GSTO1

Summary

GSTO1 (glutathione S-transferase omega 1, HGNC:13312) is a protein-coding gene on chromosome 10q25.1, encoding Glutathione S-transferase omega-1 (P78417). Exhibits glutathione-dependent thiol transferase and dehydroascorbate reductase activities.

The protein encoded by this gene is an omega class glutathione S-transferase (GST) with glutathione-dependent thiol transferase and dehydroascorbate reductase activities. GSTs are involved in the metabolism of xenobiotics and carcinogens. The encoded protein acts as a homodimer and is found in the cytoplasm. Three transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 9446 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 39 total
• Druggable target: yes — 4 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_004832

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:13312
Approved symbol	GSTO1
Name	glutathione S-transferase omega 1
Location	10q25.1
Locus type	gene with protein product
Status	Approved
Aliases	GSTTLp28, P28
Ensembl gene	ENSG00000148834
Ensembl biotype	protein_coding
OMIM	605482
Entrez	9446

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 6 protein_coding, 2 protein_coding_CDS_not_defined

ENST00000369710, ENST00000369713, ENST00000432659, ENST00000445155, ENST00000470554, ENST00000493946, ENST00000539281, ENST00000918902

RefSeq mRNA: 3 — MANE Select: NM_004832 NM_001191002, NM_001191003, NM_004832

CCDS: CCDS53572, CCDS53573, CCDS7555

Canonical transcript exons

ENST00000369713 — 6 exons

Exon	Start	End
ENSE00001833010	104254892	104254962
ENSE00001881019	104267252	104267455
ENSE00003463081	104259576	104259798
ENSE00003495115	104255163	104255271
ENSE00003536013	104266084	104266190
ENSE00003577111	104262979	104263077

Expression profiles

Bgee: expression breadth ubiquitous, 294 present calls, max score 99.20.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 148.9921 / max 704.1453, expressed in 1828 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
106876	148.3189	1828
106875	0.6296	212
106874	0.0436	21

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
monocyte	CL:0000576	99.20	gold quality
mononuclear cell	CL:0000842	99.13	gold quality
right lobe of liver	UBERON:0001114	99.06	gold quality
leukocyte	CL:0000738	99.05	gold quality
right lung	UBERON:0002167	98.89	gold quality
liver	UBERON:0002107	98.84	gold quality
middle temporal gyrus	UBERON:0002771	98.84	gold quality
nephron tubule	UBERON:0001231	98.81	gold quality
right atrium auricular region	UBERON:0006631	98.77	gold quality
heart left ventricle	UBERON:0002084	98.76	gold quality
cardiac ventricle	UBERON:0002082	98.74	gold quality
apex of heart	UBERON:0002098	98.74	gold quality
heart right ventricle	UBERON:0002080	98.70	gold quality
cardiac atrium	UBERON:0002081	98.63	gold quality
gingival epithelium	UBERON:0001949	98.61	gold quality
periodontal ligament	UBERON:0008266	98.60	gold quality
heart	UBERON:0000948	98.57	gold quality
type B pancreatic cell	CL:0000169	98.56	gold quality
left adrenal gland	UBERON:0001234	98.52	gold quality
endothelial cell	CL:0000115	98.47	gold quality
left adrenal gland cortex	UBERON:0035825	98.47	gold quality
descending thoracic aorta	UBERON:0002345	98.45	gold quality
duodenum	UBERON:0002114	98.43	gold quality
right adrenal gland	UBERON:0001233	98.42	gold quality
mucosa of stomach	UBERON:0001199	98.41	gold quality
upper lobe of left lung	UBERON:0008952	98.40	gold quality
upper lobe of lung	UBERON:0008948	98.34	gold quality
adrenal cortex	UBERON:0001235	98.33	gold quality
right adrenal gland cortex	UBERON:0035827	98.33	gold quality
adenohypophysis	UBERON:0002196	98.31	gold quality

Single-cell (SCXA)

Detected in 19 experiment(s), a significant marker in 13.

Experiment	Marker?	Max mean expression
E-HCAD-1	yes	84.13
E-CURD-114	yes	82.43
E-CURD-122	yes	65.21
E-MTAB-8142	yes	37.51
E-HCAD-4	yes	31.89
E-GEOD-130148	yes	23.18
E-HCAD-31	yes	19.80
E-GEOD-125970	yes	18.90
E-MTAB-9221	yes	17.19
E-HCAD-10	yes	15.76
E-MTAB-5061	yes	6.06
E-MTAB-9801	yes	3.40
E-MTAB-8559	no	987.90
E-MTAB-7052	no	901.10
E-GEOD-109979	no	433.10

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 40)

• Data describe the functional characterization of two variants of human glutathione-s-transferase omega. (PMID:12565892)
• Arsenic metabolism associated hGSTO1-1 in the European ancestry group was more polymorphic than the Indigenous American Ancestry groups. Mexican Hispanics, could vary in the extent of polymorphism in these genes based upon the admixture. (PMID:12928150)
• a significant association was found for GSTO1 (P=0.007) and a second transcribed member of the GST omega class, GSTO2 (P=0.005), located next to GSTO1. (PMID:14570706)
• Our results do not confirm an association between PD and frequency of hGSTO2*N142D. (PMID:15159516)
• 2 missense polymorphisms in exon 4 (Ala140Asp & Glu155DeltaGlu) were detected. Asp allele genotype affected CSF cholesterol, serum homocysteine. risk of vascular dementia, stroke, and early-onset Alzheimer’s disease. (PMID:15623683)
• no association either with age-at-onset in AD cases or with disease risk in the case-control cohort but haplotype analysis revealed a modest association of one haplotype with AD risk (p = 0.04 (PMID:15917099)
• For E155del, the mutation frequency in Ovambo and Japanese subjects was 0.000 and 0.017, respectively, similar to those for other populations. As for E208K polymorphism, no mutation allele was found in Ovambo or Japanese subjects. (PMID:17484623)
• Glutathione S-transferase omega is abundant in alveolar macrophages and airway secretions, with the levels decreased in patients with chronic obstructive pulmonary disease. (PMID:17617905)
• The GSTO1 Asp/Asp genotype presumably modulates the severity and expansion of atherosclerosis in the circle of Willis (PMID:17717316)
• The prevalence of the GSTO1 140A varied significantly among different regional populations in China, which showed that geography played a more important role in the population differentiation for this allele than the ethnicity/race (PMID:18400112)
• Polymorphisms of glutathione S-transferase A1 and O1 and breast cancer among postmenopausal Danish women. (PMID:18414193)
• These results suggest a possible effect of the GSTO1 and 2 locus on age of onset of FALS. (PMID:18427999)
• These data establish the fact that the polymorphic deletion of Glu155 can cause GSTO1-1 deficiency in vivo. (PMID:18571971)
• GSTO2*N142D genotype is significantly associated with high rish of childhood acute lymhpoblastic leukemia. (PMID:18941778)
• Report GSTO1 gene polymorphisms in worldwide populations. (PMID:18986335)
• nuclear translocation of glutathione-S-transferase-omega 1 could be involved in the cancer progression of Barrett’s esophagus (PMID:19148497)
• The GSTO1-140Asp/GSTO2-142Asp haplotype was associated with increased risk of COPD. (PMID:19513904)
• Our study shows no major gene effect of either the MTHFR or GSTO-1 genes as a modifier of ischemic stroke volume. (PMID:19624857)
• polymorphisms in GSTO1 or GSTO2 do not appear to contribute to the large individual variability in arsenic metabolism or susceptibility to arsenicosis. (PMID:19635583)
• Our findings suggest that a significantly joint effect of cigarette smoking, alcohol consumption, arsenic and occupational exposures and risk genotypes/diplotypes of CYP2E1, GSTO1 and GSTO2 on risk of urothelial carcinoma was found. (PMID:19686770)
• it is unlikely that glutathione S-transferases GSTA2, GSTM2, GSTO1, GSTO2, and GSTZ1 participate in breast cancer susceptibility. (PMID:19859803)
• GSTO1-1 overexpression appears to be associated with activation of survival pathways (Akt and ERK1/2) and inhibition of apoptotic pathways (JNK1), as well as protection against cisplatin-induced apoptosis. (PMID:20106899)
• This study provides the allele frequencies of GSTO polymorphism in a sample consisting of 116 apparently healthy individuals of both sexes from Rome (Central Italy). (PMID:20113212)
• the distribution of the GSTO2 gene differed significantly between asthmatics and controls (PMID:20374258)
• These findings supported a role of the GSTO1 rs4925 single nucleotide polymorphism in the risk of sporadic Alzheimer disease in southern Italy. (PMID:20818931)
• Has a role in the risk Urothelial carcinogenesis (PMID:21094982)
• Novel folding and stability defects cause a deficiency of human glutathione transferase omega 1. (PMID:21106529)
• GSTO-1 plays a key role in hormesis induced by low dose trichloroethylene. (PMID:21351650)
• we hypothesized that GSTO1*E155del is an uncommon genetic variant associated with Alzheimer’s Disease risk. (PMID:22100662)
• Our studies confirm the lack of association between GSTO1 variants and essential hypertension risk, also for two uncommon genetic variants with large functional effects in italian patients. (PMID:22283150)
• Results suggest a role of GSTO1-1 in the inflammatory response and the apoptotic process and indicate that A140D and E208K polymorphisms could increase risk of developing inflammatory and apoptosis-related diseases in As-exposed populations. (PMID:22293942)
• Genetic polymorphisms GSTO and As3MT modify arsenic metabolism as evidenced by altered urinary arsenic excretion (PMID:22339537)
• low monomethylarsonic acid is associated with increased risk for MetS among As-exposed subjects and the genetic polymorphism of GSTO1 (PMID:22440634)
• The minor allele of GSTO1 rs4925 associates with decreased risk in familial Parkinson disease. The minor alleles of GSTO1 rs4925 and GSTO2 rs156697 SNPs associate with lower brain levels of GSTO2, but not GSTO1. (PMID:22494505)
• the crystal structure of a human GSTO1-1 has been determined at 1.7 A resolution in complex with the reaction product ascorbic acid (PMID:22522127)
• Single nucleotide polymorphisms (SNPs) in arsenic methyltransferase and methylene-tetrahydrofolate reductase is associated with bladder cancer in those exposed to low concentrations of inorganic arsenic. SNPs in glutathione S-transferase omega-1 are not. (PMID:22747749)
• The frequencies of GSTO1 and GSTO2 genotypes were not significantly different between head and neck squamous cell carcinoma cases and controls. (PMID:23086268)
• Our study is the first to show that the frequency of GSTO1 A140D gene polymorphism in the Turkish population is similar to other Caucasian populations and that this polymorphism is not associated with susceptibility to NSCLC. (PMID:23819933)
• The common A140D genetic polymorphism in GSTO1 was found to have significant effects on the kinetics of both the deglutathionylation and glutathionylation reactions. (PMID:23888047)
• GSTT1 active genotype and GSTO1 Asp140Asp and GSTO2 Asp142Asp genotypes may have a prognostic/pharmacogenomic role in patients with muscle invasive bladder cancer. (PMID:24040330)

Cross-species orthologs

35 orthologs

Organism	Symbol	Gene ID
danio_rerio	gsto1	ENSDARG00000022183
danio_rerio	gsto2	ENSDARG00000033285
mus_musculus	Gsto1	ENSMUSG00000025068
rattus_norvegicus	Gsto1	ENSRNOG00000071889
drosophila_melanogaster	GstD1	FBGN0001149
drosophila_melanogaster	GstD2	FBGN0010038
drosophila_melanogaster	GstD3	FBGN0010039
drosophila_melanogaster	GstD4	FBGN0010040
drosophila_melanogaster	GstD5	FBGN0010041
drosophila_melanogaster	GstD6	FBGN0010042
drosophila_melanogaster	GstD7	FBGN0010043
drosophila_melanogaster	GstD8	FBGN0010044
drosophila_melanogaster	GstE12	FBGN0027590
drosophila_melanogaster	Clic	FBGN0030529
drosophila_melanogaster	GstT3	FBGN0031117
drosophila_melanogaster	GstE13	FBGN0033381
drosophila_melanogaster	GstE1	FBGN0034335
drosophila_melanogaster	GstE11	FBGN0034354
drosophila_melanogaster	GstD9	FBGN0038020
drosophila_melanogaster	GstD10	FBGN0042206
drosophila_melanogaster	GstT1	FBGN0050000
drosophila_melanogaster	GstT2	FBGN0050005
drosophila_melanogaster	GstE9	FBGN0063491
drosophila_melanogaster	GstE8	FBGN0063492
drosophila_melanogaster	GstE7	FBGN0063493
drosophila_melanogaster	GstE6	FBGN0063494
drosophila_melanogaster	GstE5	FBGN0063495
drosophila_melanogaster	GstE4	FBGN0063496
drosophila_melanogaster	GstE3	FBGN0063497
drosophila_melanogaster	GstE2	FBGN0063498
drosophila_melanogaster	GstE10	FBGN0063499
caenorhabditis_elegans	exc-4	WBGENE00001365
caenorhabditis_elegans		WBGENE00001371
caenorhabditis_elegans	gst-43	WBGENE00001791
caenorhabditis_elegans		WBGENE00021817

Paralogs (14): GSTO2 (ENSG00000065621), GSTT2 (ENSG00000099984), GSTZ1 (ENSG00000100577), GDAP1 (ENSG00000104381), CLIC5 (ENSG00000112782), GDAP1L1 (ENSG00000124194), GSTT2B (ENSG00000133433), CLIC2 (ENSG00000155962), CLIC6 (ENSG00000159212), CLIC4 (ENSG00000169504), CLIC3 (ENSG00000169583), CLIC1 (ENSG00000213719), EEF1G (ENSG00000254772), GSTT4 (ENSG00000276950)

Protein

Protein identifiers

Glutathione S-transferase omega-1 — P78417 (reviewed: P78417)

Alternative names: Glutathione S-transferase omega 1-1, Glutathione-dependent dehydroascorbate reductase, Monomethylarsonic acid reductase, S-(Phenacyl)glutathione reductase

All UniProt accessions (4): P78417, Q5TA01, Q5TA02, V9HWG9

UniProt curated annotations — full annotation on UniProt →

Function. Exhibits glutathione-dependent thiol transferase and dehydroascorbate reductase activities. Has S-(phenacyl)glutathione reductase activity. Also has glutathione S-transferase activity. Participates in the biotransformation of inorganic arsenic and reduces monomethylarsonic acid (MMA) and dimethylarsonic acid.

Subunit / interactions. Homodimer.

Subcellular location. Cytoplasm. Cytosol.

Tissue specificity. Ubiquitous. Highest expression in liver, pancreas, skeletal muscle, spleen, thymus, colon, blood leukocyte and heart. Lowest expression in brain, placenta and lung.

Activity regulation. Monomethylarsonic acid reductase activity is competitively inhibited by 1-chloro 2,4-dinitrobenzene (CDNB) and by deoxycholate.

Similarity. Belongs to the GST superfamily. Omega family.

Isoforms (3)

UniProt ID	Names	Canonical?
P78417-1	1	yes
P78417-2	2
P78417-3	3

RefSeq proteins (3): NP_001177931, NP_001177932, NP_004823* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR004045	Glutathione_S-Trfase_N	Domain
IPR004046	GST_C	Domain
IPR005442	GST_omega	Family
IPR010987	Glutathione-S-Trfase_C-like	Domain
IPR036249	Thioredoxin-like_sf	Homologous_superfamily
IPR036282	Glutathione-S-Trfase_C_sf	Homologous_superfamily
IPR040079	Glutathione_S-Trfase	Family
IPR045073	Omega/Tau-like	Family
IPR050983	GST_Omega/HSP26	Family

Pfam: PF13409, PF14497

Enzyme classification (BRENDA):

• EC 1.20.4.2 — methylarsonate reductase (BRENDA: 3 organisms, 6 substrates, 1 inhibitors, 3 Km, 0 kcat entries)
• EC 1.8.5.1 — glutathione dehydrogenase (ascorbate) (BRENDA: 48 organisms, 27 substrates, 37 inhibitors, 140 Km, 68 kcat entries)
• EC 2.5.1.18 — glutathione transferase (BRENDA: 178 organisms, 548 substrates, 680 inhibitors, 878 Km, 525 kcat entries)

Substrate kinetics (BRENDA)

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

Substrate	Km (mM)	Measurements
1-CHLORO-2,4-DINITROBENZENE	0.0003–223.6	289
GLUTATHIONE	0.0002–532.43	253
DEHYDROASCORBATE	0.019–2.5	73
GSH	0.0003–37.4	62
GLUTATHIONE	0.04–12.71	42
REDUCED GLUTATHIONE	0.017–11.4	24
ETHACRYNIC ACID	0.0001–2.43	19
GSH	0.69–5.2	17
CUMENE HYDROPEROXIDE	0.038–14.3	10
(+)-2-BROMO-3-(4-NITROPHENYL)PROPANOIC ACID	0.023–0.417	8
MONOCHLOROBIMANE	0.004–0.25	8
4-CHLORO-7-NITROBENZO-2-OXA-1,3-DIAZOLE	0.324–3.866	7
1-IODOHEXANE	0.009–0.059	6
ALACHLOR	0.042–7.23	6
PHENETHYL ISOTHIOCYANATE	0.0065–0.14	6

Catalyzed reactions (Rhea), 3 shown:

• methylarsonate + 2 glutathione + H(+) = methylarsonous acid + glutathione disulfide + H2O (RHEA:15969)
• RX + glutathione = an S-substituted glutathione + a halide anion + H(+) (RHEA:16437)
• L-dehydroascorbate + 2 glutathione = glutathione disulfide + L-ascorbate (RHEA:24424)

UniProt features (46 total): helix 14, strand 7, modified residue 6, sequence variant 6, binding site 3, splice variant 2, domain 2, turn 2, initiator methionine 1, chain 1, mutagenesis site 1, active site 1

Structure

Experimental structures (PDB)

19 structures.

PDB	Method	Resolution (Å)
5YVN	X-RAY DIFFRACTION	1.33
3VLN	X-RAY DIFFRACTION	1.7
4IS0	X-RAY DIFFRACTION	1.72
5YVO	X-RAY DIFFRACTION	1.8
6PNM	X-RAY DIFFRACTION	1.82
6PNO	X-RAY DIFFRACTION	1.82
4YQU	X-RAY DIFFRACTION	1.94
9NAD	X-RAY DIFFRACTION	1.99
1EEM	X-RAY DIFFRACTION	2
5UEH	X-RAY DIFFRACTION	2
6MHC	X-RAY DIFFRACTION	2
4YQV	X-RAY DIFFRACTION	2.06
3LFL	X-RAY DIFFRACTION	2.1
6PNN	X-RAY DIFFRACTION	2.1
6MHD	X-RAY DIFFRACTION	2.16
5V3Q	X-RAY DIFFRACTION	2.25
9LHF	X-RAY DIFFRACTION	2.3
4YQM	X-RAY DIFFRACTION	2.38
6MHB	X-RAY DIFFRACTION	2.75

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P78417-F1	95.42	0.93

Functional residue map

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

Catalytic / active sites (1): 32 (nucleophile)

Ligand- & substrate-binding residues (3): 59; 72; 85–86

Post-translational modifications (6): 129, 143, 148, 152, 2, 57

Mutagenesis-validated functional residues (1):

Position	Phenotype
32	loss of activity.

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-156581	Methylation
R-HSA-156590	Glutathione conjugation
R-HSA-196836	Vitamin C (ascorbate) metabolism
R-HSA-8950505	Gene and protein expression by JAK-STAT signaling after Interleukin-12 stimulation

MSigDB gene sets: 390 (showing top): GOBP_POSITIVE_REGULATION_OF_CALCIUM_ION_TRANSPORT, MODULE_93, GOBP_NEGATIVE_REGULATION_OF_TRANSMEMBRANE_TRANSPORT, GOBP_POSITIVE_REGULATION_OF_SEQUESTERING_OF_CALCIUM_ION, REACTOME_BIOLOGICAL_OXIDATIONS, GOBP_CIRCULATORY_SYSTEM_PROCESS, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, HSIAO_HOUSEKEEPING_GENES, HUMMERICH_BENIGN_SKIN_TUMOR_UP, LINDGREN_BLADDER_CANCER_CLUSTER_3_DN, HUMMERICH_MALIGNANT_SKIN_TUMOR_UP, GOBP_MULTICELLULAR_ORGANISMAL_MOVEMENT, SAENZ_DETOX_PATHWAY_AND_CARCINOGENESIS_DN, GOBP_SKELETAL_MUSCLE_CONTRACTION

GO Biological Process (10): glutathione metabolic process (GO:0006749), regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulum (GO:0010880), regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ion (GO:0010881), positive regulation of skeletal muscle contraction by regulation of release of sequestered calcium ion (GO:0014810), L-ascorbic acid metabolic process (GO:0019852), xenobiotic catabolic process (GO:0042178), negative regulation of release of sequestered calcium ion into cytosol (GO:0051280), positive regulation of release of sequestered calcium ion into cytosol (GO:0051281), cellular response to arsenic-containing substance (GO:0071243), cellular oxidant detoxification (GO:0098869)

GO Molecular Function (6): glutathione transferase activity (GO:0004364), oxidoreductase activity (GO:0016491), glutathione dehydrogenase (ascorbate) activity (GO:0045174), methylarsonate reductase activity (GO:0050610), protein binding (GO:0005515), transferase activity (GO:0016740)

GO Cellular Component (3): cytoplasm (GO:0005737), cytosol (GO:0005829), extracellular exosome (GO:0070062)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Phase II - Conjugation of compounds	2
Metabolism of water-soluble vitamins and cofactors	1
Interleukin-12 signaling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
regulation of release of sequestered calcium ion into cytosol	3
release of sequestered calcium ion into cytosol	2
catalytic activity	2
cellular anatomical structure	2
modified amino acid metabolic process	1
sulfur compound metabolic process	1
release of sequestered calcium ion into cytosol by sarcoplasmic reticulum	1
regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulum	1
regulation of cardiac muscle contraction by calcium ion signaling	1
regulation of skeletal muscle contraction by regulation of release of sequestered calcium ion	1
positive regulation of striated muscle contraction	1
monosaccharide metabolic process	1
carboxylic acid metabolic process	1
lactone metabolic process	1
xenobiotic metabolic process	1
catabolic process	1
negative regulation of calcium ion transmembrane transport	1
positive regulation of calcium ion transmembrane transport	1
response to arsenic-containing substance	1
cellular response to chemical stimulus	1
cellular detoxification	1
transferase activity, transferring alkyl or aryl (other than methyl) groups	1
glutathione disulfide oxidoreductase activity	1
antioxidant activity	1
oxidoreductase activity, acting on a sulfur group of donors, quinone or similar compound as acceptor	1
oxidoreductase activity, acting on phosphorus or arsenic in donors, disulfide as acceptor	1
binding	1
intracellular anatomical structure	1
cytoplasm	1
extracellular vesicle	1

Protein interactions and networks

STRING

1926 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GSTO1	HPGDS	O60760	871
GSTO1	GLRX	P35754	814
GSTO1	GSTP1	P09211	709
GSTO1	GSTK1	Q9Y2Q3	699
GSTO1	GSTM1	P09488	686
GSTO1	SLCO6A1	Q86UG4	686
GSTO1	GSTT2B	P0CG30	670
GSTO1	GSTA1	P08263	666
GSTO1	GSTM3	P21266	649
GSTO1	GSTA4	O15217	637
GSTO1	GSTM2	P28161	632
GSTO1	AS3MT	Q9HBK9	623
GSTO1	GSR	P00390	616
GSTO1	TXN	P10599	607
GSTO1	GSTA3	Q16772	593

IntAct

24 interactions, top by confidence:

A	B	Type	Score
MED20	MED19	psi-mi:“MI:0914”(association)	0.840
HSPB1	GSTO1	psi-mi:“MI:0915”(physical association)	0.510
GSTO1	CPNE7	psi-mi:“MI:0915”(physical association)	0.400
	TK2	psi-mi:“MI:0915”(physical association)	0.400
GSTO1	CFTR	psi-mi:“MI:0915”(physical association)	0.370
CFTR	GSTO1	psi-mi:“MI:0915”(physical association)	0.370
FGR	HNRNPCL1	psi-mi:“MI:0914”(association)	0.350
SH2D3C	ANXA2P2	psi-mi:“MI:0914”(association)	0.350
TRIM24	DDTL	psi-mi:“MI:0914”(association)	0.350
M		psi-mi:“MI:0914”(association)	0.350
ZDHHC5	HACD3	psi-mi:“MI:0914”(association)	0.350
UBA5	PGK1	psi-mi:“MI:0914”(association)	0.350
TP53	HGS	psi-mi:“MI:0914”(association)	0.350
GSTO2	GSTO1	psi-mi:“MI:0914”(association)	0.350
FN1	ESYT2	psi-mi:“MI:0914”(association)	0.350
GATA2	EFCAB5	psi-mi:“MI:0914”(association)	0.350
TRAF6	GSTO1	psi-mi:“MI:0915”(physical association)	0.000
GSTO1	RBM48	psi-mi:“MI:0915”(physical association)	0.000
GSTO1	EEF1G	psi-mi:“MI:0915”(physical association)	0.000
GSTO1	CEP126	psi-mi:“MI:0915”(physical association)	0.000
GSTO1	KAT5	psi-mi:“MI:0915”(physical association)	0.000
GSTO1	SETDB1	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (117): GSTO1 (Two-hybrid), GSTO1 (Affinity Capture-Western), C11orf54 (Co-fractionation), CAPN1 (Co-fractionation), CAPN9 (Co-fractionation), DUT (Co-fractionation), ECH1 (Co-fractionation), FKBP1B (Co-fractionation), GSTA4 (Co-fractionation), GSTO1 (Co-fractionation), GSTO1 (Co-fractionation), GSTO1 (Co-fractionation), GSTO1 (Co-fractionation), GSTO1 (Co-fractionation), HSPE1 (Co-fractionation)

ESM2 similar proteins: A0A1W2PR19, A6QQZ0, O09131, O65857, O76483, O88741, P09488, P0CG29, P0CG30, P21266, P28161, P28342, P30109, P30568, P30713, P42760, P46409, P46430, P46439, P46440, P48774, P57108, P78417, Q01579, Q03013, Q03425, Q03662, Q4V8E6, Q5BK56, Q5R8E8, Q61133, Q64471, Q84TK0, Q8R5I6, Q8TB36, Q9BEA9, Q9BEB0, Q9C6C8, Q9D4P7, Q9FE46

Diamond homologs: A8XT16, O09131, P30347, P34277, P34345, P49248, P78417, P81124, Q10N44, Q6AXV9, Q8K2Q2, Q9H4Y5, Q9N1F5, Q9VSL3, Q9Z339, A2XMN2, O43708, P0ACA1, P0ACA2, P28342, P32111, P45207, P46421, Q10CE7, Q65XA0, Q7VLK4, Q8L7C9, Q8LE52, Q9CA57, Q9FWR4, Q9LZ06, Q9WVL0, Q9ZW27, Q9ZW28, Q9ZW29, Q9ZW30, F4IA73, O04437, O43123, O86043

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	27
Likely benign	4
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

796 predictions. Top by Δscore:

Variant	Effect	Δscore
10:104254937:G:GT	donor_gain	1.0000
10:104259572:TCAGG:T	acceptor_loss	1.0000
10:104259573:CAGGC:C	acceptor_loss	1.0000
10:104259574:A:AG	acceptor_gain	1.0000
10:104259574:AGGCA:A	acceptor_loss	1.0000
10:104259575:G:GG	acceptor_gain	1.0000
10:104259729:G:T	donor_gain	1.0000
10:104259794:CTAAG:C	donor_loss	1.0000
10:104259795:TAAGG:T	donor_loss	1.0000
10:104259796:AAG:A	donor_loss	1.0000
10:104259797:AG:A	donor_loss	1.0000
10:104259798:GGTT:G	donor_loss	1.0000
10:104259799:G:T	donor_loss	1.0000
10:104259800:T:A	donor_loss	1.0000
10:104262975:CTA:C	acceptor_loss	1.0000
10:104262977:AGG:A	acceptor_loss	1.0000
10:104262978:GGT:G	acceptor_gain	1.0000
10:104263073:AGGAG:A	donor_loss	1.0000
10:104263074:GGAG:G	donor_gain	1.0000
10:104263074:GGAGG:G	donor_loss	1.0000
10:104263075:G:GT	donor_gain	1.0000
10:104263075:GAGGT:G	donor_loss	1.0000
10:104263076:AGGT:A	donor_loss	1.0000
10:104263077:GGT:G	donor_loss	1.0000
10:104263078:G:A	donor_loss	1.0000
10:104263079:T:A	donor_loss	1.0000
10:104266078:GTTCA:G	acceptor_loss	1.0000
10:104266079:TTCAG:T	acceptor_loss	1.0000
10:104266080:TCAGG:T	acceptor_loss	1.0000
10:104266081:CAGG:C	acceptor_loss	1.0000

AlphaMissense

1593 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
10:104255228:T:C	F34L	0.994
10:104255230:T:A	F34L	0.994
10:104255230:T:G	F34L	0.994
10:104259616:T:A	W62R	0.992
10:104259616:T:C	W62R	0.992
10:104255219:T:C	F31L	0.988
10:104255221:C:A	F31L	0.988
10:104255221:C:G	F31L	0.988
10:104255222:T:C	C32R	0.986
10:104255263:G:C	K45N	0.981
10:104255263:G:T	K45N	0.981
10:104259609:G:C	K59N	0.981
10:104259609:G:T	K59N	0.981
10:104267352:T:C	F225L	0.981
10:104267354:C:A	F225L	0.981
10:104267354:C:G	F225L	0.981
10:104255210:A:C	S28R	0.980
10:104255212:C:A	S28R	0.980
10:104255212:C:G	S28R	0.980
10:104255202:G:C	R25P	0.979
10:104255253:T:C	L42P	0.979
10:104255239:G:C	R37S	0.977
10:104255239:G:T	R37S	0.977
10:104259618:G:C	W62C	0.977
10:104259618:G:T	W62C	0.977
10:104259702:T:G	C90W	0.975
10:104266150:T:A	W178R	0.975
10:104266150:T:C	W178R	0.975
10:104266156:T:A	W180R	0.975
10:104266156:T:C	W180R	0.975

dbSNP variants (sampled 300 via entrez): RS1000117213 (10:104256127 C>A,G), RS1000490830 (10:104255806 G>T), RS1000711862 (10:104258798 C>G,T), RS1000825968 (10:104265893 T>C,G), RS1000997548 (10:104264667 A>G), RS1001042688 (10:104257402 G>A,C), RS1001323824 (10:104264363 A>G,T), RS1001528501 (10:104257740 A>G), RS1002049956 (10:104258833 G>A,C), RS1002389383 (10:104257405 A>G), RS1002600839 (10:104253693 A>C,T), RS1003018292 (10:104254933 C>G), RS1003044599 (10:104260468 C>A,T), RS1003116832 (10:104260786 C>T), RS1003285460 (10:104267236 T>C)

Disease associations

OMIM: gene MIM:605482 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST006585_129	Blood protein levels	3.000000e-139
GCST009391_174	Metabolite levels	1.000000e-06

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0010488	glycerol-3-phosphate measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3174 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 178,630 (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
CHEMBL1503	OMEPRAZOLE	4	52,284
CHEMBL374478	RIFAMPIN	4	93,834
CHEMBL451887	CARFILZOMIB	4	12,508
CHEMBL456	ETHACRYNIC ACID	4	20,004

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — 2.5.1.18 Glutathione transferases

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
C1-27	Inhibition	6.89	pIC50
compound 25 [PMID: 32105470]	Inhibition	6.6	pIC50

Binding affinities (BindingDB)

1 measured of 1 human assays (2 total across all organisms); most potent 1 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
N-[3-(N-(2-chloroacetyl)-4-nitroanilino)propyl]-2,2,2-trifluoro-N-prop-2-ynylacetamide	IC50	23 nM

ChEMBL bioactivities

88 potent at pChembl≥5 of 92 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.66	IC50	0.22	nM	CHEMBL4593975
9.49	IC50	0.32	nM	CHEMBL4513682
8.25	IC50	5.6	nM	CHEMBL4463748
7.68	IC50	21	nM	CHEMBL4215608
7.68	IC50	21	nM	CHEMBL4210652
7.60	IC50	25	nM	CHEMBL4443686
7.55	IC50	28	nM	CHEMBL1502738
7.52	IC50	30	nM	CHEMBL4529442
7.52	IC50	30	nM	CHEMBL4445050
7.51	IC50	31	nM	CHEMBL4210652
7.46	IC50	35	nM	CHEMBL4215608
7.40	IC50	40	nM	CHEMBL4203414
7.40	IC50	40	nM	CHEMBL4568270
7.29	IC50	51	nM	CHEMBL4454963
7.27	IC50	54	nM	CHEMBL1486332
7.22	IC50	60	nM	CHEMBL4458115
7.16	IC50	70	nM	CHEMBL4454026
7.10	IC50	80	nM	CHEMBL4443397
7.10	IC50	80	nM	CHEMBL4458365
7.03	Kd	94.47	nM	CHEMBL5653589
7.03	ED50	94.47	nM	CHEMBL5653589
6.96	IC50	110	nM	CHEMBL4437777
6.92	IC50	120	nM	CHEMBL1598561
6.89	IC50	130	nM	CHEMBL4210652
6.89	IC50	130	nM	CHEMBL4588856
6.82	IC50	150	nM	CARFILZOMIB
6.82	IC50	150	nM	CHEMBL4435063
6.82	IC50	150	nM	CHEMBL4475326
6.80	IC50	160	nM	CHEMBL4449225
6.80	IC50	160	nM	CHEMBL4445668
6.77	IC50	170	nM	CHEMBL4463910
6.75	IC50	180	nM	CHEMBL4465385
6.72	IC50	190	nM	CHEMBL4525870
6.70	IC50	200	nM	CHEMBL4520358
6.68	IC50	210	nM	CHEMBL4544892
6.66	IC50	220	nM	CHEMBL4462744
6.64	IC50	230	nM	CHEMBL4455136
6.60	IC50	250	nM	CHEMBL3781794
6.60	IC50	250	nM	CHEMBL4589666
6.57	IC50	270	nM	CHEMBL4459484
6.52	IC50	300	nM	CHEMBL4473088
6.47	IC50	340	nM	CHEMBL4441594
6.46	IC50	350	nM	CHEMBL3780419
6.44	IC50	360	nM	CHEMBL4548287
6.43	IC50	370	nM	CHEMBL4444587
6.40	IC50	400	nM	CHEMBL4437360
6.36	Ki	440	nM	CHEMBL4210652
6.33	IC50	470	nM	CHEMBL4464480
6.28	IC50	530	nM	CHEMBL4572743
6.24	IC50	570	nM	CHEMBL4555732

PubChem BioAssay actives

87 with measured affinity, of 157 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
N-[4-(2-hydroxyphenyl)-1,3-thiazol-2-yl]-N-[(3-methyl-1,2-oxazol-5-yl)methyl]prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.0002	uM
N-[4-(4-chloro-2-hydroxyphenyl)-1,3-thiazol-2-yl]-N-[(3-methyl-1,2-oxazol-5-yl)methyl]prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.0003	uM
2-chloro-N-[4-(2-hydroxyphenyl)-1,3-thiazol-2-yl]-N-[(3-methyl-1,2-oxazol-5-yl)methyl]acetamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.0056	uM
2-chloro-N-[4-chloro-3-(dimethylsulfamoyl)phenyl]acetamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.0210	uM
2-(N-(2-chloroacetyl)-3-fluoroanilino)-N-cyclohexyl-2-pyridin-2-ylacetamide	1384574: Inhibition of human recombinant GSTO1-1 incubated for 30 mins by fluorescence polarization based gel-based competitive ABPP assay	ic50	0.0210	uM
N-[(3-methyl-1,2-oxazol-5-yl)methyl]-N-[4-[4-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.0250	uM
N-[3-(N-(2-chloroacetyl)-4-nitroanilino)propyl]-2,2,2-trifluoroacetamide	1384565: Inhibition of GSTO1-1 (unknown origin) by enzymatic assay	ic50	0.0280	uM
2-chloro-N-[4-chloro-3-(2-methoxyethylsulfamoyl)phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.0300	uM
N-[2-(oxetan-3-ylamino)-2-oxoethyl]-N-(4-phenyl-1,3-thiazol-2-yl)prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.0300	uM
N-[4-(4-fluoro-2-hydroxyphenyl)-1,3-thiazol-2-yl]-N-[(3-methyl-1,2-oxazol-5-yl)methyl]prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.0400	uM
8-(3,7-dimethyloctoxy)-3-(1-hydroxy-4-oxocyclohexa-2,5-dien-1-yl)benzo[f]chromen-1-one	1384568: Inhibition of GSTO1-1 (unknown origin) by 4-NPG substrate based assay	ic50	0.0400	uM
N-[(3-methyl-1,2-oxazol-5-yl)methyl]-N-(4-phenyl-1,3-thiazol-2-yl)prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.0510	uM
2-(N-(2-chloroacetyl)-4-fluoroanilino)-N-cyclohexyl-2-pyridin-3-ylacetamide	1384565: Inhibition of GSTO1-1 (unknown origin) by enzymatic assay	ic50	0.0540	uM
2-chloro-N-[3-(dimethylsulfamoyl)-4-(trifluoromethyl)phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.0600	uM
2-chloro-N-[4-chloro-3-(propan-2-ylsulfamoyl)phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.0700	uM
2-chloro-N-[4-chloro-3-[2-methoxyethyl(methyl)sulfamoyl]phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.0800	uM
N-[2-(cyclohexylamino)-2-oxoethyl]-N-(4-phenyl-1,3-thiazol-2-yl)prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.0800	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148468: Binding affinity to human GSTO1 incubated for 45 mins by Kinobead based pull down assay	kd	0.0945	uM
2-chloro-N-[4-chloro-3-(3-methoxypropylsulfamoyl)phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.1100	uM
2-chloro-N-[(3,4-dimethoxyphenyl)methyl]-N-[3-phenyl-3-(4-propan-2-yloxyphenyl)propyl]acetamide	1384568: Inhibition of GSTO1-1 (unknown origin) by 4-NPG substrate based assay	ic50	0.1200	uM
2-chloro-N-[3-(dimethylsulfamoyl)-4-iodophenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.1300	uM
Carfilzomib	1384570: Inhibition of GSTO1-1 (unknown origin) pre-incubated for 1 hr before GSH addition by CDNB-GSH conjugation assay	ic50	0.1500	uM
tert-butyl 2-[(4-phenyl-1,3-thiazol-2-yl)-prop-2-enoylamino]acetate	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.1500	uM
N-[4-bromo-3-(dimethylsulfamoyl)phenyl]-2-chloroacetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.1500	uM
2-chloro-N-[4-chloro-3-[3-methoxypropyl(methyl)sulfamoyl]phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.1600	uM
2-chloro-N-(4-chloro-3-morpholin-4-ylsulfonylphenyl)acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.1600	uM
N-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.1700	uM
2-chloro-N-[4-chloro-3-[2-hydroxyethyl(methyl)sulfamoyl]phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.1800	uM
N-[4-(2-hydroxyphenyl)thiophen-2-yl]-N-[(3-methyl-1,2-oxazol-5-yl)methyl]prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.1900	uM
2-chloro-N-[4-chloro-3-(oxolan-2-ylmethylsulfamoyl)phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.2000	uM
2-chloro-N-[3-(dimethylsulfamoyl)-4-(trifluoromethoxy)phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.2100	uM
ethyl 5-phenyl-2-(prop-2-enoylamino)thiophene-3-carboxylate	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.2200	uM
N-[2-(2-morpholin-4-ylethylamino)-2-oxoethyl]-N-(4-phenyl-1,3-thiazol-2-yl)prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.2300	uM
2-chloro-N-[3-morpholin-4-ylsulfonyl-4-(trifluoromethyl)phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.2500	uM
1-[2-fluoro-5-(oxiran-2-yl)phenyl]sulfonyl-3-(1,2,3,5,6,7-hexahydro-s-indacen-4-yl)urea	1286178: Irreversible inhibition of GSTO 1-1 in LPS activated human monocytes after 30 mins by ELISA analysis in presence of ATP	ic50	0.2500	uM
ethyl 4-phenyl-2-(prop-2-enoylamino)-1,3-thiazole-5-carboxylate	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.2700	uM
N-[4-[4-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.3000	uM
2-chloro-N-[4-chloro-3-(oxolan-3-ylsulfamoyl)phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.3400	uM
1-[2,6-di(propan-2-yl)phenyl]-3-[2-fluoro-5-(oxiran-2-yl)phenyl]sulfonylurea	1286178: Irreversible inhibition of GSTO 1-1 in LPS activated human monocytes after 30 mins by ELISA analysis in presence of ATP	ic50	0.3500	uM
N-[4-(2-methoxyphenyl)-1,3-thiazol-2-yl]-N-[(3-methyl-1,2-oxazol-5-yl)methyl]prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.3600	uM
methyl 2-[(4-phenyl-1,3-thiazol-2-yl)-prop-2-enoylamino]acetate	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.3700	uM
N-(4-naphthalen-2-yl-1,3-thiazol-2-yl)prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.4000	uM
S-(diethylcarbamoylsulfanyl) N,N-diethylcarbamothioate	1384565: Inhibition of GSTO1-1 (unknown origin) by enzymatic assay	ic50	0.4000	uM
N-(4-phenyl-1,3-thiazol-2-yl)prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.4700	uM
N-(2-morpholin-4-yl-2-oxoethyl)-N-(4-phenyl-1,3-thiazol-2-yl)prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.5300	uM
ethyl 2-[(4-phenyl-1,3-thiazol-2-yl)-prop-2-enoylamino]acetate	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.5700	uM
2-chloro-N-[4-chloro-3-(methylsulfamoyl)phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.5800	uM
N-[4-(3-chlorophenyl)-1,3-thiazol-2-yl]prop-2-enamide	1602167: Inhibition of CMFDA binding to human N-terminal 6x-His-tagged GSTO1-1 preincubated for 30 mins followed by CMFDA addition and measured after 30 mins by in-gel fluorescence binding assay	ic50	0.6000	uM
2-chloro-N-[4-chloro-3-(2-hydroxyethylsulfamoyl)phenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.7000	uM
2-chloro-N-[3-(dimethylsulfamoyl)-4-phenylphenyl]acetamide	1605489: Inhibition of recombinant GSTO1-1 (unknown origin) expressed in Escherichia coli using S-(4-nitrophenacyl)glutathione as substrate preincubated for 2 mins followed by substrate addition by 4-NPG assay	ic50	0.7100	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Arsenic	decreases metabolic processing, affects reaction, increases abundance, affects abundance, increases response to substance (+4 more)	14
sodium arsenite	increases abundance, increases expression, affects expression, decreases expression	8
bisphenol A	affects cotreatment, decreases methylation, decreases expression, increases expression	6
Cadmium	decreases reaction, increases abundance, increases palmitoylation, decreases activity, decreases expression (+1 more)	5
Cadmium Chloride	increases palmitoylation, decreases activity, decreases expression, increases expression, decreases reaction (+1 more)	5
Acetaminophen	decreases expression	4
Valproic Acid	decreases expression, increases expression, affects expression	4
trichostatin A	affects cotreatment, increases expression	3
monomethylarsonous acid	increases metabolic processing, increases expression, increases chemical synthesis	3
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression, increases expression	3
Cisplatin	affects expression, affects cotreatment, increases expression, affects response to substance	3
Tobacco Smoke Pollution	affects response to substance, affects expression, increases expression	3
Particulate Matter	decreases expression, increases abundance, increases expression	3
arsenite	affects binding, increases reaction, increases chemical synthesis	2
monomethylarsonic acid	increases chemical synthesis, increases metabolic processing, increases reduction	2
LDN 193189	affects cotreatment, decreases expression	2
Decitabine	affects expression, increases expression	2
Ascorbic Acid	increases abundance, affects binding, affects cotreatment, increases expression, decreases expression (+1 more)	2
Benzo(a)pyrene	decreases expression, decreases reaction	2
Tretinoin	increases expression	2
Trichloroethylene	increases expression	2
aristolochic acid I	increases expression	1
bismuth tripotassium dicitrate	increases expression	1
lead acetate	decreases expression, decreases reaction, increases abundance	1
sodium arsenate	increases abundance, increases expression	1
pyrogallol 1,3-dimethyl ether	affects localization, decreases expression, affects cotreatment	1
ascorbate-2-phosphate	increases expression, affects binding, affects cotreatment	1
tris(2-butoxyethyl) phosphate	affects expression	1
2-bromopalmitate	increases palmitoylation, decreases reaction, increases abundance	1
ochratoxin A	decreases expression	1

ChEMBL screening assays

41 unique, capped per target: 37 binding, 2 functional, 2 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1115109	Binding	Displacement of phenylsulphonate-rhodamine from GSTO1 in human MDA-MB-231 cells proteomes at 20 uM after 30 mins by SDS-PAGE gel fluorescence assay	Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9). — Bioorg Med Chem Lett
CHEMBL1738107	Functional	PUBCHEM_BIOASSAY: Late stage assay provider results from the probe development effort to identify inhibitors of GSTO1: Gel-based activity-based protein profiling (ABPP) IC50 Set 2. (Class of assay: confirmatory) [Related pubchem assays (dep	PubChem BioAssay data set
CHEMBL1743232	ADMET	Substrates for human cytosolic glutathione transferase GSTO1	Casarett and Doull’s Toxicology The Basic Science of Poisons, 7th edition

Cellosaurus cell lines

1 cell lines: 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B2YD	Abcam HEK293T GSTO1 KO	Transformed cell line	Female

Clinical trials (associated diseases)

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