ARNT

Summary

ARNT (aryl hydrocarbon receptor nuclear translocator, HGNC:700) is a protein-coding gene on chromosome 1q21.3, encoding Aryl hydrocarbon receptor nuclear translocator (P27540). Required for activity of the AHR.

This gene encodes a protein containing a basic helix-loop-helix domain and two characteristic PAS domains along with a PAC domain. The encoded protein binds to ligand-bound aryl hydrocarbon receptor and aids in the movement of this complex to the nucleus, where it promotes the expression of genes involved in xenobiotic metabolism. This protein is also a co-factor for transcriptional regulation by hypoxia-inducible factor 1. Chromosomal translocation of this locus with the ETV6 (ets variant 6) gene on chromosome 12 have been described in leukemias. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 405 — RefSeq curated summary.

At a glance

• GWAS associations: 13
• Clinical variants (ClinVar): 115 total
• Druggable target: yes
• Cancer driver (intOGen): loss-of-function (tumor-suppressor-like) across 1 cancer types
• Transcription factor: yes — 73 downstream targets (CollecTRI)
• MANE Select transcript: NM_001668

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:700
Approved symbol	ARNT
Name	aryl hydrocarbon receptor nuclear translocator
Location	1q21.3
Locus type	gene with protein product
Status	Approved
Aliases	HIF-1beta, bHLHe2, ARNT1
Ensembl gene	ENSG00000143437
Ensembl biotype	protein_coding
OMIM	126110
Entrez	405

Gene structure

Transcript identifiers

Ensembl transcripts: 42 — 34 protein_coding, 4 retained_intron, 2 protein_coding_CDS_not_defined, 2 nonsense_mediated_decay

ENST00000354396, ENST00000358595, ENST00000468970, ENST00000471844, ENST00000478972, ENST00000497108, ENST00000504358, ENST00000505755, ENST00000505979, ENST00000510273, ENST00000512296, ENST00000515192, ENST00000904319, ENST00000904320, ENST00000904321, ENST00000904322, ENST00000904323, ENST00000904324, ENST00000904325, ENST00000904326, ENST00000904327, ENST00000904328, ENST00000904329, ENST00000904330, ENST00000904331, ENST00000904332, ENST00000904333, ENST00000904334, ENST00000904335, ENST00000921685, ENST00000921686, ENST00000921687, ENST00000921688, ENST00000921689, ENST00000921690, ENST00000921691, ENST00000921692, ENST00000948856, ENST00000948857, ENST00000948858, ENST00000948859, ENST00000948860

RefSeq mRNA: 8 — MANE Select: NM_001668 NM_001197325, NM_001286035, NM_001286036, NM_001350224, NM_001350225, NM_001350226, NM_001668, NM_178427

CCDS: CCDS65641, CCDS65642, CCDS970, CCDS971

Canonical transcript exons

ENST00000358595 — 22 exons

Exon	Start	End
ENSE00000960030	150836280	150836493
ENSE00001044520	150816788	150816890
ENSE00001044525	150817082	150817202
ENSE00001044548	150816259	150816406
ENSE00001044549	150817361	150817433
ENSE00001151505	150814077	150814239
ENSE00001186051	150826543	150826617
ENSE00001414390	150829093	150829227
ENSE00001417988	150829904	150829980
ENSE00001804030	150823194	150823345
ENSE00001855735	150809713	150812110
ENSE00002062254	150876543	150876599
ENSE00003490670	150813172	150813338
ENSE00003494055	150817920	150818030
ENSE00003501885	150831818	150831903
ENSE00003506098	150858349	150858460
ENSE00003540653	150842424	150842468
ENSE00003564332	150834538	150834640
ENSE00003567352	150852762	150852806
ENSE00003617727	150839441	150839654
ENSE00003624903	150832334	150832399
ENSE00003681606	150846263	150846307

Expression profiles

Bgee: expression breadth ubiquitous, 281 present calls, max score 94.74.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 18.7408 / max 288.8883, expressed in 1806 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
14366	12.1304	1791
14367	6.0539	1666
201728	0.2747	96
14368	0.2525	93
14363	0.0294	5

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
colonic epithelium	UBERON:0000397	94.74	gold quality
calcaneal tendon	UBERON:0003701	93.95	gold quality
sural nerve	UBERON:0015488	93.82	gold quality
endocervix	UBERON:0000458	93.72	gold quality
left ovary	UBERON:0002119	93.44	gold quality
right ovary	UBERON:0002118	93.04	gold quality
mucosa of stomach	UBERON:0001199	92.99	gold quality
tendon	UBERON:0000043	92.75	gold quality
stromal cell of endometrium	CL:0002255	92.74	gold quality
ectocervix	UBERON:0012249	92.49	gold quality
body of uterus	UBERON:0009853	92.48	gold quality
ovary	UBERON:0000992	92.28	gold quality
monocyte	CL:0000576	92.03	gold quality
right coronary artery	UBERON:0001625	91.80	gold quality
popliteal artery	UBERON:0002250	91.72	gold quality
tibial artery	UBERON:0007610	91.71	gold quality
right lung	UBERON:0002167	91.61	gold quality
tendon of biceps brachii	UBERON:0008188	91.61	gold quality
mononuclear cell	CL:0000842	91.43	gold quality
left coronary artery	UBERON:0001626	91.43	gold quality
tibial nerve	UBERON:0001323	91.37	gold quality
leukocyte	CL:0000738	91.30	gold quality
descending thoracic aorta	UBERON:0002345	91.28	gold quality
aorta	UBERON:0000947	91.10	gold quality
adrenal tissue	UBERON:0018303	91.04	gold quality
left uterine tube	UBERON:0001303	90.91	gold quality
vagina	UBERON:0000996	90.88	gold quality
coronary artery	UBERON:0001621	90.87	gold quality
skin of leg	UBERON:0001511	90.73	gold quality
muscle of leg	UBERON:0001383	90.49	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	11.26
E-MTAB-4850	no	270.96
E-CURD-10	no	142.25

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

73 targets.

Target	Regulation
ABCA1
ABCB1	Activation
AHR	Unknown
AHRR	Activation
ALDH3A1	Unknown
ALOX12	Activation
AQP5
ARNT
BHLHE40	Unknown
BNIP3	Activation
BRCA1	Unknown
CA9	Activation
CAT
CCNE1	Repression
CDK2	Repression
CDKN1A
CDKN1B	Unknown
CDKN2B
COMMD1
CRYAB
CTSD	Unknown
CUL2
CYP1A1	Activation
CYP1A2	Unknown
CYP1B1	Activation
CYP21A1P
EGLN2	Unknown
EPO	Activation
ESR1	Unknown
ESR2

JASPAR motifs

Motif	Name	Family
MA0259.1	ARNT::HIF1A	PAS domain factors
MA0259.2	ARNT::HIF1A	PAS domain factors

JASPAR matrix evidence (PMIDs): PMID:16234508

Upstream regulators (CollecTRI, top): AHR, AHRR, ARNT, DBP, E2F2, FOS, HIF1A, MLX, MLXIPL, MYOD1, NFIL3, NPAS1, PHB2, SIM2, SP1

miRNA regulators (miRDB)

126 targeting ARNT, 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-8485	100.00	77.57	4731
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-4476	100.00	68.18	2030
HSA-MIR-6876-5P	100.00	67.68	2126
HSA-MIR-1252-5P	100.00	69.80	2774
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-6127	100.00	66.76	2188
HSA-MIR-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-23B-5P	99.98	66.07	587
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-495-3P	99.96	72.81	4197
HSA-MIR-5688	99.96	73.23	4504
HSA-MIR-4666A-3P	99.96	71.71	3434
HSA-MIR-23A-3P	99.95	74.24	3163
HSA-MIR-23B-3P	99.95	74.24	3163
HSA-MIR-23C	99.95	73.92	3192
HSA-MIR-545-3P	99.95	70.74	2783
HSA-LET-7C-3P	99.95	73.42	2862
HSA-MIR-651-3P	99.94	73.48	5177
HSA-MIR-23A-5P	99.94	65.39	468
HSA-MIR-338-5P	99.92	72.34	2951
HSA-MIR-10527-5P	99.91	72.28	3754
HSA-MIR-9902	99.89	69.15	2250
HSA-MIR-548E-5P	99.89	72.73	4486
HSA-MIR-3140-3P	99.88	68.47	2069

Literature-anchored findings (GeneRIF, showing 40)

• 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)
• 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)
• modification by SUMO-1 chiefly at Lys(245) within the PAS domain of this protein, both in vivo and in vitro (PMID:12354770)
• 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)
• function as potent coactivator of estrogen receptor-dependent transcription (PMID:12754377)
• 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)
• formation of stable protein-DNA complexes by DR/Arnt and HIF-1alpha/Arnt heterodimers with their cognate DNA sequences requires Per/Arnt/Sim A domains (PMID:14638687)
• nucleotide preference of the heterodimers of HLF and Arnt, and of AHR and Arnt (PMID:15190133)
• Studies using a small interfering RNA to down-regulate Arnt protein expression revealed that TCDD-induced G(1) arrest is absolutely dependent on the Arnt protein. (PMID:15492120)
• ER alpha-AHR-ARNT protein-protein interactions mediate estradiol-dependent transrepression of dioxin-inducible gene transcription (PMID:15837795)
• Stat3 is required for both basal and growth signal-induced expression of HIF-1 (PMID:16007214)
• The role of ARNT/HIF1beta and altered gene expression in impaired beta cell function and the pathogenesis of human type 2 diabetes. (PMID:16096055)
• Ainp2 enhances the 3-methylchloranthrene-induced activity in HepG2 cells, suggesting that Ainp2 plays a role in the Arnt-dependent function. (PMID:16111650)
• Phosphorylation of Ser77 within the alternative exon of ARNT has a major influence on the activity of alternatively (Alt) spliced ARNT homodimers, but not an Alt ARNT heterodimer. (PMID:16129408)
• In our cohort of patients, the polymorphism in codon 511 of the ARNT gene is not associated with RM. (PMID:16364012)
• dioxin receptor is silenced by promoter hypermethylation in human acute lymphoblastic leukemia through inhibition of Sp1 binding (PMID:16410262)
• for the bHLH.PAS transcription factors Dioxin Receptor and Arnt, the DR PAS A domain has a role in dimerization and affinity for an atypical E-box DNA sequence (PMID:16520375)
• In hypoxia, HIF-alpha is stabilized and either dimerizes with HIF-beta to form transcriptionally active HIF for a hypoxia response, or it interacts with unrelated proteins, enabling convergence of HIF oxygen sensing with other signaling pathways. (PMID:16554418)
• xenobiotic (TCDD) treatments of breast cancer cells containing reduced levels of BRCA1 cause the transcription factor ARNT to become unstable (PMID:16567799)
• Allele and genotype frequencies of AHR and ARNT polymorphisms were similar between infertile men and controls. (PMID:17559847)
• Overexpression of presenilin-1 increased HIF-1beta, suggesting that HIF is downstream of presenilin (PMID:18174159)
• ARNT variants are unlikely to explain the linkage signal on chromosome 1q, but may alter insulin secretion in nondiabetic subjects (PMID:18366646)
• identified hypoxia inducible factor 1beta (HIF1beta) as a TG2 binding partner (PMID:18375543)
• The downregulation of ETS1 expression with small interfering RNA (siRNA) involves HIF1beta in regulating hypoxia-inducible genes. (PMID:18381358)
• reduced availability of glucose under hypoxia downregulates HIF-1 in part through the inhibition of HIF-1 alpha mRNA (PMID:18762723)
• Hybrids of the bHLH and bZIP protein motifs display different DNA-binding activities in vivo vs. in vitro. (PMID:18949049)
• Curcumin attenuates cytochrome P450 induction in response to TCDD by ROS-dependently degrading AhR and ARNT. (PMID:19018768)
• subtypes of VHL mutations support an intermediate level of HIF-1alpha and HIF-2alpha regulation via a remnant VBC complex. (PMID:19030229)
• crystal structures of the heterodimer formed by the C-terminal PAS domains from the HIF2alpha and ARNT subunits of the HIF2 transcription factor, both in the absence and presence of an artificial ligand. (PMID:19129502)
• identification of ARNT as a CD30-interacting protein that modulated the activity of the RelB subunit of the transcription factor NF-kappaB; findings indicate that ARNT functions in concert with RelB in a CD30-induced negative feedback mechanism (PMID:19131627)
• ARNT plays an important role in EGF-regulated COX-2 gene expression and may thus be related to either a cause or a consequence of tumorigenesis in cervical cancer (PMID:19203995)
• The SUMOylation of both AhRR and Arnt is important for the efficient transcriptional repression activity of the AhRR/Arnt heterodimer (PMID:19251700)
• The results of the present study demonstrate that HIF-1alpha and HIF-1beta enhances expression of VEGF and glucose metabolism-related genes in response to hypoxia in gastric cancer. (PMID:19287200)
• A deficiency of ARNT action in the liver could contribute to the altered metabolic function in humans with type 2 diabetes. (PMID:19416713)
• HIF-1beta availability determines ABCA1 expression and cholesterol efflux in macrophages under hypoxia and may contribute to the interpersonal variability of atherosclerotic lesion progression. (PMID:19828131)
• the expression of ARNT protein is significantly reduced in aryl hydrocarbon receptor interacting protein mutation+ tumors (PMID:19850893)
• the expression of miR-101 is also modulated at different physiological conditions, such as androgen stimulation and HIF-1alpha/HIF-1beta induction. (PMID:20478051)
• These results reveal a novel mechanism by which ARNT acts as a modulator to bridge the c-Jun/Sp1 interaction and plays a role in EGF-mediated gene expression under normoxic conditions. (PMID:20508969)
• Reverse transcriptase-polymerase chain reaction analysis disclosed the existence of a ETV6-ARNT fusion gene in a patient with childhood T lymphoblastic leukemia. (PMID:20804916)
• Cloning and functional analysis of the HIF-1beta promoter identifies a prominent region for interferon (IFN)-gamma-dependent repression. (PMID:21199896)

Cross-species orthologs

7 orthologs

Organism	Symbol	Gene ID
danio_rerio	arnt	ENSDARG00000021855
mus_musculus	Arnt	ENSMUSG00000015522
rattus_norvegicus	Arnt	ENSRNOG00000031174
drosophila_melanogaster	Met	FBGN0002723
drosophila_melanogaster	gce	FBGN0261703
drosophila_melanogaster	tgo	FBGN0264075
caenorhabditis_elegans	aha-1	WBGENE00000095

Paralogs (6): BMAL2 (ENSG00000029153), BMAL1 (ENSG00000133794), CLOCK (ENSG00000134852), PASD1 (ENSG00000166049), NPAS2 (ENSG00000170485), ARNT2 (ENSG00000172379)

Protein

Protein identifiers

Aryl hydrocarbon receptor nuclear translocator — P27540 (reviewed: P27540)

Alternative names: Class E basic helix-loop-helix protein 2, Dioxin receptor, nuclear translocator, Hypoxia-inducible factor 1-beta

All UniProt accessions (3): P27540, A6NGV6, D6RDB3

UniProt curated annotations — full annotation on UniProt →

Function. Required for activity of the AHR. Upon ligand binding, AHR translocates into the nucleus, where it heterodimerizes with ARNT and induces transcription by binding to xenobiotic response elements (XRE). Not required for the ligand-binding subunit to translocate from the cytosol to the nucleus after ligand binding. The complex initiates transcription of genes involved in the regulation of a variety of biological processes, including angiogenesis, hematopoiesis, drug and lipid metabolism, cell motility and immune modulation. The heterodimer binds to core DNA sequence 5’-TACGTG-3’ within the hypoxia response element (HRE) of target gene promoters and functions as a transcriptional regulator of the adaptive response to hypoxia. 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. Monomer. Homodimer only upon binding to a DNA. Efficient DNA binding requires dimerization with another bHLH protein. Interacts with TACC3. Interacts with HIF1A, EPAS1, NPAS1 and NPAS3; forms a heterodimer that binds core DNA sequence 5’-TACGTG-3’ within the hypoxia response element (HRE) of target gene promoters. Forms a heterodimer with AHRR, as well as with other bHLH proteins. Interacts with NOCA7. Interacts with TACC3. Interacts with AHR; 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. Interacts with SIM1 and NPAS4.

Subcellular location. Nucleus.

Isoforms (4)

UniProt ID	Names	Canonical?
P27540-1	1, Long	yes
P27540-2	2, Short
P27540-3	3
P27540-4	4

RefSeq proteins (8): NP_001184254, NP_001272964, NP_001272965, NP_001337153, NP_001337154, NP_001337155, NP_001659, NP_848514 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000014	PAS	Domain
IPR001067	Nuc_translocat	Family
IPR001610	PAC	Repeat
IPR011598	bHLH_dom	Domain
IPR013767	PAS_fold	Domain
IPR035965	PAS-like_dom_sf	Homologous_superfamily
IPR036638	HLH_DNA-bd_sf	Homologous_superfamily
IPR050933	Circadian_TF	Family

Pfam: PF00010, PF00989, PF14598

UniProt features (71 total): helix 14, strand 11, compositionally biased region 8, region of interest 7, mutagenesis site 7, turn 6, domain 4, splice variant 4, sequence variant 4, modified residue 2, initiator methionine 1, chain 1, cross-link 1, sequence conflict 1

Structure

Experimental structures (PDB)

44 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
3F1P	X-RAY DIFFRACTION	1.17
3F1N	X-RAY DIFFRACTION	1.48
2B02	X-RAY DIFFRACTION	1.5
3H82	X-RAY DIFFRACTION	1.5
4GHI	X-RAY DIFFRACTION	1.5
6D0C	X-RAY DIFFRACTION	1.5
4H6J	X-RAY DIFFRACTION	1.52
6X21	X-RAY DIFFRACTION	1.54
9I64	X-RAY DIFFRACTION	1.56
3F1O	X-RAY DIFFRACTION	1.6
4EQ1	X-RAY DIFFRACTION	1.6
6CZW	X-RAY DIFFRACTION	1.6
6D0B	X-RAY DIFFRACTION	1.6
3H7W	X-RAY DIFFRACTION	1.65
4XT2	X-RAY DIFFRACTION	1.7
8CK3	X-RAY DIFFRACTION	1.71
4GS9	X-RAY DIFFRACTION	1.72
5TBM	X-RAY DIFFRACTION	1.85
6D09	X-RAY DIFFRACTION	1.85
5UFP	X-RAY DIFFRACTION	1.9
6X28	X-RAY DIFFRACTION	1.92
6X37	X-RAY DIFFRACTION	1.94
8G4A	X-RAY DIFFRACTION	1.97
6X2H	X-RAY DIFFRACTION	2
6X3D	X-RAY DIFFRACTION	2
8CK4	X-RAY DIFFRACTION	2.29
8CK8	X-RAY DIFFRACTION	2.3
8XSA	X-RAY DIFFRACTION	2.6
8XS7	X-RAY DIFFRACTION	2.77
8XS9	X-RAY DIFFRACTION	2.8

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P27540-F1	56.53	0.21

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 (3): 2, 77, 58

Mutagenesis-validated functional residues (7):

Position	Phenotype
91	diminishes dna interaction.
93	diminishes dna interaction.
94	severely diminishes dna interaction.
98	severely diminishes dna interaction.
99	diminishes dna interaction.
101	severely diminishes dna interaction.
102	severely diminishes dna interaction.

Function

Pathways and Gene Ontology

Reactome pathways

19 pathways

ID	Pathway
R-HSA-1234158	Regulation of gene expression by Hypoxia-inducible Factor
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-9768919	NPAS4 regulates expression of target genes
R-HSA-1234174	Cellular response to hypoxia
R-HSA-1430728	Metabolism
R-HSA-211859	Biological oxidations
R-HSA-211897	Cytochrome P450 - arranged by substrate type
R-HSA-212436	Generic Transcription Pathway
R-HSA-2262752	Cellular responses to stress
R-HSA-400206	Regulation of lipid metabolism by PPARalpha
R-HSA-556833	Metabolism of lipids
R-HSA-73857	RNA Polymerase II Transcription
R-HSA-74160	Gene expression (Transcription)
R-HSA-8953897	Cellular responses to stimuli
R-HSA-9634815	Transcriptional Regulation by NPAS4

MSigDB gene sets: 0 (showing top):

GO Biological Process (18): response to hypoxia (GO:0001666), embryonic placenta development (GO:0001892), positive regulation of endothelial cell proliferation (GO:0001938), regulation of transcription by RNA polymerase II (GO:0006357), positive regulation of vascular endothelial growth factor production (GO:0010575), cell differentiation (GO:0030154), positive regulation of vascular endothelial growth factor receptor signaling pathway (GO:0030949), positive regulation of protein sumoylation (GO:0033235), cellular response to oxidative stress (GO:0034599), positive regulation of erythrocyte differentiation (GO:0045648), positive regulation of glycolytic process (GO:0045821), positive regulation of transcription by RNA polymerase II (GO:0045944), positive regulation of hormone biosynthetic process (GO:0046886), negative regulation of inflammatory response (GO:0050728), regulation of DNA-templated transcription (GO:0006355), intracellular receptor signaling pathway (GO:0030522), positive regulation of DNA-templated transcription (GO:0045893), intestinal epithelial structure maintenance (GO:0060729)

GO Molecular Function (14): RNA polymerase II cis-regulatory region sequence-specific DNA binding (GO:0000978), DNA-binding transcription factor activity, RNA polymerase II-specific (GO:0000981), cis-regulatory region sequence-specific DNA binding (GO:0000987), DNA-binding transcription factor activity (GO:0003700), nuclear receptor activity (GO:0004879), aryl hydrocarbon receptor binding (GO:0017162), protein homodimerization activity (GO:0042803), sequence-specific DNA binding (GO:0043565), protein heterodimerization activity (GO:0046982), RNA polymerase II-specific DNA-binding transcription factor binding (GO:0061629), sequence-specific double-stranded DNA binding (GO:1990837), DNA binding (GO:0003677), protein binding (GO:0005515), protein dimerization activity (GO:0046983)

GO Cellular Component (9): chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), nuclear body (GO:0016604), aryl hydrocarbon receptor complex (GO:0034751), nuclear aryl hydrocarbon receptor complex (GO:0034753), RNA polymerase II transcription regulator complex (GO:0090575), transcription regulator complex (GO:0005667)

Reactome top-level categories

Rollup of top-13 pathways:

Category	Pathways
Cytochrome P450 - arranged by substrate type	2
Phase I - Functionalization of compounds	2
Metabolism	2
Cellular response to hypoxia	1
Regulation of lipid metabolism by PPARalpha	1
Biological oxidations	1
Transcriptional Regulation by NPAS4	1
Cellular responses to stress	1
RNA Polymerase II Transcription	1
Cellular responses to stimuli	1
Metabolism of lipids	1
Gene expression (Transcription)	1
Generic Transcription Pathway	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
regulation of DNA-templated transcription	3
cellular anatomical structure	3
transcription by RNA polymerase II	2
regulation of transcription by RNA polymerase II	2
DNA-templated transcription	2
RNA polymerase II transcription regulatory region sequence-specific DNA binding	2
transcription cis-regulatory region binding	2
protein dimerization activity	2
nuclear protein-containing complex	2
response to stress	1
response to decreased oxygen levels	1
in utero embryonic development	1
placenta development	1
embryonic organ development	1
endothelial cell proliferation	1
regulation of endothelial cell proliferation	1
positive regulation of epithelial cell proliferation	1
positive regulation of cytokine production	1
vascular endothelial growth factor production	1
regulation of vascular endothelial growth factor production	1
cellular developmental process	1
positive regulation of signal transduction	1
regulation of vascular endothelial growth factor receptor signaling pathway	1
vascular endothelial growth factor receptor signaling pathway	1
protein sumoylation	1
regulation of protein sumoylation	1
positive regulation of protein modification by small protein conjugation or removal	1
response to oxidative stress	1
cellular response to chemical stress	1
erythrocyte differentiation	1
positive regulation of myeloid cell differentiation	1
regulation of erythrocyte differentiation	1
glycolytic process	1
regulation of glycolytic process	1
positive regulation of purine nucleotide catabolic process	1
positive regulation of carbohydrate metabolic process	1
positive regulation of ATP metabolic process	1
positive regulation of DNA-templated transcription	1
positive regulation of biosynthetic process	1
positive regulation of hormone metabolic process	1

Protein interactions and networks

STRING

2310 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ARNT	EP300	Q09472	992
ARNT	EPAS1	Q99814	991
ARNT	HIF1A	Q16665	991
ARNT	HIF3A	Q9Y2N7	991
ARNT	EIF5B	O60841	956
ARNT	EGLN3	Q9H6Z9	930
ARNT	EGLN1	Q9GZT9	922
ARNT	VHL	P40337	901
ARNT	ELOC	Q15369	856
ARNT	CYP1A1	P04798	853
ARNT	EGLN2	Q96KS0	834
ARNT	CREBBP	Q92793	830
ARNT	HIF1AN	Q9NWT6	762
ARNT	ELOB	Q15370	746
ARNT	RELB	Q01201	728

IntAct

127 interactions, top by confidence:

A	B	Type	Score
HIF1A	ARNT	psi-mi:“MI:0915”(physical association)	0.940
ARNT	HIF1A	psi-mi:“MI:0407”(direct interaction)	0.940
ARNT	HIF1A	psi-mi:“MI:0915”(physical association)	0.940
HIF1A	ARNT	psi-mi:“MI:0914”(association)	0.940
EPAS1	ARNT	psi-mi:“MI:0407”(direct interaction)	0.890
EPAS1	ARNT	psi-mi:“MI:0915”(physical association)	0.890
ARNT	EPAS1	psi-mi:“MI:0915”(physical association)	0.890
ARNT	EPAS1	psi-mi:“MI:0407”(direct interaction)	0.890
PCCB	PCCA	psi-mi:“MI:0914”(association)	0.770
AHR	ARNT	psi-mi:“MI:0914”(association)	0.740
ARNT	AHR	psi-mi:“MI:0914”(association)	0.740
HIF1A	CBX4	psi-mi:“MI:0914”(association)	0.670
FOXR2	MYC	psi-mi:“MI:0914”(association)	0.530
BCAT1	ARNT	psi-mi:“MI:0914”(association)	0.530
FOXR2	NME2P1	psi-mi:“MI:0914”(association)	0.530
NPAS1	DNAJB5	psi-mi:“MI:0914”(association)	0.530
CIAO3	INPPL1	psi-mi:“MI:0914”(association)	0.530
SLX1A	BACH1	psi-mi:“MI:0914”(association)	0.530
ARNT	HSPA8	psi-mi:“MI:0914”(association)	0.530
BAG2	HGS	psi-mi:“MI:0914”(association)	0.530

BioGRID (457): ARNT (Affinity Capture-Western), ARNT (Affinity Capture-Western), ARNT (Affinity Capture-MS), ARNT (Affinity Capture-MS), ARNT (Affinity Capture-MS), ARNT (Affinity Capture-MS), NCOA1 (Affinity Capture-Western), NCOA1 (Two-hybrid), ARNT (Reconstituted Complex), ARNT (Affinity Capture-MS), ARNT (Affinity Capture-MS), ARNT (Affinity Capture-MS), ARNT (Affinity Capture-MS), ARNT (Affinity Capture-MS), ARNT (Affinity Capture-Western)

ESM2 similar proteins: A0A0J9VT58, A0A0J9VYS2, A0A0J9W3S9, A0A0J9W9G2, A0A0J9WAS0, A0A0J9WVC0, A0A364LYQ6, A1C602, A1DG01, A2QFG8, A3LQV7, A5DF43, A5DRJ2, A8N767, B0D0T8, B0XVV1, B2AR36, B2W978, C4QV17, C4R1K8, C4Y4V1, C5DX31, C5E1J9, C5E2K7, C7YM38, D8Q8R5, O02748, O59746, P19541, P27540, P87233, Q00858, Q01371, Q03571, Q09750, Q0CHR0, Q0U7C8, Q2GSA4, Q2UMM2, Q4PD88

Diamond homologs: A0MLS5, A6NFD8, O00327, O02219, O02748, O08785, O15516, O15945, O61734, O88529, P27540, P41739, P53762, P79832, P90953, P97460, Q2NL18, Q2VPD4, Q5R4T2, Q5RAK8, Q5ZQU2, Q61324, Q6YGZ4, Q6YGZ5, Q78E60, Q7TS99, Q8BGD7, Q8IUM7, Q8QGQ6, Q8QGQ7, Q8WYA1, Q91YA8, Q91YA9, Q91YB0, Q91YB2, Q99743, Q9BE97, Q9DBX7, Q9DG12, Q9EPW1

SIGNOR signaling

17 interactions.

A	Effect	B	Mechanism
CSNK2A1	down-regulates	ARNT	phosphorylation
ARNT	“down-regulates quantity by repression”	CCNE1	“transcriptional regulation”
ARNT	“down-regulates quantity by repression”	CDK2	“transcriptional regulation”
ARNT	“down-regulates quantity by repression”	FOS	“transcriptional regulation”
ARNT	“down-regulates quantity by repression”	JUN	“transcriptional regulation”
ARNT	“up-regulates quantity by expression”	CYP1A1	“transcriptional regulation”
ARNT	“up-regulates quantity by expression”	CA9	“transcriptional regulation”
ARNT	“up-regulates quantity by expression”	CYP1B1	“transcriptional regulation”
ARNT	“form complex”	“HIF-1 complex”	binding
ARNT	“down-regulates quantity by repression”	TH	“transcriptional regulation”
SIM1	“down-regulates activity”	ARNT	binding
SIM1	“up-regulates activity”	ARNT	binding
SIM2	“up-regulates activity”	ARNT	binding
ARNT	“form complex”	AHR-ARNT	binding
ROS	“up-regulates quantity by expression”	ARNT
ARNT	“up-regulates activity”	HIF1A	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 104 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Signaling by WNT	7	11.0×	2e-03
TCF dependent signaling in response to WNT	6	9.9×	6e-03
Interleukin-4 and Interleukin-13 signaling	6	8.7×	6e-03

GO biological processes:

GO term	Partners	Fold	FDR
positive regulation of miRNA transcription	6	18.9×	2e-04
osteoblast differentiation	6	7.9×	1e-02
cellular response to hypoxia	6	7.9×	1e-02
regulation of gene expression	7	6.3×	1e-02
transcription by RNA polymerase II	8	6.1×	7e-03

Disease & clinical

Cancer significance

From intOGen — cancer-driver classification: loss-of-function (tumor-suppressor-like) across 1 cancer types — SCLC.

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	73
Likely benign	2
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

3225 predictions. Top by Δscore:

Variant	Effect	Δscore
1:150813166:TCTTA:T	donor_loss	1.0000
1:150813167:CTTAC:C	donor_loss	1.0000
1:150813168:TTACC:T	donor_loss	1.0000
1:150813169:TACCT:T	donor_loss	1.0000
1:150813170:ACCT:A	donor_loss	1.0000
1:150813171:C:G	donor_loss	1.0000
1:150813334:AGGAG:A	acceptor_gain	1.0000
1:150813335:GGAG:G	acceptor_gain	1.0000
1:150813336:GAG:G	acceptor_gain	1.0000
1:150813336:GAGC:G	acceptor_loss	1.0000
1:150813337:AG:A	acceptor_gain	1.0000
1:150813339:C:CC	acceptor_gain	1.0000
1:150813349:A:T	acceptor_gain	1.0000
1:150814235:ACCTG:A	acceptor_gain	1.0000
1:150814236:CCTGC:C	acceptor_gain	1.0000
1:150814237:CTG:C	acceptor_gain	1.0000
1:150814240:C:CC	acceptor_gain	1.0000
1:150816254:TTTA:T	donor_loss	1.0000
1:150816256:TACC:T	donor_loss	1.0000
1:150816258:CCTG:C	donor_loss	1.0000
1:150816407:C:CC	acceptor_gain	1.0000
1:150817078:ATACC:A	donor_loss	1.0000
1:150817080:A:AC	donor_gain	1.0000
1:150817080:AC:A	donor_gain	1.0000
1:150817080:ACC:A	donor_gain	1.0000
1:150817080:ACCCG:A	donor_gain	1.0000
1:150817081:C:CT	donor_gain	1.0000
1:150817081:CC:C	donor_gain	1.0000
1:150817081:CCC:C	donor_gain	1.0000
1:150817081:CCCG:C	donor_gain	1.0000

AlphaMissense

5183 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:150823211:A:C	C459W	1.000
1:150823213:A:G	C459R	1.000
1:150823244:G:C	N448K	1.000
1:150823244:G:T	N448K	1.000
1:150823250:G:C	F446L	1.000
1:150823250:G:T	F446L	1.000
1:150823251:A:G	F446S	1.000
1:150823252:A:G	F446L	1.000
1:150823256:A:C	F444L	1.000
1:150823256:A:T	F444L	1.000
1:150823258:A:G	F444L	1.000
1:150826613:A:G	L391P	1.000
1:150829124:C:G	R379P	1.000
1:150829135:A:C	F375L	1.000
1:150829135:A:T	F375L	1.000
1:150829137:A:G	F375L	1.000
1:150829160:T:G	H367P	1.000
1:150829163:C:G	R366P	1.000
1:150829164:G:C	R366G	1.000
1:150829166:G:A	S365F	1.000
1:150829166:G:T	S365Y	1.000
1:150829167:A:G	S365P	1.000
1:150829171:G:C	F363L	1.000
1:150829171:G:T	F363L	1.000
1:150829172:A:G	F363S	1.000
1:150829173:A:G	F363L	1.000
1:150829910:T:A	R342S	1.000
1:150829910:T:G	R342S	1.000
1:150829911:C:G	R342T	1.000
1:150829914:C:T	G341D	1.000

dbSNP variants (sampled 300 via entrez): RS1000042944 (1:150828800 T>G), RS1000145063 (1:150874814 T>C), RS1000175450 (1:150862157 T>C), RS1000182714 (1:150811126 G>A,T), RS1000225673 (1:150840214 C>A), RS1000266304 (1:150875142 A>G), RS1000339120 (1:150818594 A>T), RS1000379028 (1:150850114 C>G), RS1000391569 (1:150818292 A>G), RS1000416963 (1:150837074 A>G), RS1000437196 (1:150876616 A>G), RS1000471849 (1:150843550 T>A,C), RS1000527663 (1:150856339 C>T), RS1000538210 (1:150810587 C>T), RS1000549677 (1:150825487 G>C)

Disease associations

OMIM: gene MIM:126110 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

13 associations (top):

Study	Trait	p-value
GCST001266_1	Melanoma	9.000000e-11
GCST001791_8	Urate levels	1.000000e-07
GCST001966_1	Rhegmatogenous retinal detachment	1.000000e-07
GCST003419_2	Congenital left-sided heart lesions	9.000000e-07
GCST004142_27	Melanoma	9.000000e-11
GCST005951_38	Body mass index	4.000000e-09
GCST008529_34	Tea consumption	7.000000e-06
GCST008745_87	Estimated glomerular filtration rate in non-diabetics	4.000000e-13
GCST008747_2	Estimated glomerular filtration rate	1.000000e-29
GCST009602_74	Metabolic syndrome	1.000000e-08
GCST010148_2	Cutaneous squamous cell carcinoma	7.000000e-09
GCST012227_1043	Hip circumference adjusted for BMI	4.000000e-09
GCST90002402_491	Platelet count	8.000000e-09

EFO canonical traits (7, from GWAS)

EFO ID	Trait name
EFO:0004531	urate measurement
EFO:0004340	body mass index
EFO:0010091	tea consumption measurement
EFO:0000195	metabolic syndrome
EFO:1001927	cutaneous squamous cell carcinoma
EFO:0008039	BMI-adjusted hip circumference
EFO:0004309	platelet count

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3885518 (PROTEIN-PROTEIN INTERACTION), CHEMBL5618 (SINGLE PROTEIN)

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

PharmGKB variants

4 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2134688	ARNT		0.00	0
rs2228099	ARNT		0.00	0
rs3215133	ARNT		0.00	0
rs12410394	ARNT, CTXND2		0.00	0

ChEMBL bioactivities

50 potent at pChembl≥5 of 54 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.00	IC50	1	nM	CHEMBL5394054
9.00	IC50	1	nM	CHEMBL5427105
9.00	IC50	1	nM	CHEMBL5417823
8.70	IC50	2	nM	CHEMBL4173075
8.52	IC50	3	nM	CHEMBL5414407
8.40	IC50	4	nM	CHEMBL4639113
8.40	IC50	4	nM	CHEMBL4641092
8.22	IC50	6	nM	CHEMBL5398227
8.22	IC50	6	nM	CHEMBL5440288
8.15	IC50	7	nM	CHEMBL5397307
7.70	IC50	20	nM	CHEMBL5399126
7.60	IC50	25	nM	CHEMBL5417825
7.48	IC50	33	nM	CHEMBL5439202
7.07	IC50	86	nM	CHEMBL5439150
7.05	IC50	90	nM	CHEMBL2311967
7.00	IC50	100	nM	CHEMBL2311933
6.96	IC50	110	nM	CHEMBL5433232
6.92	IC50	120	nM	CHEMBL2311932
6.92	IC50	120	nM	CHEMBL5404562
6.77	IC50	170	nM	CHEMBL2311966
6.75	IC50	180	nM	CHEMBL2311959
6.52	IC50	300	nM	CHEMBL5431351
6.48	IC50	330	nM	CHEMBL2311947
6.40	IC50	400	nM	CHEMBL2311968
6.37	IC50	430	nM	CHEMBL2311930
6.36	IC50	440	nM	CHEMBL5420728
6.34	IC50	460	nM	CHEMBL2311960
6.30	IC50	500	nM	CHEMBL2311951
6.18	IC50	660	nM	CHEMBL5395791
6.12	IC50	760	nM	CHEMBL2311965
5.96	IC50	1100	nM	CHEMBL5404788
5.85	IC50	1400	nM	CHEMBL5412636
5.85	IC50	1400	nM	CHEMBL5433224
5.80	IC50	1600	nM	CHEMBL5428447
5.80	IC50	1600	nM	CHEMBL5395720
5.70	IC50	2000	nM	CHEMBL2311931
5.70	IC50	2000	nM	CHEMBL2311949
5.70	IC50	2000	nM	CHEMBL5439117
5.68	IC50	2100	nM	CHEMBL2311962
5.64	IC50	2300	nM	CHEMBL5411078
5.55	IC50	2800	nM	CHEMBL2311961
5.54	IC50	2900	nM	CHEMBL5423909
5.41	IC50	3900	nM	CHEMBL5412171
5.39	IC50	4100	nM	CHEMBL5393977
5.38	IC50	4200	nM	CHEMBL5415217
5.35	IC50	4500	nM	CHEMBL5437026
5.32	IC50	4800	nM	CHEMBL5419647
5.16	IC50	6900	nM	CHEMBL5404293
5.07	IC50	8500	nM	CHEMBL5394506
5.00	IC50	1e+04	nM	CHEMBL5439050

PubChem BioAssay actives

51 with measured affinity, of 142 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
3-[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-1-yl]-5-fluorobenzonitrile	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0010	uM
(4S)-1-(3-chloro-5-fluorophenyl)-5,5-difluoro-3-methylsulfonyl-6,7-dihydro-4H-2-benzothiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0010	uM
3-chloro-5-[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-6,7-dihydro-4H-2-benzothiophen-1-yl]benzonitrile	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0010	uM
3-[[(1S)-2,2-difluoro-1-hydroxy-7-methylsulfonyl-1,3-dihydroinden-4-yl]oxy]-5-fluorobenzonitrile	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0020	uM
(4S)-1-(3-chloro-5-fluorophenyl)-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0030	uM
(4S)-1-(3,5-difluorophenyl)-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0040	uM
3-chloro-5-[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-1-yl]benzonitrile	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0040	uM
(4S,5R)-1-(3-chloro-5-fluorophenyl)-5-fluoro-3-methylsulfonyl-5,6-dihydro-4H-cyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0060	uM
3-[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-6,7-dihydro-4H-2-benzothiophen-1-yl]-5-fluorobenzonitrile	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0060	uM
(4S)-1-(3,4-difluorophenyl)-5,5-difluoro-3-methylsulfonyl-6,7-dihydro-4H-2-benzothiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0070	uM
(4S)-1-(3,4-difluorophenyl)-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0200	uM
3-[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-1-yl]benzonitrile	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0250	uM
(4S)-1-(3,5-difluorophenyl)-5,5-difluoro-3-methylsulfonyl-6,7-dihydro-4H-2-benzothiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0330	uM
3-chloro-5-[[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-1-yl]oxy]benzonitrile	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.0860	uM
N-[4-chloro-3-(trifluoromethyl)phenyl]-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	0.0900	uM
N-(3-chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	0.1000	uM
(4S)-5,5-difluoro-1-(4-fluorophenyl)-3-methylsulfonyl-6,7-dihydro-4H-2-benzothiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.1100	uM
(4S)-1-(3,5-difluorophenoxy)-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.1200	uM
N-(3,4-dichlorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	0.1200	uM
N-(3-chloro-4-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	0.1700	uM
N-(3-chlorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	0.1800	uM
3-[[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-1-yl]oxy]-5-fluorobenzonitrile	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.3000	uM
N-[(2-chloro-4-fluorophenyl)methyl]-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	0.3300	uM
N-(4-chloro-3-nitrophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	0.4000	uM
N-[3-fluoro-5-(trifluoromethyl)phenyl]-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	0.4300	uM
(4S)-5,5-difluoro-1-(4-fluorophenyl)-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.4400	uM
4-nitro-N-[3-(trifluoromethyl)phenyl]-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	0.4600	uM
N-[[4-fluoro-2-(trifluoromethyl)phenyl]methyl]-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	0.5000	uM
(4S,5S)-1-(3-chloro-5-fluorophenyl)-5-fluoro-3-methylsulfonyl-5,6-dihydro-4H-cyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	0.6600	uM
N-(3-chloro-2-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	0.7600	uM
(4S)-1-cyclohexyloxy-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	1.0000	uM
(4S)-1-(2,2-dimethylpropoxy)-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	1.1000	uM
(4S)-1-cyclobutyloxy-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	1.4000	uM
(4S)-5,5-difluoro-1-(2-methylpropoxy)-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	1.4000	uM
(4S)-1-(2,2-difluoroethoxy)-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	1.6000	uM
(4S)-5,5-difluoro-1-(2-methylbutoxy)-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	1.6000	uM
(4S)-5,5-difluoro-3-methylsulfonyl-1-[(2S)-3,3,3-trifluoro-2-methylpropoxy]-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	2.0000	uM
N-[(3-chloro-5-fluorophenyl)methyl]-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	2.0000	uM
N-(3,5-difluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	2.0000	uM
N-(3-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	2.1000	uM
(4S)-5,5-difluoro-3-methylsulfonyl-1-(3,3,3-trifluoro-2-methylpropoxy)-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	2.3000	uM
4-nitro-N-(3-nitrophenyl)-2,1,3-benzoxadiazol-5-amine	723543: Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	ic50	2.8000	uM
(4S)-5,5-difluoro-3-methylsulfonyl-1-(2,2,2-trifluoroethoxy)-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	2.9000	uM
(4S)-5,5-difluoro-1-(3-fluorophenoxy)-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	3.9000	uM
(4S)-5,5-difluoro-3-methylsulfonyl-1-(3,3,3-trifluoropropoxy)-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	4.1000	uM
(4S)-5,5-difluoro-3-methylsulfonyl-1-propoxy-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	4.2000	uM
(4S)-5,5-difluoro-3-methylsulfonyl-1-[(2R)-3,3,3-trifluoro-2-methylpropoxy]-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	4.5000	uM
(4S)-1-(cyclopropylmethoxy)-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	4.8000	uM
(4S)-1-(2,2-difluoropropoxy)-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	6.9000	uM
(4S)-1-[(3,3-difluorocyclobutyl)methoxy]-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol	1975371: Inhibition of human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged HIF-2alpha PAS-B domain (240 to 350 residues)/human recombinant N-terminal His6Gb1-TEV-GEFKGL-tagged and C-terminal FLAG-E362R-tagged ARNT PAS-B domain (356 to 470 residues) interaction preincubated for 15 mins at 23 degreeC and measured after 240 mins by Alphascreen analysis	ic50	8.5000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Tetrachlorodibenzodioxin	affects cotreatment, affects localization, decreases reaction, increases reaction, decreases expression (+5 more)	39
Benzo(a)pyrene	increases reaction, increases methylation, affects binding, decreases response to substance, affects reaction (+9 more)	13
cobaltous chloride	affects localization, affects reaction, decreases reaction, increases expression, increases reaction (+1 more)	8
Oxygen	increases activity, decreases activity, decreases reaction, decreases response to substance, affects reaction (+3 more)	7
Estradiol	decreases expression, increases expression, increases activity, affects binding, decreases reaction (+3 more)	6
Resveratrol	affects binding, decreases reaction, increases reaction, increases localization	4
Hydrogen Peroxide	decreases reaction, increases expression, affects cotreatment, decreases expression	4
Methylcholanthrene	decreases response to substance, increases reaction, increases expression, increases localization, affects binding	4
Valproic Acid	affects expression, decreases expression, decreases methylation	4
3,4,3’,4’-tetrachlorobiphenyl	affects binding, increases reaction, increases activity, decreases reaction	3
Curcumin	decreases expression, increases ubiquitination, decreases reaction, increases degradation	3
Ozone	increases abundance, affects cotreatment, decreases expression, increases expression	3
Tobacco Smoke Pollution	affects expression, decreases expression	3
Aflatoxin B1	increases methylation, affects reaction, increases phosphorylation, affects response to substance, affects localization (+1 more)	3
beta-Naphthoflavone	affects binding, decreases reaction, increases activity, increases reaction	3
kaempferol	affects binding, decreases reaction, increases reaction, increases phosphorylation	2
alpha-naphthoflavone	affects binding, increases activity, decreases reaction, increases expression	2
2,3,7,8-tetrachlorodibenzofuran	increases activity, affects binding, increases reaction	2
potassium chromate(VI)	affects localization, affects cotreatment, decreases expression	2
butylbenzyl phthalate	decreases reaction, increases expression, affects binding, affects localization, increases reaction	2
2,3,4,7,8-pentachlorodibenzofuran	affects binding, increases reaction, increases activity	2
methacrylaldehyde	affects cotreatment, decreases expression, increases expression, increases abundance	2
epigallocatechin gallate	decreases reaction, increases phosphorylation, affects cotreatment, decreases expression	2
2-tert-butyl-4-quinone	affects binding, affects reaction, increases reaction	2
benzyloxycarbonylleucyl-leucyl-leucine aldehyde	decreases reaction, increases degradation, decreases expression	2
6-formylindolo(3,2-b)carbazole	increases localization, affects reaction, decreases expression, increases reaction	2
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	decreases reaction, increases expression, affects cotreatment, decreases expression	2
2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazophenyl)amide	increases expression, decreases reaction	2
6,2’,4’-trimethoxyflavone	affects binding, decreases reaction	2
Acrolein	increases expression, increases abundance, affects cotreatment, decreases expression	2

ChEMBL screening assays

16 unique, capped per target: 16 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2319602	Binding	Inhibition of GST-tagged PAS-B domain of HIF-2alpha-Flag-tagged PAS-B domain of ARNT heterodimerization (unknown origin) by luminescence proximity assay	Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor. — J Med Chem

Cellosaurus cell lines

6 cell lines: 6 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_4010	vT{2}	Cancer cell line	Female
CVCL_B8BH	Abcam HCT 116 ARNT KO	Cancer cell line	Male
CVCL_B8SL	Abcam MCF-7 ARNT KO	Cancer cell line	Female
CVCL_B9DK	Abcam A-549 ARNT KO	Cancer cell line	Male
CVCL_KZ74	PathHunter U2OS AHR Protein Interaction	Cancer cell line	Female
CVCL_XL52	HAP1 ARNT (-)	Cancer cell line	Male

Clinical trials (associated diseases)

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