID	HGVS	Classification
1349767	NM_001621.5(AHR):c.1910_1911del (p.Gln637fs)	Pathogenic
1356494	NM_001621.5(AHR):c.1192C>T (p.Arg398Ter)	Pathogenic
2036021	NM_001621.5(AHR):c.1273del (p.Asp425fs)	Pathogenic
2070119	NM_001621.5(AHR):c.1565C>A (p.Ser522Ter)	Pathogenic
3340538	NM_001621.5(AHR):c.899_908+15del	Pathogenic
619236	NM_001621.5(AHR):c.1160+1G>A	Pathogenic
1063117	NM_001621.5(AHR):c.575-2A>G	Likely pathogenic
3383354	NM_001621.5(AHR):c.528G>A (p.Trp176Ter)	Likely pathogenic

SpliceAI

1039 predictions. Top by Δscore:

Variant	Effect	Δscore
7:17299327:AAC:A	donor_gain	1.0000
7:17299328:AC:A	donor_gain	1.0000
7:17299330:G:GG	donor_gain	1.0000
7:17309926:T:TA	acceptor_gain	1.0000
7:17309931:TTCAG:T	acceptor_gain	1.0000
7:17309932:TCAG:T	acceptor_gain	1.0000
7:17309933:CAG:C	acceptor_gain	1.0000
7:17309933:CAGAG:C	acceptor_gain	1.0000
7:17309934:A:AG	acceptor_gain	1.0000
7:17309934:A:AT	acceptor_loss	1.0000
7:17309934:AGA:A	acceptor_gain	1.0000
7:17309934:AGAG:A	acceptor_gain	1.0000
7:17309935:G:GA	acceptor_gain	1.0000
7:17309935:GA:G	acceptor_gain	1.0000
7:17309935:GAG:G	acceptor_gain	1.0000
7:17309935:GAGT:G	acceptor_gain	1.0000
7:17309935:GAGTA:G	acceptor_gain	1.0000
7:17310120:GATG:G	donor_gain	1.0000
7:17310122:TGG:T	donor_loss	1.0000
7:17310123:GGT:G	donor_loss	1.0000
7:17310124:G:GG	donor_gain	1.0000
7:17310124:GT:G	donor_loss	1.0000
7:17310125:T:A	donor_loss	1.0000
7:17322496:CATA:C	acceptor_loss	1.0000
7:17322497:A:AG	acceptor_gain	1.0000
7:17322497:ATAGT:A	acceptor_loss	1.0000
7:17322498:T:G	acceptor_gain	1.0000
7:17322498:TAGTT:T	acceptor_loss	1.0000
7:17322499:A:AG	acceptor_gain	1.0000
7:17322499:AGTT:A	acceptor_gain	1.0000

AlphaMissense

5642 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
7:17309979:A:G	K37E	1.000
7:17309981:G:C	K37N	1.000
7:17309981:G:T	K37N	1.000
7:17309985:C:G	H39D	1.000
7:17309987:T:A	H39Q	1.000
7:17309987:T:G	H39Q	1.000
7:17309989:G:C	R40T	1.000
7:17309989:G:T	R40I	1.000
7:17309990:A:C	R40S	1.000
7:17309990:A:T	R40S	1.000
7:17309995:G:C	R42P	1.000
7:17309998:T:A	L43H	1.000
7:17309998:T:C	L43P	1.000
7:17310063:G:C	D65H	1.000
7:17310064:A:C	D65A	1.000
7:17310064:A:T	D65V	1.000
7:17310066:A:G	K66E	1.000
7:17310079:T:A	L70H	1.000
7:17310079:T:C	L70P	1.000
7:17310082:G:T	R71M	1.000
7:17310085:T:C	L72P	1.000
7:17330881:T:C	F234L	1.000
7:17330883:T:A	F234L	1.000
7:17330883:T:G	F234L	1.000
7:17299301:C:A	R13S	0.999
7:17309977:C:A	S36Y	0.999
7:17309977:C:T	S36F	0.999
7:17309980:A:C	K37T	0.999
7:17309980:A:T	K37M	0.999
7:17309983:G:C	R38P	0.999

dbSNP variants (sampled 300 via entrez): RS1000009536 (7:17320724 C>T), RS1000049380 (7:17341666 T>A), RS1000055820 (7:17305921 C>T), RS1000137040 (7:17314471 T>G), RS1000235061 (7:17305620 C>A), RS1000293346 (7:17311976 C>T), RS1000401100 (7:17324248 G>C), RS1000470442 (7:17317841 T>C), RS1000622428 (7:17323930 G>A), RS1000672298 (7:17305366 G>A), RS1000673807 (7:17317833 C>G,T), RS1000718139 (7:17337260 A>C), RS1000951621 (7:17345278 A>C,T), RS1001061710 (7:17300814 A>G,T), RS1001098597 (7:17342832 A>C)

Disease associations

OMIM: gene MIM:600253 | disease phenotypes: MIM:618345, MIM:620958

GenCC curated gene-disease

Disease	Classification	Inheritance
retinitis pigmentosa 85	Strong	Autosomal recessive
foveal hypoplasia 3	Moderate	Autosomal recessive
retinitis pigmentosa	Supportive	Autosomal dominant
foveal hypoplasia	Limited	Autosomal recessive

Mondo (5): retinitis pigmentosa 85 (MONDO:0032689), inherited retinal dystrophy (MONDO:0019118), foveal hypoplasia 3 (MONDO:0975805), foveal hypoplasia (MONDO:0044203), retinitis pigmentosa (MONDO:0019200)

Orphanet (1): OBSOLETE: Inherited retinal disorder (Orphanet:71862)

HPO phenotypes

49 total (30 of 49 shown, HPO-id order):

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0000405	Conductive hearing impairment
HP:0000407	Sensorineural hearing impairment
HP:0000501	Glaucoma
HP:0000505	Visual impairment
HP:0000510	Rod-cone dystrophy
HP:0000512	Abnormal electroretinogram
HP:0000543	Optic disc pallor
HP:0000546	Retinal degeneration
HP:0000551	Color vision defect
HP:0000563	Keratoconus
HP:0000602	Ophthalmoplegia
HP:0000613	Photophobia
HP:0000618	Blindness
HP:0000639	Nystagmus
HP:0000648	Optic atrophy
HP:0000662	Nyctalopia
HP:0000666	Horizontal nystagmus
HP:0000842	Hyperinsulinemia
HP:0001105	Retinal atrophy
HP:0001123	Visual field defect
HP:0001477	Compensatory chin elevation
HP:0002353	EEG abnormality
HP:0003623	Neonatal onset
HP:0004328	Abnormal anterior eye segment morphology
HP:0007663	Reduced visual acuity
HP:0007675	Progressive night blindness
HP:0007703	Abnormal retinal pigmentation
HP:0007737	Spicular pigmentation of the retina
HP:0007750	Hypoplasia of the fovea

GWAS associations

58 associations (top):

Study	Trait	p-value
GCST000992_2	Coffee consumption	2.000000e-11
GCST001032_6	Caffeine consumption	2.000000e-19
GCST001217_36	Metabolic traits	5.000000e-15
GCST002650_3	Coffee consumption (cups per day)	3.000000e-17
GCST002651_4	Coffee consumption	7.000000e-15
GCST003043_185	Inflammatory bowel disease	6.000000e-07
GCST003045_17	Ulcerative colitis	6.000000e-09
GCST003123_17	Severe influenza A (H1N1) infection	7.000000e-11
GCST003655_11	Cutaneous squamous cell carcinoma	4.000000e-08
GCST003846_1	Caffeine metabolism (plasma 1,3,7-trimethylxanthine (caffeine) level)	2.000000e-13
GCST003846_2	Caffeine metabolism (plasma 1,3,7-trimethylxanthine (caffeine) level)	5.000000e-13
GCST003846_3	Caffeine metabolism (plasma 1,3,7-trimethylxanthine (caffeine) level)	5.000000e-09
GCST003846_4	Caffeine metabolism (plasma 1,3,7-trimethylxanthine (caffeine) level)	5.000000e-06
GCST003846_5	Caffeine metabolism (plasma 1,3,7-trimethylxanthine (caffeine) level)	6.000000e-06
GCST003846_6	Caffeine metabolism (plasma 1,3,7-trimethylxanthine (caffeine) level)	2.000000e-06
GCST003851_1	Caffeine metabolism (plasma 1,7-dimethylxanthine (paraxanthine) to 1,3,7-trimethylxanthine (caffeine) ratio)	2.000000e-09
GCST003851_2	Caffeine metabolism (plasma 1,7-dimethylxanthine (paraxanthine) to 1,3,7-trimethylxanthine (caffeine) ratio)	5.000000e-10
GCST003851_24	Caffeine metabolism (plasma 1,7-dimethylxanthine (paraxanthine) to 1,3,7-trimethylxanthine (caffeine) ratio)	5.000000e-10
GCST003851_25	Caffeine metabolism (plasma 1,7-dimethylxanthine (paraxanthine) to 1,3,7-trimethylxanthine (caffeine) ratio)	1.000000e-09
GCST003851_29	Caffeine metabolism (plasma 1,7-dimethylxanthine (paraxanthine) to 1,3,7-trimethylxanthine (caffeine) ratio)	7.000000e-16
GCST003851_3	Caffeine metabolism (plasma 1,7-dimethylxanthine (paraxanthine) to 1,3,7-trimethylxanthine (caffeine) ratio)	1.000000e-09
GCST003851_30	Caffeine metabolism (plasma 1,7-dimethylxanthine (paraxanthine) to 1,3,7-trimethylxanthine (caffeine) ratio)	3.000000e-17
GCST003851_31	Caffeine metabolism (plasma 1,7-dimethylxanthine (paraxanthine) to 1,3,7-trimethylxanthine (caffeine) ratio)	2.000000e-09
GCST004250_36	Alanine aminotransferase (ALT) levels after remission induction therapy in actute lymphoblastic leukemia (ALL)	4.000000e-06
GCST004749_17	Lung cancer in ever smokers	3.000000e-07
GCST005330_4	Coffee consumption	5.000000e-07
GCST005342_3	Plasma kynurenine levels in major depressive disorder	6.000000e-06
GCST005790_2	Rosacea symptom severity	3.000000e-06
GCST006463_11	Urinary albumin excretion (no hypertensive medication)	1.000000e-18
GCST006586_17	Urinary albumin excretion	3.000000e-25

EFO canonical traits (20, from GWAS)

EFO ID	Trait name
EFO:0004330	coffee consumption
EFO:0004725	metabolite measurement
EFO:0006782	cups of coffee per day measurement
EFO:1001488	influenza A (H1N1)
EFO:1001927	cutaneous squamous cell carcinoma
EFO:0007872	caffeine metabolite measurement
EFO:0007965	response to combination chemotherapy
EFO:0008529	kynurenine measurement
EFO:0009180	rosacea severity measurement
EFO:0004285	albuminuria
EFO:0007778	urinary albumin to creatinine ratio
EFO:0006781	coffee consumption measurement
EFO:0010089	bitter beverage consumption measurement
EFO:0010093	bitter non-alcoholic beverage consumption measurement
EFO:0010090	sweet beverage consumption measurement
EFO:0010091	tea consumption measurement
EFO:0009282	sodium measurement
EFO:0009283	potassium measurement
EFO:0004612	high density lipoprotein cholesterol measurement
EFO:0004530	triglyceride measurement

MeSH disease descriptors (2)

Descriptor	Name	Tree numbers
D058499	Retinal Dystrophies	C11.768.585.658
D012174	Retinitis Pigmentosa	C11.270.684; C11.768.585.658.500; C16.320.290.684

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (4): CHEMBL3201 (SINGLE PROTEIN), CHEMBL4742276 (PROTEIN-PROTEIN INTERACTION), CHEMBL4748226 (PROTEIN-PROTEIN INTERACTION), CHEMBL6193798 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

9 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 55,346 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL259571	TAPINAROF	4	641
CHEMBL446452	ARUNDINE	3	2,826
CHEMBL599552	INDIGO	3	6,024
CHEMBL1276127	INDIRUBIN	2	181
CHEMBL1773683	EZUTROMID	2	128
CHEMBL6068017	ILANTIMOD	2	24
CHEMBL150	KAEMPFEROL	1	25,940
CHEMBL299155	TRANSTORINE	1	5,635
CHEMBL498416	L-KYNURENINE	1	13,947

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB clinical annotations

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs4410790	Metabolism/PK	3	olanzapine	Psychotic Disorder

PharmGKB variants

3 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2066853	AHR		0.00	0
rs4410790	AHR	3	2.25	1	olanzapine
rs75519181	AHR		0.00	0

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: other protein — Aryl hydrocarbon receptor

Most potent curated ligand interactions (4 total), top 4:

Ligand	Action	Affinity	Parameter
indolo[3,2-b]carbazole	Agonist	9.72	pKd
ezutromid	Antagonist	7.3	pKd
tapinarof	Agonist	7.0	pKd
indole-3-carbinol	Agonist	4.57	pKd

Binding affinities (BindingDB)

8 measured of 9 human assays (9 total across all organisms); most potent 8 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
2-[(1-methylindol-3-yl)methyl]-1H-indole-3-carbaldehyde	EC50	55 nM	US-9969686: Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
3-(1H-indol-2-ylmethyl)-1-methylindole	EC50	86 nM	US-9969686: Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
2-[(5-chloro-1H-indol-3-yl)methyl]-1H-indole-3-carbaldehyde	EC50	93 nM	US-9969686: Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
3-(1H-indol-2-ylmethyl)-5-methoxy-1H-indole	EC50	94 nM	US-9969686: Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
2-(1H-indol-3-ylmethyl)-1H-indole	EC50	215 nM	US-9969686: Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
2-[(5-methoxy-1H-indol-3-yl)methyl]-1H-indole-3-carbaldehyde	EC50	230 nM	US-9969686: Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
2-(1H-indol-3-ylmethyl)-1H-indole-3-carbaldehyde	EC50	270 nM	US-9969686: Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
2-[(7-chloro-1H-indol-3-yl)methyl]-1H-indole-3-carbaldehyde	EC50	320 nM	US-9969686: Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them

ChEMBL bioactivities

411 potent at pChembl≥5 of 482 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	EC50	0.01	nM	CHEMBL5289699
10.52	EC50	0.03	nM	CHEMBL5203882
10.15	Kd	0.07	nM	CHEMBL472031
10.01	EC50	0.0971	nM	CHEMBL5285977
9.89	Kd	0.13	nM	CHEMBL4580482
9.86	EC50	0.137	nM	CHEMBL5270440
9.81	EC50	0.154	nM	CHEMBL5597486
9.79	EC50	0.161	nM	CHEMBL5266782
9.72	Kd	0.19	nM	CHEMBL509307
9.72	EC50	0.189	nM	CHEMBL5265853
9.70	EC50	0.2	nM	INDIRUBIN
9.70	Ki	0.2	nM	CHEMBL179510
9.67	EC50	0.214	nM	CHEMBL5271031
9.64	EC50	0.227	nM	CHEMBL5597246
9.62	EC50	0.237	nM	CHEMBL5589840
9.59	EC50	0.26	nM	CHEMBL4646273
9.57	EC50	0.27	nM	CHEMBL5190861
9.56	EC50	0.275	nM	CHEMBL5284079
9.55	EC50	0.279	nM	CHEMBL5596667
9.55	EC50	0.283	nM	CHEMBL5597439
9.53	EC50	0.297	nM	CHEMBL5274394
9.52	EC50	0.304	nM	CHEMBL5280290
9.47	EC50	0.34	nM	CHEMBL5021347
9.47	EC50	0.34	nM	CHEMBL5270280
9.41	EC50	0.389	nM	CHEMBL5275365
9.39	EC50	0.404	nM	CHEMBL5596304
9.36	EC50	0.44	nM	CHEMBL5194336
9.35	EC50	0.4467	nM	CHEMBL137408
9.33	EC50	0.468	nM	CHEMBL5267272
9.29	EC50	0.511	nM	CHEMBL5269910
9.15	EC50	0.7	nM	CHEMBL5186309
9.08	EC50	0.83	nM	CHEMBL5181725
9.05	IC50	0.885	nM	CHEMBL5281742
8.93	EC50	1.169	nM	CHEMBL136453
8.92	EC50	1.2	nM	CHEMBL4750416
8.83	EC50	1.479	nM	CHEMBL136430
8.82	EC50	1.5	nM	CHEMBL341968
8.80	EC50	1.6	nM	CHEMBL5198290
8.70	EC50	2	nM	CHEMBL137055
8.70	EC50	2	nM	CHEMBL4750416
8.70	EC50	2	nM	CHEMBL4764225
8.69	EC50	2.04	nM	CHEMBL472031
8.60	EC50	2.5	nM	CHEMBL4764225
8.59	IC50	2.6	nM	CHEMBL4536502
8.49	EC50	3.2	nM	CHEMBL5186309
8.30	EC50	5	nM	INDIGO
8.30	EC50	5	nM	BENZO[DEF]CHRYSENE
8.18	EC50	6.607	nM	CHEMBL137665
8.08	EC50	8.4	nM	BETA-NAPHTHOFLAVONE
8.07	IC50	8.5	nM	CHEMBL6092015

PubChem BioAssay actives

208 with measured affinity, of 766 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
2,10,20-triazapentacyclo[11.7.1.03,8.09,21.014,19]henicosa-1,3,5,7,9,11,13(21),14,16,18-decaene	1946334: Agonist activity at AhR (unknown origin)	ec50	<0.0001	uM
6-bromo-2-(4-bromophenyl)-[1,2,4]triazolo[1,5-a]pyridine	1901915: Agonist activity at AhR in human recombinant HepG2-Lucia AhR cell incubated for 24 hrs by luciferase reporter gene assay	ec50	<0.0001	uM
1,3,8-trichloro-6-methyldibenzofuran	1527832: Binding affinity to AhR (unknown origin)	kd	0.0001	uM
(5R)-1,5-dimethyl-2-oxo-N-phenyl-5,6,7,8-tetrahydroquinoline-3-carboxamide	1956510: Agonist activity at human AHR in HEK293 cells assessed as nuclear translocation over cytosol incubated for 45 mins by Hoechst staining based assay	ec50	0.0001	uM
5,11-dihydroindolo[3,2-b]carbazole-12-carbaldehyde	1946333: Binding affinity to AhR (unknown origin) assessed as dissociation constant	kd	0.0001	uM
1-methyl-N-(4-methylphenyl)-2-oxoquinoline-3-carboxamide	1948803: Agonist activity at EGFP-tagged human AhR transfected in HEK293 cells assessed as induction of nuclear translocation incubated for 45 mins by fluorescence based assay	ec50	0.0001	uM
2-(2-hydroxy-1H-indol-3-yl)indol-3-one	1946335: Activation of human AhR expressed in Saccharomyces cerevisiae YCM3 coexpressing ARNT incubated for 18 hrs	ec50	0.0002	uM
1,3-dichloro-5-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]benzene	1946337: Binding affinity to AhR (unknown origin) assessed as inhibition constant	ki	0.0002	uM
N-(4-fluorophenyl)-1-methyl-2-oxoquinoline-3-carboxamide	1948803: Agonist activity at EGFP-tagged human AhR transfected in HEK293 cells assessed as induction of nuclear translocation incubated for 45 mins by fluorescence based assay	ec50	0.0002	uM
(5R)-N-(1H-indol-2-yl)-1,5-dimethyl-2-oxo-6,7-dihydro-5H-cyclopenta[b]pyridine-3-carboxamide	1956510: Agonist activity at human AHR in HEK293 cells assessed as nuclear translocation over cytosol incubated for 45 mins by Hoechst staining based assay	ec50	0.0002	uM
(5S)-1,5-dimethyl-2-oxo-N-phenyl-5,6,7,8-tetrahydroquinoline-3-carboxamide	1956510: Agonist activity at human AHR in HEK293 cells assessed as nuclear translocation over cytosol incubated for 45 mins by Hoechst staining based assay	ec50	0.0002	uM
3,5-dihydro-2H-pyrido[3,4-f][1,4]oxazepin-4-yl(1H-indazol-3-yl)methanone	2120443: Agonist activity at human AHR stably tranfected in HEK293-T-REx cells co-expressing EGFP assessed as increase in AHR nuclear translocation incubated for 45 mins by Hoechst staining based fluorescence imaging analysis	ec50	0.0002	uM
3,5-dihydro-2H-1,4-benzoxazepin-4-yl-(7-fluoro-2H-indazol-3-yl)methanone	2120443: Agonist activity at human AHR stably tranfected in HEK293-T-REx cells co-expressing EGFP assessed as increase in AHR nuclear translocation incubated for 45 mins by Hoechst staining based fluorescence imaging analysis	ec50	0.0002	uM
(7-fluoro-1,2,3,5-tetrahydro-1,4-benzodiazepin-4-yl)-(1H-indazol-3-yl)methanone	2120443: Agonist activity at human AHR stably tranfected in HEK293-T-REx cells co-expressing EGFP assessed as increase in AHR nuclear translocation incubated for 45 mins by Hoechst staining based fluorescence imaging analysis	ec50	0.0002	uM
5,11-dihydroindolo[3,2-b]carbazole	1946333: Binding affinity to AhR (unknown origin) assessed as dissociation constant	kd	0.0002	uM
6-bromo-2-(4-bromophenyl)-3-oxido-[1,2,4]triazolo[1,5-a]pyridin-3-ium	1901915: Agonist activity at AhR in human recombinant HepG2-Lucia AhR cell incubated for 24 hrs by luciferase reporter gene assay	ec50	0.0003	uM
5-methyl-11H-indolo[3,2-b]carbazole-6-carbaldehyde	1656901: Agonist activity at AhR in human HepG2 cells assessed as induction of CYP1A1 expression after 24 hrs by ethoxyresorufin-O-deethylase assay	ec50	0.0003	uM
(6S)-1,6-dimethyl-2-oxo-N-phenyl-5,6,7,8-tetrahydroquinoline-3-carboxamide	1956510: Agonist activity at human AHR in HEK293 cells assessed as nuclear translocation over cytosol incubated for 45 mins by Hoechst staining based assay	ec50	0.0003	uM
(6R)-1,6-dimethyl-2-oxo-N-phenyl-6,7-dihydro-5H-cyclopenta[b]pyridine-3-carboxamide	1956510: Agonist activity at human AHR in HEK293 cells assessed as nuclear translocation over cytosol incubated for 45 mins by Hoechst staining based assay	ec50	0.0003	uM
N-(5-fluoro-1,3-thiazol-2-yl)-1,5-dimethyl-2-oxo-6,7-dihydro-5H-cyclopenta[b]pyridine-3-carboxamide	1956510: Agonist activity at human AHR in HEK293 cells assessed as nuclear translocation over cytosol incubated for 45 mins by Hoechst staining based assay	ec50	0.0003	uM
N-(4-methoxyphenyl)-1-methyl-2-oxoquinoline-3-carboxamide	1948803: Agonist activity at EGFP-tagged human AhR transfected in HEK293 cells assessed as induction of nuclear translocation incubated for 45 mins by fluorescence based assay	ec50	0.0003	uM
3,5-dihydro-2H-pyrido[3,4-f][1,4]oxazepin-4-yl-(5-fluoro-1H-indazol-3-yl)methanone	2120443: Agonist activity at human AHR stably tranfected in HEK293-T-REx cells co-expressing EGFP assessed as increase in AHR nuclear translocation incubated for 45 mins by Hoechst staining based fluorescence imaging analysis	ec50	0.0003	uM
(7-fluoro-2H-indazol-3-yl)-(1,2,3,5-tetrahydro-1,4-benzodiazepin-4-yl)methanone	2120443: Agonist activity at human AHR stably tranfected in HEK293-T-REx cells co-expressing EGFP assessed as increase in AHR nuclear translocation incubated for 45 mins by Hoechst staining based fluorescence imaging analysis	ec50	0.0003	uM
2-(4-bromophenyl)-6-chloro-3-oxido-[1,2,4]triazolo[1,5-a]pyridin-3-ium	1901915: Agonist activity at AhR in human recombinant HepG2-Lucia AhR cell incubated for 24 hrs by luciferase reporter gene assay	ec50	0.0003	uM
6-bromo-2-[4-(trifluoromethyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridine	1901915: Agonist activity at AhR in human recombinant HepG2-Lucia AhR cell incubated for 24 hrs by luciferase reporter gene assay	ec50	0.0004	uM
N-(5-fluoro-2-pyridinyl)-1-methyl-2-oxoquinoline-3-carboxamide	1948803: Agonist activity at EGFP-tagged human AhR transfected in HEK293 cells assessed as induction of nuclear translocation incubated for 45 mins by fluorescence based assay	ec50	0.0004	uM
(6-fluoro-3,5-dihydro-2H-1,4-benzoxazepin-4-yl)-(1H-indazol-3-yl)methanone	2120443: Agonist activity at human AHR stably tranfected in HEK293-T-REx cells co-expressing EGFP assessed as increase in AHR nuclear translocation incubated for 45 mins by Hoechst staining based fluorescence imaging analysis	ec50	0.0004	uM
2,8-dibromo-3,7-dichlorodibenzo-p-dioxin	39064: Affinity on cytosolic Aromatic hydrocarbon receptor (Ah)	ec50	0.0004	uM
N-(4-fluorophenyl)-11-oxo-1-azatricyclo[6.3.1.04,12]dodeca-4,6,8(12),9-tetraene-10-carboxamide	1948803: Agonist activity at EGFP-tagged human AhR transfected in HEK293 cells assessed as induction of nuclear translocation incubated for 45 mins by fluorescence based assay	ec50	0.0005	uM
N-(4-fluorophenyl)-1-methyl-2-oxo-1,8-naphthyridine-3-carboxamide	1948803: Agonist activity at EGFP-tagged human AhR transfected in HEK293 cells assessed as induction of nuclear translocation incubated for 45 mins by fluorescence based assay	ec50	0.0005	uM
(13aS)-10-bromo-11-chloro-5,6,13,13a-tetrahydroisoquinolino[2,1-b]isoquinolin-8-one	1897737: Activation of AhR in human HaCaT cells assessed as induction of XRE-dependent reporter activity incubated for 4 hrs by Renilla/Firefly based dual-luciferase reporter assay	ec50	0.0007	uM
6-bromo-2-(4-chlorophenyl)-[1,2,4]triazolo[1,5-a]pyridine	1901915: Agonist activity at AhR in human recombinant HepG2-Lucia AhR cell incubated for 24 hrs by luciferase reporter gene assay	ec50	0.0008	uM
N-[(2S)-1-hydroxypropan-2-yl]-2-pyridin-3-yl-6-[4-(trifluoromethoxy)phenyl]pyrimidine-4-carboxamide	1946343: Antagonist activity at AhR (unknown origin)	ic50	0.0009	uM
2,3,7-tribromodibenzo-p-dioxin	39064: Affinity on cytosolic Aromatic hydrocarbon receptor (Ah)	ec50	0.0012	uM
1H-indol-3-yl-[6-(trifluoromethyl)-2-pyridinyl]methanone	1946334: Agonist activity at AhR (unknown origin)	ec50	0.0012	uM
2,3-dibromo-7,8-dichlorodibenzo-p-dioxin	39064: Affinity on cytosolic Aromatic hydrocarbon receptor (Ah)	ec50	0.0015	uM
2,3,7,8-tetrabromodibenzo-p-dioxin	39064: Affinity on cytosolic Aromatic hydrocarbon receptor (Ah)	ec50	0.0015	uM
2-(1H-indole-3-carbonyl)-N-methyl-1,3-thiazole-4-carboxamide	1907905: Agonist activity at AhR (unknown origin) transfected in human AZ-AHR reporter cells derived from human HepG2 cells incubated for 4 hrs by luciferase reporter gene assay	ec50	0.0016	uM
6-(1H-indole-3-carbonyl)pyridine-2-carbonitrile	1732081: Agonist activity at AHR in human HepG2 cells incubated for 4.5 hrs by Luciferase reporter assay	ec50	0.0020	uM
1,3,7,8-tetrabromodibenzo-p-dioxin	39064: Affinity on cytosolic Aromatic hydrocarbon receptor (Ah)	ec50	0.0020	uM
7-chloro-3,10-diazapentacyclo[10.7.1.02,10.04,9.016,20]icosa-1(19),2,4(9),5,7,12,14,16(20),17-nonaen-11-one	1527837: Displacement of [3H] 3-MC from AhR (unknown origin)	ic50	0.0026	uM
2-(3-hydroxy-1H-indol-2-yl)indol-3-one	1946335: Activation of human AhR expressed in Saccharomyces cerevisiae YCM3 coexpressing ARNT incubated for 18 hrs	ec50	0.0050	uM
benzo[a]pyrene	39218: Concentration to bind to human AhR-modied electrode	ec50	0.0050	uM
1,2,3,7,8-pentabromodibenzo-p-dioxin	39064: Affinity on cytosolic Aromatic hydrocarbon receptor (Ah)	ec50	0.0066	uM
3-phenylbenzo[f]chromen-1-one	1527836: Agonist activity at AhR (unknown origin)	ec50	0.0084	uM
2,3,7,8-tetrachlorodibenzo-p-dioxin	1946335: Activation of human AhR expressed in Saccharomyces cerevisiae YCM3 coexpressing ARNT incubated for 18 hrs	ec50	0.0090	uM
6-bromo-2-(3-bromophenyl)-[1,2,4]triazolo[1,5-a]pyridine	1901915: Agonist activity at AhR in human recombinant HepG2-Lucia AhR cell incubated for 24 hrs by luciferase reporter gene assay	ec50	0.0096	uM
2-bromo-3,7,8-trichlorodibenzo-p-dioxin	39064: Affinity on cytosolic Aromatic hydrocarbon receptor (Ah)	ec50	0.0115	uM
4-(1H-indol-3-ylmethyl)-6H-azepino[4,5-b]indol-5-one	1946334: Agonist activity at AhR (unknown origin)	ec50	0.0120	uM
Tapinarof	2129036: Agonist activity at human AhR by TR-FRET assay	ec50	0.0130	uM

CTD chemical–gene interactions

542 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Tetrachlorodibenzodioxin	decreases sumoylation, decreases expression, increases expression, decreases uptake, increases secretion (+21 more)	246
Benzo(a)pyrene	increases expression, affects binding, increases abundance, increases metabolic processing, increases phosphorylation (+16 more)	75
Methylcholanthrene	affects localization, affects binding, increases response to substance, affects activity, affects cotreatment (+10 more)	32
beta-Naphthoflavone	decreases chemical synthesis, decreases secretion, affects binding, decreases reaction, increases activity (+8 more)	31
Resveratrol	increases expression, affects localization, increases reaction, affects cotreatment, increases activity (+6 more)	27
2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazophenyl)amide	decreases activity, affects cotreatment, increases activity, decreases expression, increases localization (+7 more)	23
alpha-naphthoflavone	decreases reaction, increases phosphorylation, increases expression, decreases response to substance, decreases uptake (+11 more)	22
Estradiol	affects binding, decreases reaction, increases reaction, decreases expression, increases expression (+3 more)	18
Particulate Matter	decreases reaction, increases activity, affects localization, increases abundance, increases expression (+3 more)	15
3,4,5,3’,4’-pentachlorobiphenyl	decreases activity, decreases reaction, affects response to substance, affects binding, increases activity (+4 more)	13
2,3,7,8-tetrachlorodibenzofuran	affects binding, increases activity, decreases reaction, increases reaction, affects response to substance (+1 more)	12
benzyloxycarbonylleucyl-leucyl-leucine aldehyde	affects binding, increases localization, increases ubiquitination, increases expression, increases degradation (+7 more)	12
6-formylindolo(3,2-b)carbazole	decreases expression, increases expression, affects reaction, affects localization, increases reaction (+4 more)	12
Omeprazole	increases reaction, affects localization, affects binding, decreases reaction, increases activity (+5 more)	11
Quercetin	increases activity, affects activity, decreases localization, increases expression, affects reaction (+6 more)	11
2-(1’H-indole-3’-carbonyl)thiazole-4-carboxylic acid methyl ester	affects expression, affects binding, affects cotreatment, decreases expression, decreases reaction (+2 more)	10
Vehicle Emissions	increases abundance, increases secretion, affects reaction, increases activity, affects localization (+5 more)	9
3,4,3’,4’-tetrachlorobiphenyl	increases expression, decreases abundance, decreases reaction, affects binding, increases activity (+1 more)	8
benz(a)anthracene	affects reaction, increases expression, increases activity, increases reaction, affects binding (+1 more)	8
Air Pollutants	affects localization, decreases expression, decreases reaction, increases abundance, increases expression (+2 more)	8
Tobacco Smoke Pollution	affects cotreatment, affects activity, increases activity, affects response to substance, decreases expression (+2 more)	8
kaempferol	increases phosphorylation, affects binding, decreases reaction, increases activity, increases reaction	7
bisphenol A	decreases methylation, increases activity, increases expression, affects binding, increases reaction (+1 more)	7
indirubin	affects binding, increases activity	7
6-methyl-1,3,8-trichlorodibenzofuran	affects binding, decreases reaction, increases localization, affects response to substance, decreases expression (+3 more)	7
3’-methoxy-4’-nitroflavone	decreases activity, affects activity, decreases response to substance, affects reaction, increases expression (+4 more)	7
Dexamethasone	affects localization, affects binding, increases expression, decreases expression, increases reaction (+3 more)	7
Hexachlorobenzene	increases activity, decreases expression, decreases reaction, affects binding, increases phosphorylation (+4 more)	7
Oxygen	decreases stability, decreases reaction, decreases activity, affects reaction, decreases expression (+10 more)	7
Valproic Acid	affects cotreatment, increases expression, affects expression, decreases methylation	7

ChEMBL screening assays

293 unique, capped per target: 225 binding, 58 admet, 7 functional, 3 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1030733	Binding	Activation of AhR expressed in guinea pig cytosolic fractions over expressed with XRE by ELISA based Ah-immunoassay relative to TCDD	Synthesis and biological evaluation of fused thio- and selenopyrans as new indolocarbazole analogues with aryl hydrocarbon receptor affinity. — Bioorg Med Chem
CHEMBL1068662	Functional	Agonist activity at aryl hydrocarbon receptor in human MCF7 cells after 24 hrs CYP1A1-dependent EROD assay	beta-Naphthoflavone analogs as potent and soluble aryl hydrocarbon receptor agonists: improvement of solubility by disruption of molecular planarity. — Bioorg Med Chem
CHEMBL1614450	ADMET	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for activators of the Aryl Hydrocarbon Receptor (AHR). (Class of assay: confirmatory) [Related pubchem assays: 2796 (Primary screen (AHR activators in singl	PubChem BioAssay data set

Cellosaurus cell lines

13 cell lines: 12 cancer cell line, 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B6A7	HepaRG AHR KO	Cancer cell line	Female
CVCL_B7VV	Abcam Raji AHR KO	Cancer cell line	Male
CVCL_B9WD	Abcam THP-1 AHR KO	Cancer cell line	Male
CVCL_C0V1	HepG2 AhR-CYP1A1 clone 4	Cancer cell line	Male
CVCL_C0V2	HepG2 AhR-CYP1A1 clone 9	Cancer cell line	Male
CVCL_C0V3	HepG2 AhR-CYP1A1 clone 10	Cancer cell line	Male
CVCL_C6YE	Abcam PC-3 AHR KO	Cancer cell line	Male
CVCL_D8YX	Ubigene HEK293 AHR KO	Transformed cell line	Female
CVCL_D9XG	Ubigene HeLa AHR KO	Cancer cell line	Female
CVCL_E1CP	Ubigene THP-1 AHR KO	Cancer cell line	Male

Clinical trials (associated diseases)

259 trials via MONDO — disease-level, not drug-specific.

Trial	Phase	Status	Title
NCT00717080	PHASE4	COMPLETED	The Role of Capsular Tension Ring (CTR) in Anterior Capsular Contraction
NCT00000114	PHASE3	COMPLETED	Randomized Trial of Vitamin A and Vitamin E Supplementation for Retinitis Pigmentosa
NCT00000116	PHASE3	COMPLETED	Randomized Trial of DHA for Retinitis Pigmentosa Patients Receiving Vitamin A
NCT00346333	PHASE3	COMPLETED	Clinical Trial of Lutein for Patients With Retinitis Pigmentosa Receiving Vitamin A
NCT01786395	PHASE3	TERMINATED	Phase III Efficacy and Safety Clinical Study of UF-021 for Treatment of Retinitis Pigmentosa
NCT04224207	PHASE3	COMPLETED	Management of Retinitis Pigmentosa by Mesenchymal Stem Cells by Wharton’s Jelly Derived Mesenchymal Stem Cells
NCT04636853	PHASE3	COMPLETED	CB-PRP in Retinitis Pigmentosa and Dry Age-related Macular Degeneration
NCT05537220	PHASE3	ACTIVE_NOT_RECRUITING	Oral N-acetylcysteine for Retinitis Pigmentosa
NCT05800301	PHASE3	COMPLETED	Management of Retinitis Pigmentosa Via Combination of Wharton’s Jelly-derived Mesenchymal Stem Cells and Magnovision
NCT05926583	PHASE3	ACTIVE_NOT_RECRUITING	A Study of AAV5-hRKp.RPGR for the Treatment of Japanese Participants With X-linked Retinitis Pigmentosa
NCT06388200	PHASE3	ACTIVE_NOT_RECRUITING	A Phase 3 Study Of OCU400 Gene Therapy for the Treatment Of Retinitis Pigmentosa
NCT07082855	PHASE3	NOT_YET_RECRUITING	A Multicenter, Randomized, Double-Blind, Controlled Clinical Study of Minocycline for the Treatment of Retinitis Pigmentosa
NCT07290530	PHASE3	NOT_YET_RECRUITING	24-Month Trial of NPI-001 for the Preservation of Photoreceptors in Retinitis Pigmentosa Associated With Usher Syndrome
NCT00100230	PHASE2	COMPLETED	DHA and X-Linked Retinitis Pigmentosa
NCT00447980	PHASE2	COMPLETED	A Study of Encapsulated Cell Technology (ECT) Implant for Participants With Early Stage Retinitis Pigmentosa
NCT00447993	PHASE2	COMPLETED	A Study of Encapsulated Cell Technology (ECT) Implant for Patients With Late Stage Retinitis Pigmentosa
NCT01233609	PHASE2	COMPLETED	Trial of Oral Valproic Acid for Retinitis Pigmentosa
NCT01399515	PHASE2	COMPLETED	Efficacy and Safety of Oral Valproic Acid for Retinitis Pigmentosa
NCT01530659	PHASE2	COMPLETED	Retinal Imaging in CNTF -Releasing Encapsulated Cell Implant Treated Patients for Early-stage Retinitis Pigmentosa
NCT01560715	PHASE2	COMPLETED	Autologous Bone Marrow-Derived Stem Cells Transplantation For Retinitis Pigmentosa
NCT02609165	PHASE2	COMPLETED	Nerve Growth Factor Eye Drops Treatment in Patients With Retinitis Pigmentosa and Cystoid Macular Edema
NCT02661711	PHASE2	COMPLETED	Aflibercept for Macular Oedema With Underlying Retinitis Pigmentosa (AMOUR) Study
NCT02804360	PHASE2	UNKNOWN	Intravitreal Dexamethasone Implant in Retinitis Pigmentosa-related Macular Edema- a Retrospective Study
NCT02837640	PHASE2	UNKNOWN	Studying a Potential Protective Effect of L-Dopa on Retinitis Pigmentosa
NCT03073733	PHASE2	COMPLETED	Safety and Efficacy of Intravitreal Injection of Human Retinal Progenitor Cells in Adults With Retinitis Pigmentosa
NCT04068207	PHASE2	COMPLETED	Minocycline Treatment in Retinitis Pigmentosa
NCT04356716	PHASE2	COMPLETED	Sildenafil for Treatment of Choroidal Ischemia
NCT04604899	PHASE2	COMPLETED	Safety of Repeat Intravitreal Injection of Human Retinal Progenitor Cells (jCell) in Adult Subjects With Retinitis Pigmentosa
NCT04763369	PHASE2	UNKNOWN	Investigation of Therapeutic Efficacy and Safety of UMSCs for the Management of Retinitis Pigmentosa (RP)
NCT04864496	PHASE2	UNKNOWN	Effects of Treatment With N- Acetylcysteine on Visual Outcomes in Patients With Retinitis Pigmentosa
NCT04945772	PHASE2	COMPLETED	Efficacy and Safety of MCO-010 Optogenetic Therapy in Adults With Retinitis Pigmentosa [RESTORE]
NCT05085964	PHASE2	TERMINATED	An Open-Label Extension Study to Evaluate Safety & Tolerability of QR-421a in Subjects With Retinitis Pigmentosa
NCT05392179	PHASE2	COMPLETED	A Study in Subjects With Retinitis Pigmentosa
NCT06627179	PHASE2	RECRUITING	Study to Evaluate Ultevursen in Subjects With Retinitis Pigmentosa (RP) Due to Mutations in Exon 13 of the USH2A Gene
NCT06628947	PHASE2	RECRUITING	A Phase II Study of Intravitreal KIO-301 in Patients With Late-stage Retinitis Pigmentosa
NCT06912633	PHASE2	RECRUITING	Safety of a Single, Intravitreal Injection of 6.0M jCell (Famzeretcel) in Retinitis Pigmentosa (RP)
NCT03763227	PHASE2	COMPLETED	Intravitreal Ranibizumab (Lucentis®) in the Treatment of Non-leaking Macular Cysts in Retinal Dystrophy
NCT00063765	PHASE1	COMPLETED	Evaluation of Safety of Ciliary Neurotrophic Factor Implants in the Eye
NCT00065455	PHASE1	COMPLETED	Investigating the Effect of Vitamin A Supplementation on Retinitis Pigmentosa
NCT00458575	PHASE1	TERMINATED	A Study to Evaluate the Safety of CNTO 2476 in Patients With Advanced Retinitis Pigmentosa