HK3

Summary

HK3 (hexokinase 3, HGNC:4925) is a protein-coding gene on chromosome 5q35.2, encoding Hexokinase-3 (P52790). Catalyzes the phosphorylation of hexose, such as D-glucose and D-fructose, to hexose 6-phosphate (D-glucose 6-phosphate and D-fructose 6-phosphate, respectively).

Hexokinases phosphorylate glucose to produce glucose-6-phosphate, the first step in most glucose metabolism pathways. This gene encodes hexokinase 3. Similar to hexokinases 1 and 2, this allosteric enzyme is inhibited by its product glucose-6-phosphate.

Source: NCBI Gene 3101 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 234 total — 1 pathogenic
• Druggable target: yes
• MANE Select transcript: NM_002115

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4925
Approved symbol	HK3
Name	hexokinase 3
Location	5q35.2
Locus type	gene with protein product
Status	Approved
Aliases	HKIII
Ensembl gene	ENSG00000160883
Ensembl biotype	protein_coding
OMIM	142570
Entrez	3101

Gene structure

Transcript identifiers

Ensembl transcripts: 15 — 11 protein_coding, 2 nonsense_mediated_decay, 2 retained_intron

ENST00000292432, ENST00000504910, ENST00000506834, ENST00000509717, ENST00000514058, ENST00000514666, ENST00000874508, ENST00000970948, ENST00000970949, ENST00000970950, ENST00000970951, ENST00000970952, ENST00000970953, ENST00000970954, ENST00000970955

RefSeq mRNA: 1 — MANE Select: NM_002115 NM_002115

CCDS: CCDS4407

Canonical transcript exons

ENST00000292432 — 19 exons

Exon	Start	End
ENSE00001055181	176889645	176889744
ENSE00001055207	176891388	176891550
ENSE00001158893	176888332	176888565
ENSE00001158898	176888709	176888864
ENSE00001158903	176889381	176889564
ENSE00001158929	176891037	176891191
ENSE00001325170	176880869	176881217
ENSE00001330253	176896064	176896185
ENSE00001516223	176899267	176899346
ENSE00003541734	176887451	176887746
ENSE00003550601	176890635	176890730
ENSE00003562836	176881692	176881847
ENSE00003635525	176890822	176890941
ENSE00003636275	176887201	176887337
ENSE00003636771	176881944	176882127
ENSE00003660955	176881302	176881535
ENSE00003669470	176883770	176883869
ENSE00003687167	176887002	176887121
ENSE00003694543	176884039	176884134

Expression profiles

Bgee: expression breadth ubiquitous, 176 present calls, max score 98.60.

FANTOM5 (CAGE): breadth broad, TPM avg 7.3204 / max 454.5905, expressed in 282 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
65053	6.3032	275
65052	1.0172	184

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
monocyte	CL:0000576	98.60	gold quality
granulocyte	CL:0000094	98.46	gold quality
mononuclear cell	CL:0000842	98.39	gold quality
leukocyte	CL:0000738	98.22	gold quality
spleen	UBERON:0002106	95.80	gold quality
bone marrow cell	CL:0002092	95.18	gold quality
blood	UBERON:0000178	94.79	gold quality
bone marrow	UBERON:0002371	94.50	gold quality
upper lobe of left lung	UBERON:0008952	91.80	gold quality
trabecular bone tissue	UBERON:0002483	91.58	gold quality
right lung	UBERON:0002167	91.00	gold quality
upper lobe of lung	UBERON:0008948	90.32	gold quality
right adrenal gland cortex	UBERON:0035827	84.60	gold quality
vermiform appendix	UBERON:0001154	84.55	gold quality
right adrenal gland	UBERON:0001233	83.72	gold quality
omental fat pad	UBERON:0010414	82.74	gold quality
peritoneum	UBERON:0002358	82.62	gold quality
adipose tissue of abdominal region	UBERON:0007808	82.07	gold quality
lung	UBERON:0002048	81.77	gold quality
left uterine tube	UBERON:0001303	81.70	gold quality
amniotic fluid	UBERON:0000173	81.69	gold quality
left adrenal gland	UBERON:0001234	80.76	gold quality
left adrenal gland cortex	UBERON:0035825	80.64	gold quality
right lobe of liver	UBERON:0001114	79.54	gold quality
apex of heart	UBERON:0002098	79.36	gold quality
adrenal cortex	UBERON:0001235	78.89	gold quality
mucosa of stomach	UBERON:0001199	78.78	gold quality
left coronary artery	UBERON:0001626	78.53	gold quality
right atrium auricular region	UBERON:0006631	78.27	gold quality
right coronary artery	UBERON:0001625	78.08	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-MTAB-9067	yes	941.92
E-MTAB-6678	yes	26.98
E-ANND-3	yes	16.47
E-MTAB-9801	yes	7.76

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CEBPA, KLF5, RARA

miRNA regulators (miRDB)

14 targeting HK3, 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-190A-3P	100.00	80.35	5520
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-137-3P	99.87	74.74	2401
HSA-MIR-4639-5P	99.81	67.37	1028
HSA-MIR-4441	99.49	66.56	3216
HSA-MIR-942-5P	99.41	68.40	1977
HSA-MIR-4505	99.27	67.81	2678
HSA-MIR-5787	99.22	67.86	2628
HSA-MIR-4270	99.02	66.26	1987
HSA-MIR-3922-5P	98.77	66.53	1059
HSA-MIR-4518	98.12	66.82	1030
HSA-MIR-4483	98.09	64.12	1642
HSA-MIR-1266-5P	97.71	66.92	1052

Literature-anchored findings (GeneRIF, showing 13)

• Data demonstrated that in addition to galectin-3, HK III and cyclin A profiles could be important biomarkers in predicting malignancy in follicular thyroid nodules. (PMID:17868400)
• The expression pattern of HK3 is reported in newly diagnosed esophageal adenocarcinoma by means of immunohistochemistry. (PMID:19554504)
• Data show that HKIII exerts protective effects against oxidative stress, perhaps by increasing ATP levels, reducing oxidant-induced ROS production, preserving mitochondrial membrane potential, and increasing mitochondrial biogenesis. (PMID:21072205)
• HK3 is: (1) directly activated by PU.1, (2) repressed by PML-RARA, and (3) functionally involved in neutrophil differentiation and cell viability of acute promyelocytic leukemia cells. (PMID:22498738)
• Altogether, our data provide an explanation for low HK3 and KLF5 expression in particular AML subtype and establish these genes as novel CEBPA targets during neutrophil differentiation. (PMID:24584857)
• Through glycolysis and arachidonic acid metabolism, HK3 and PTGS2 might play important roles in pediatric ALL and its prognosis, and thus, might be potential targets for therapeutic intervention to suppress pediatric ALL. (PMID:25172542)
• The transport of glucose across the cell membrane by glucose transporters (GLUTs) and intracellular phosphorylation by hexokinases (HKs) are the initial steps of the glycolytic pathway. (PMID:25766729)
• HK1 and HK2 expression alterations were detected, that could be explained by common deregulation mechanisms of these genes in colorectal tumors. The HK3 expression level was significantly increased in 60% of samples. (PMID:26855992)
• HK3 expression is significantly upregulated in human masticatory mucosa during wound healing (PMID:28005267)
• Upregulation of HK3 is associated with EMT in CRC and may be a crucial metabolic adaptation for rapid proliferation, survival, and metastases of CRC cells (PMID:29504907)
• Hexokinase 3 dysfunction promotes tumorigenesis and immune escape by upregulating monocyte/macrophage infiltration into the clear cell renal cell carcinoma microenvironment. (PMID:34239350)
• Hexokinase 3 enhances myeloid cell survival via non-glycolytic functions. (PMID:35538058)
• Glioma hexokinase 3 positively correlates with malignancy and macrophage infiltration. (PMID:38687460)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Hk3	ENSMUSG00000025877
rattus_norvegicus	Hk3	ENSRNOG00000026235

Paralogs (4): GCK (ENSG00000106633), HKDC1 (ENSG00000156510), HK1 (ENSG00000156515), HK2 (ENSG00000159399)

Protein

Protein identifiers

Hexokinase-3 — P52790 (reviewed: P52790)

Alternative names: Hexokinase type III, Hexokinase-C

All UniProt accessions (4): P52790, H0Y8U9, H0Y9N6, H0YAG4

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes the phosphorylation of hexose, such as D-glucose and D-fructose, to hexose 6-phosphate (D-glucose 6-phosphate and D-fructose 6-phosphate, respectively). Mediates the initial step of glycolysis by catalyzing phosphorylation of D-glucose to D-glucose 6-phosphate.

Activity regulation. Hexokinase is an allosteric enzyme inhibited by its product D-glucose 6-phosphate.

Domain organisation. The N- and C-terminal halves of this hexokinase contain a hexokinase domain. The catalytic activity is associated with the C-terminus while regulatory function is associated with the N-terminus.

Pathway. Carbohydrate metabolism; hexose metabolism. Carbohydrate degradation; glycolysis; D-glyceraldehyde 3-phosphate and glycerone phosphate from D-glucose: step 1/4.

Similarity. Belongs to the hexokinase family.

RefSeq proteins (1): NP_002106* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001312	Hexokinase	Family
IPR019807	Hexokinase_BS	Binding_site
IPR022672	Hexokinase_N	Domain
IPR022673	Hexokinase_C	Domain
IPR043129	ATPase_NBD	Homologous_superfamily

Pfam: PF00349, PF03727

Enzyme classification (BRENDA):

• EC 2.7.1.1 — hexokinase (BRENDA: 77 organisms, 225 substrates, 336 inhibitors, 483 Km, 134 kcat entries)

Substrate kinetics (BRENDA)

21 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	—	184
D-GLUCOSE	0.003–45	112
D-FRUCTOSE	0.025–1510	46
D-MANNOSE	0.014–25.41	36
2-DEOXY-D-GLUCOSE	0.033–19.2	24
D-GLUCOSAMINE	0.06–2	12
UTP	0.288–30	7
ITP	1.9–16.6	6
CTP	0.52–5	5
GTP	0.231–0.788	4
N-ACETYL-D-GLUCOSAMINE	0.32–41.6	2
1,5-ANHYDRO-D-GLUCITOL	20	1
1-THIO-D-GLUCOSE	5	1
2-DEOXY-2-FLUORO-D-GLUCOSE	0.2	1
2-DEOXYGLUCOSE	18	1

Catalyzed reactions (Rhea), 3 shown:

• D-fructose + ATP = D-fructose 6-phosphate + ADP + H(+) (RHEA:16125)
• D-glucose + ATP = D-glucose 6-phosphate + ADP + H(+) (RHEA:17825)
• a D-hexose + ATP = a D-hexose 6-phosphate + ADP + H(+) (RHEA:22740)

UniProt features (89 total): binding site 28, helix 20, sequence conflict 19, strand 8, region of interest 5, sequence variant 3, domain 2, turn 2, chain 1, compositionally biased region 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
3HM8	X-RAY DIFFRACTION	2.8

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P52790-F1	90.50	0.73

Functional residue map

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

Ligand- & substrate-binding residues (28): 95–102; 168; 185–186; 221–222; 222; 245; 248; 273; 304–307; 426–428; 438–439; 542–547 …

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-6798695	Neutrophil degranulation
R-HSA-70171	Glycolysis

MSigDB gene sets: 226 (showing top): GOBP_NUCLEOSIDE_DIPHOSPHATE_METABOLIC_PROCESS, REACTOME_INNATE_IMMUNE_SYSTEM, GOCC_SECRETORY_GRANULE, MODULE_45, MODULE_64, GOBP_CARBOHYDRATE_DERIVATIVE_CATABOLIC_PROCESS, GOBP_MONOSACCHARIDE_CATABOLIC_PROCESS, GOBP_CARBOHYDRATE_PHOSPHORYLATION, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, MODULE_16, KEGG_GLYCOLYSIS_GLUCONEOGENESIS, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_CARBOHYDRATE_DERIVATIVE_METABOLIC_PROCESS, GOBP_GLUCOSE_6_PHOSPHATE_METABOLIC_PROCESS, GOBP_NUCLEOBASE_CONTAINING_SMALL_MOLECULE_METABOLIC_PROCESS

GO Biological Process (11): intracellular glucose homeostasis (GO:0001678), fructose 6-phosphate metabolic process (GO:0006002), glucose metabolic process (GO:0006006), glycolytic process (GO:0006096), glucose 6-phosphate metabolic process (GO:0051156), canonical glycolysis (GO:0061621), carbohydrate metabolic process (GO:0005975), hexose metabolic process (GO:0019318), organophosphate metabolic process (GO:0019637), carbohydrate phosphorylation (GO:0046835), carbohydrate derivative metabolic process (GO:1901135)

GO Molecular Function (12): glucokinase activity (GO:0004340), hexokinase activity (GO:0004396), ATP binding (GO:0005524), D-glucose binding (GO:0005536), fructokinase activity (GO:0008865), mannokinase activity (GO:0019158), nucleotide binding (GO:0000166), catalytic activity (GO:0003824), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740), phosphotransferase activity, alcohol group as acceptor (GO:0016773)

GO Cellular Component (5): extracellular region (GO:0005576), mitochondrion (GO:0005739), cytosol (GO:0005829), secretory granule lumen (GO:0034774), ficolin-1-rich granule lumen (GO:1904813)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Innate Immune System	1
Glucose metabolism	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
hexokinase activity	3
organophosphate metabolic process	2
carbohydrate derivative metabolic process	2
transferase activity, transferring phosphorus-containing groups	2
cellular anatomical structure	2
cytoplasm	2
glucose homeostasis	1
intracellular chemical homeostasis	1
hexose metabolic process	1
phosphoglycerate kinase activity	1
phosphoglycerate mutase activity	1
phosphopyruvate hydratase activity	1
pyruvate kinase activity	1
pyruvate metabolic process	1
generation of precursor metabolites and energy	1
aerobic respiration	1
carbohydrate catabolic process	1
pyridine nucleotide catabolic process	1
glyceraldehyde-3-phosphate dehydrogenase [NAD(P)+] (phosphorylating) activity	1
ADP catabolic process	1
ATP metabolic process	1
nicotinamide nucleotide metabolic process	1
glucokinase activity	1
glyceraldehyde-3-phosphate dehydrogenase (NAD+) (phosphorylating) activity	1
glucose catabolic process	1
glycolytic process through glucose-6-phosphate	1
primary metabolic process	1
monosaccharide metabolic process	1
phosphorus metabolic process	1
carbohydrate metabolic process	1
phosphorylation	1
metabolic process	1
glucose 6-phosphate metabolic process	1
phosphotransferase activity, alcohol group as acceptor	1
carbohydrate kinase activity	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
monosaccharide binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1

Protein interactions and networks

STRING

1886 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
HK3	G6PD	P11413	628
HK3	H6PD	O95479	593
HK3	PFKL	P17858	570
HK3	PFKM	P08237	532
HK3	PKM	P14618	531
HK3	PFKP	Q01813	516
HK3	GPI	P06744	508
HK3	G6PC3	Q9BUM1	507
HK3	G6PC1	P35575	506
HK3	PKLR	P11973	492
HK3	PFKFB3	Q16875	490
HK3	SYCP2L	Q5T4T6	479
HK3	TREH	O43280	449
HK3	G6PC2	Q9NQR9	445
HK3	PGD	P52209	435

IntAct

67 interactions, top by confidence:

A	B	Type	Score
HK3	MEOX2	psi-mi:“MI:0915”(physical association)	0.560
HK3	APBB2	psi-mi:“MI:0915”(physical association)	0.560
HK3	DNM2	psi-mi:“MI:0915”(physical association)	0.560
HK3	ATN1	psi-mi:“MI:0915”(physical association)	0.560
HK3		psi-mi:“MI:0915”(physical association)	0.560
HK3	PRPS1	psi-mi:“MI:0915”(physical association)	0.560
KLK6	HK3	psi-mi:“MI:0915”(physical association)	0.560
HK3	WFS1	psi-mi:“MI:0915”(physical association)	0.560
HK3	CCT5	psi-mi:“MI:0915”(physical association)	0.560
RNF11	HK3	psi-mi:“MI:0915”(physical association)	0.560
HTT	HK3	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (43): HK3 (Affinity Capture-MS), HK3 (Affinity Capture-MS), HK3 (Affinity Capture-MS), HK3 (Affinity Capture-MS), HK3 (Affinity Capture-MS), HKDC1 (Affinity Capture-MS), HK3 (Affinity Capture-MS), HK3 (Affinity Capture-MS), HK3 (Affinity Capture-MS), HK2 (Affinity Capture-MS), HK3 (Affinity Capture-MS), HK1 (Affinity Capture-MS), HK3 (Affinity Capture-MS), HK3 (Affinity Capture-MS), HK3 (Two-hybrid)

ESM2 similar proteins: A0A0K0JFP3, A2PYL6, A2PYL7, A2PYL8, O08528, O64390, P05708, P17710, P17712, P19367, P27595, P27881, P27926, P33284, P35557, P50506, P50521, P52789, P52790, P52792, P80581, P83776, P93834, Q04409, Q09756, Q1W674, Q1WM15, Q1WM16, Q26609, Q2KNB4, Q2KNB7, Q2KNB9, Q2TB90, Q3TRM8, Q42525, Q5RC71, Q5W676, Q69TF4, Q6CUZ3, Q6Q8A5

Diamond homologs: A0A0K0JFP3, A2PYL6, A2PYL7, A2PYL8, O08528, O64390, P04806, P04807, P05708, P17709, P17710, P17712, P19367, P27595, P27881, P27926, P33284, P35557, P50506, P52789, P52790, P52792, P80581, P83776, P93834, Q04409, Q09756, Q1W674, Q1WM15, Q1WM16, Q26609, Q2KNB4, Q2KNB5, Q2KNB7, Q2KNB9, Q2TB90, Q3TRM8, Q42525, Q56XE8, Q5RC71

SIGNOR signaling

2 interactions.

A	Effect	B	Mechanism
HK3	“up-regulates quantity”	“alpha-D-glucose 6-phosphate(2-)”	“chemical modification”
HK3	“down-regulates quantity”	α-D-glucose	“chemical modification”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	193
Likely benign	20
Benign	4

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
1703528	GRCh37/hg19 5q32-35.3(chr5:149010383-180719789)	Pathogenic

SpliceAI

0 predictions. Top by Δscore:

AlphaMissense

5963 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
5:176883835:T:A	D663V	1.000
5:176883835:T:G	D663A	1.000
5:176883835:T:C	D663G	0.999
5:176883836:C:G	D663H	0.999
5:176883837:A:C	N662K	0.999
5:176883837:A:T	N662K	0.999
5:176884119:A:G	W625R	0.999
5:176884119:A:T	W625R	0.999
5:176887029:G:C	F610L	0.999
5:176887029:G:T	F610L	0.999
5:176887031:A:G	F610L	0.999
5:176887042:A:G	F606S	0.999
5:176883827:C:A	G666W	0.998
5:176883834:G:C	D663E	0.998
5:176883834:G:T	D663E	0.998
5:176883838:T:A	N662I	0.998
5:176884064:A:G	L643S	0.998
5:176884105:G:C	F629L	0.998
5:176884105:G:T	F629L	0.998
5:176884107:A:G	F629L	0.998
5:176884111:C:A	K627N	0.998
5:176884111:C:G	K627N	0.998
5:176884117:C:A	W625C	0.998
5:176884117:C:G	W625C	0.998
5:176887035:G:C	F608L	0.998
5:176887035:G:T	F608L	0.998
5:176887037:A:G	F608L	0.998
5:176887316:A:G	L541P	0.998
5:176881129:C:G	G906R	0.997
5:176883836:C:A	D663Y	0.997

dbSNP variants (sampled 300 via entrez): RS1000053364 (5:176896873 G>A), RS1000118772 (5:176890417 T>A,C), RS1000567799 (5:176892016 G>A), RS1000637707 (5:176883455 C>G), RS1000693156 (5:176886895 C>T), RS1000939071 (5:176898251 T>G), RS1001083447 (5:176899260 T>C), RS1001144198 (5:176883854 C>G,T), RS1001522133 (5:176891724 C>T), RS1001570941 (5:176882365 C>A), RS1001614069 (5:176895178 G>A,T), RS1001725207 (5:176895368 C>G,T), RS1002149889 (5:176884957 C>T), RS1002195865 (5:176889117 C>T), RS1002539781 (5:176897754 G>A,C)

Disease associations

OMIM: gene MIM:142570 | disease phenotypes: MIM:601379

GenCC curated gene-disease

Mondo (2): Hunter-McAlpine craniosynostosis (MONDO:0011065), long QT syndrome (MONDO:0002442)

Orphanet (1): Hunter-McAlpine syndrome (Orphanet:97340)

HPO phenotypes

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

GWAS associations

0 associations (top):

MeSH disease descriptors (2)

Descriptor	Name	Tree numbers
D008133	Long QT Syndrome	C14.280.067.565; C14.280.123.625; C16.131.240.400.715; C23.550.073.547
C536072	Hunter-McAlpine syndrome (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2709 (SINGLE PROTEIN)

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

CTD chemical–gene interactions

24 total (human), top 24 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Tretinoin	increases expression	3
bisphenol A	increases expression, decreases expression	2
aristolochic acid I	increases expression	1
bisphenol F	decreases expression	1
triphenyl phosphate	affects expression	1
sodium bichromate	decreases expression	1
sodium arsenite	affects expression	1
S-(1,2-dichlorovinyl)cysteine	affects cotreatment, decreases expression	1
tamibarotene	increases expression	1
CGP 52608	affects binding, increases reaction	1
bisphenol S	decreases expression	1
(+)-JQ1 compound	decreases expression	1
bisphenol AF	decreases expression	1
Arsenic Trioxide	decreases expression	1
Air Pollutants	affects expression, increases abundance	1
Benzo(a)pyrene	decreases methylation, increases methylation	1
Estradiol	decreases expression	1
Lipopolysaccharides	affects cotreatment, decreases expression	1
Niclosamide	decreases expression	1
Ozone	affects expression, increases abundance	1
Testosterone	decreases expression	1
Valproic Acid	increases methylation	1
Aflatoxin B1	increases methylation	1
Antirheumatic Agents	decreases expression	1

ChEMBL screening assays

1 unique, capped per target: 1 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2166288	Binding	Activation of human hexokinase 3 at 500 times EC50 concentration	Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. — J Med Chem

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT02513940	PHASE4	COMPLETED	Influence of Testosterone Administration on Drug-Induced QT Interval Prolongation and Torsades de Pointes
NCT03834883	PHASE4	COMPLETED	Reducing the Risk of Drug-Induced QT Interval Lengthening in Women
NCT04169100	PHASE4	UNKNOWN	Novel Form of Acquired Long QT Syndrome
NCT04675788	PHASE4	COMPLETED	Novel Approaches for Minimizing Drug-Induced QT Interval Lengthening
NCT01648205	PHASE2	COMPLETED	Long-term Efficacy Study of Sodium Channel Blocker in LQT3 Patients
NCT02412709	PHASE2	UNKNOWN	Long QT Syndrome Screening in Newborns
NCT04581408	PHASE2	COMPLETED	Mutation-specific Therapy for the Long QT Syndrome
NCT00316459	PHASE1	COMPLETED	Study Evaluating the Effects of Multiple Oral Doses of ERB-041 on Cardiac Repolarization in Healthy Subjects
NCT01849003	PHASE1	COMPLETED	Study of the Effect of GS-6615 in Subjects With LQT-3
NCT02365532	PHASE1	COMPLETED	Effect of Oral GS-6615 on Dofetilide-Induced QT Prolongation, Safety, and Tolerability in Healthy Adults
NCT02412098	PHASE1	COMPLETED	Pharmacokinetics of Eleclazine in Adults With Normal and Impaired Hepatic Function
NCT02441829	PHASE1	COMPLETED	Pharmacokinetics of Eleclazine in Adults With Normal and Impaired Renal Function
NCT05759962	PHASE1	COMPLETED	Phase 1 Study of LQT-1213 in Healthy Adults
NCT05906732	PHASE1/PHASE2	TERMINATED	Study of LQT-1213 on QTc-induced Prolongation in Healthy Adult Subjects (Part1) and on Congenital Long QT in Patients Diagnosed With Type 2 or 3 Long QT Syndrome (Part 2).
NCT00005176	Not specified	COMPLETED	Long QT Syndrome-Population Genetics and Cardiac Studies
NCT00005250	Not specified	COMPLETED	Linkage Study of Long QT Syndrome In An Amish Kindred
NCT00005367	Not specified	COMPLETED	Epidemiology of Long QTand Asian Sudden Death in Sleep
NCT00221832	Not specified	UNKNOWN	Molecular Genetic Screening and Identification of Congenital Arrhythmogenic Diseases
NCT00292032	Not specified	COMPLETED	Registry of Unexplained Cardiac Arrest
NCT00335036	Not specified	TERMINATED	Pediatric Lead Extractability and Survival Evaluation (PLEASE)
NCT00399412	Not specified	COMPLETED	ECG Signal Collection From Long QT Syndrome, Wide QRS Complexes, Heart Failure, and Cardiac Resynchronization Patients
NCT00488254	Not specified	COMPLETED	The Long QT Syndrome in Pregnancy
NCT00588965	Not specified	COMPLETED	Effect of Beta-blocker Therapy on QTc Response in Exercise and Recovery in Normal Subjects
NCT01705925	Not specified	COMPLETED	Multicenter Evaluation of Children and Young Adults With Genotype Positive Long QT Syndrome
NCT01903564	Not specified	COMPLETED	Fetal and Neonatal Magnetophysiology
NCT02082431	Not specified	COMPLETED	Determine the Incidence of Long QT Amongst a Large Cohort of Subjects Diagnosed With Unilateral or Bilateral Sensorineural Hearing Loss.
NCT02413450	Not specified	ENROLLING_BY_INVITATION	Derivation of Human Induced Pluripotent Stem (iPS) Cells to Heritable Cardiac Arrhythmias
NCT02425189	Not specified	COMPLETED	The Canadian National Long QT Syndrome Registry
NCT02439645	Not specified	TERMINATED	A Registry to Determine the Clinical and Genetic Risk Factors for Torsade De Pointes
NCT02439658	Not specified	UNKNOWN	Genetics of QT Prolongation With Antiarrhythmics
NCT02549664	Not specified	COMPLETED	Exercise in Genetic Cardiovascular Conditions
NCT02581241	Not specified	COMPLETED	Abnormal QT-Response to the Sudden Tachycardia Provoked by Standing in Individuals With Drug-induced Long QT Syndrome
NCT02680080	Not specified	COMPLETED	Effect of Grapefruit on QT Interval in Healthy Volunteers and Patients With Congenital Long QT Syndrome
NCT02775513	Not specified	UNKNOWN	Metabolism of Patients With Genetically Caused Cardiac Arrhythmia
NCT02814981	Not specified	UNKNOWN	Hydroxyzine and Risk of Prolongation of QT Interval
NCT02876380	Not specified	COMPLETED	Prospective Identification of Long QT Syndrome in Fetal Life
NCT03182777	Not specified	COMPLETED	Safety of Local Dental Anesthesia in Patients With Cardiac Channelopathies
NCT03544918	Not specified	COMPLETED	Prevalence of Congenital Long QT Syndrome and Acquired QT Prolongation in a Hospital Cohort
NCT03642405	Not specified	UNKNOWN	Drug-induced Repolarization ECG Changes
NCT03678311	Not specified	COMPLETED	Long QT Syndrome and Sleep Apnea