OGA

gene
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Also known as MEA5NCOAT

Summary

OGA (O-GlcNAcase, HGNC:7056) is a protein-coding gene on chromosome 10q24.32, encoding Protein O-GlcNAcase (O60502). Cleaves GlcNAc but not GalNAc from O-glycosylated proteins. It is a selective cancer dependency (DepMap: 11.5% of cell lines).

The dynamic modification of cytoplasmic and nuclear proteins by O-linked N-acetylglucosamine (O-GlcNAc) addition and removal on serine and threonine residues is catalyzed by OGT (MIM 300255), which adds O-GlcNAc, and MGEA5, a glycosidase that removes O-GlcNAc modifications (Gao et al., 2001 [PubMed 11148210]).

Source: NCBI Gene 10724 — RefSeq curated summary.

At a glance

  • GWAS associations: 2
  • Clinical variants (ClinVar): 88 total
  • Druggable target: yes — 1 molecules with ChEMBL bioactivity
  • Cancer dependency (DepMap): dependent in 11.5% of screened cell lines
  • MANE Select transcript: NM_012215

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:7056
Approved symbolOGA
NameO-GlcNAcase
Location10q24.32
Locus typegene with protein product
StatusApproved
AliasesMEA5, NCOAT
Ensembl geneENSG00000198408
Ensembl biotypeprotein_coding
OMIM604039
Entrez10724

Gene structure

Transcript identifiers

Ensembl transcripts: 25 — 19 protein_coding, 6 protein_coding_CDS_not_defined

ENST00000357797, ENST00000361464, ENST00000370094, ENST00000429860, ENST00000439817, ENST00000461645, ENST00000462994, ENST00000479811, ENST00000482611, ENST00000492204, ENST00000494347, ENST00000883195, ENST00000883196, ENST00000883197, ENST00000883198, ENST00000883199, ENST00000883200, ENST00000883201, ENST00000883202, ENST00000883203, ENST00000883204, ENST00000928740, ENST00000928741, ENST00000928742, ENST00000928743

RefSeq mRNA: 2 — MANE Select: NM_012215 NM_001142434, NM_012215

CCDS: CCDS44471, CCDS7520

Canonical transcript exons

ENST00000361464 — 16 exons

ExonStartEnd
ENSE00000721914101798842101799455
ENSE00000721926101810184101810314
ENSE00000721929101813030101813127
ENSE00000721932101813555101813606
ENSE00000811427101793913101793998
ENSE00000811428101800242101800400
ENSE00000811429101803735101804019
ENSE00000811430101806045101806143
ENSE00003471052101792839101792943
ENSE00003531550101807730101807901
ENSE00003533549101787364101787523
ENSE00003538234101791354101791439
ENSE00003640803101797980101798154
ENSE00003691121101790896101791088
ENSE00003847848101817824101818444
ENSE00003848061101784450101786587

Expression profiles

Bgee: expression breadth ubiquitous, 292 present calls, max score 99.10.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 41.7872 / max 1031.2089, expressed in 1811 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter IDTPM avgSamples expressed
11110836.48531807
1111052.0225904
1111071.7255970
1111041.5539618

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
spermCL:000001999.10gold quality
skin of abdomenUBERON:000141698.64gold quality
skin of legUBERON:000151198.64gold quality
cerebellar hemisphereUBERON:000224598.58gold quality
cerebellar cortexUBERON:000212998.56gold quality
tibial nerveUBERON:000132398.54gold quality
right uterine tubeUBERON:000130298.49gold quality
mucosa of stomachUBERON:000119998.47gold quality
right hemisphere of cerebellumUBERON:001489098.46gold quality
left ovaryUBERON:000211998.44gold quality
ventricular zoneUBERON:000305398.43gold quality
colonic epitheliumUBERON:000039798.39gold quality
cortical plateUBERON:000534398.38gold quality
descending thoracic aortaUBERON:000234598.31gold quality
ganglionic eminenceUBERON:000402398.30gold quality
right ovaryUBERON:000211898.28gold quality
calcaneal tendonUBERON:000370198.28gold quality
endocervixUBERON:000045898.27gold quality
male germ cellCL:000001598.25gold quality
cerebellumUBERON:000203798.23gold quality
ectocervixUBERON:001224998.20gold quality
right coronary arteryUBERON:000162598.11gold quality
right lungUBERON:000216798.10gold quality
body of uterusUBERON:000985398.10gold quality
vaginaUBERON:000099698.03gold quality
granulocyteCL:000009497.99gold quality
tendonUBERON:000004397.99gold quality
popliteal arteryUBERON:000225097.99gold quality
tibial arteryUBERON:000761097.98gold quality
nippleUBERON:000203097.97gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 1.

ExperimentMarker?Max mean expression
E-GEOD-75367no2938.59
E-MTAB-6075no1398.35
E-GEOD-106540no593.49
E-ANND-3no0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): ALX1, AP1, AR, CREB1, DLX4, FOSB, FOXP3, GRHL3, IRF2, JUN, JUND, KAT5, KAT7, MEF2C, MYC, NCOA1, NFATC1, NFE2, NFKB, PDX1, RELA, SMARCA1, SMARCA5, SRF, TFAP2A, USF1

miRNA regulators (miRDB)

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

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-7110-3P100.0073.182486
HSA-MIR-3064-3P100.0070.091254
HSA-MIR-6873-3P100.0071.422626
HSA-MIR-3613-3P100.0076.367965
HSA-MIR-30A-5P100.0076.313233
HSA-MIR-30B-5P100.0076.293248
HSA-MIR-30C-5P100.0076.293248
HSA-MIR-30D-5P100.0076.323233
HSA-MIR-30E-5P100.0076.323242
HSA-MIR-513B-5P99.9969.962150
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-520G-5P99.9966.76658
HSA-MIR-371B-5P99.9975.344759
HSA-MIR-520D-5P99.9873.344883
HSA-MIR-524-5P99.9873.434882
HSA-MIR-27A-3P99.9872.132955
HSA-MIR-27B-3P99.9872.132955
HSA-MIR-998599.9872.112939
HSA-MIR-569699.9872.364487
HSA-MIR-373-5P99.9875.364753
HSA-MIR-616-5P99.9875.584775
HSA-MIR-314899.9775.066478
HSA-MIR-548AJ-3P99.9673.385345
HSA-MIR-548X-3P99.9673.385345
HSA-MIR-548AA99.9670.643753
HSA-MIR-548AP-3P99.9670.643753
HSA-MIR-548T-3P99.9670.643753
HSA-MIR-128-3P99.9571.172484
HSA-MIR-216A-3P99.9571.192505
HSA-MIR-971899.9468.91918

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 11.5% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

  • This protein is a cytosolic, neutral, O-GlcNAc specific hexosaminidase termed O-GlcNAcase. (PMID:11148210)
  • Investigated this locus in Pima Indians who have the world’s highest prevalence of NIDDM. Concluded that mutations in MGEA5 are unlikely to contribute to NIDDM in this population (PMID:12359146)
  • In type 2 Diabetes patients in Mexico City, the frequency of the T allele of MGEAT5 was higher (2.6%) in the cases than in controls (1.8%), but not a significant deviation from Hardy_Weinberg proportions. (PMID:17546623)
  • review of modifications, phosphorylation and a specific form of glycosylation, O-linked -N-acetylglucosaminylation by O-GlcNAc, relevant to pathological tau phosphorylation (PMID:18641620)
  • the short nuclear variant of O-GlcNAcase, which has the identical catalytic domain as the full-length enzyme, has similar trends in a pH-rate profile and Taft linear free energy analysis as the full-length enzyme (PMID:19423084)
  • characterization of O-GlcNAcase transition states using several series of substrates to generate multiple simultaneous free-energy relationships (PMID:19715310)
  • This study analyzes the activity of the enzyme involved in the removal of these sugar residues, i.e. beta-N-acetylglucosaminidase (O-GlcNAcase) as well as the level of N-acetylglucosamine in benign and malignant thyroid lesions. (PMID:20198314)
  • N-terminal region of OGA contains the catalytic site and the C-terminal region stabilizes the protein structure and affects substrate affinity. (PMID:20673219)
  • Results provide evidence that OGA may possess a substrate-recognition mechanism tinvolving interactions with O-GlcNAcylated proteins beyond the GlcNAc-binding site. (PMID:20863279)
  • Direct evidence links muscle atrophy and the disruption of O-GlcNAcase activity in male bitransgenic mice. (PMID:21178104)
  • Reducing ChREBP(OG) levels via OGA overexpression decreased lipogenic protein content (ACC, FAS), prevented hepatic steatosis, and improved the lipidic profile of OGA-treated db/db mice. (PMID:21471514)
  • Decrease in MGEA5 and increase in O-GlcNAc transferease expression in higher grade tumors suggests that increased O-GlcNAc modification may be implicated in breast tumor progression and metastasis. (PMID:21567137)
  • Chromosomal translocation t(1;10) is consistent with rearrangements of TGFBR3 and MGEA5 in both myxoinflammatory fibroblastic sarcoma and hemosiderotic fibrolipomatous tumor. (PMID:21717526)
  • Data show that the interplay between O-GlcNAc and phosphorylation on proteins and indicate that these effects can be mediated by changes in hOGT and hOGA kinetic activity. (PMID:22311971)
  • O-linked beta-N-acetylglucosaminylation (O-GlcNAcylation) in primary and metastatic colorectal cancer clones and effect of N-acetyl-beta-D-glucosaminidase silencing on cell phenotype and transcriptome. (PMID:22730328)
  • Analysis of urinary content of MGEA5 and OGT may be useful for bladder cancer diagnostics. (PMID:22783592)
  • Estrogen replacement therapy and plyometric training influence muscle OGT and OGA gene expression, which may be one of the mechanisms by which HRT and PT prevent aging-related loss of muscle mass. (PMID:24365779)
  • Report the presence of TGFBR3 and/or MGEA5 rearrangements in pleomorphic hyalinizing angiectatic tumors and the spectrum of related neoplasms. (PMID:24705316)
  • Amino acid composition of splice variants, post-translational modifications, and stable associations with regulatory proteins influence subcellular distribution/substrate specificity of OGA and OGT (O-linked N-acetylglucosamine transferase). [REVIEW] (PMID:25173736)
  • This work identifies the first target of miR-539 in the heart and the first miRNA that regulates OGA. (PMID:25183011)
  • OGA overexpression in endothelial cells improves endothelial function and may have a beneficial effect on coronary vascular complications in diabetes. (PMID:26269457)
  • E2F1 negatively regulates both Ogt and Mgea5 expression in an Rb1 protein-dependent manner. (PMID:26527687)
  • TGFBR3 and/or MGEA5 rearrangements are much more common in hybrid hemosiderotic fibrolipomatous tumor-myxoinflammatory fibroblastic sarcomas than in classical myxoinflammatory fibroblastic sarcomas. (PMID:26980036)
  • the O-linked N-acetylglucosamine (O-GlcNAc) processing enzymes, O-GlcNAc-transferase (OGT) and O-GlcNAcase (OGA), interact with the (A)gamma-globin promoter at the -566 GATA repressor site (PMID:27231347)
  • OGA is physically associated with the known RNA polymerase II (pol II) pausing/elongation factors SPT5 and TRIM28-KAP1-TIF1beta, and a purified OGA-SPT5-TIF1beta complex has elongation properties. (PMID:27601472)
  • hOGA forms an unusual arm-in-arm homodimer in which the catalytic domain of one monomer is covered by the stalk domain of the sister monomer to create a substrate-binding cleft. (PMID:28319083)
  • Data suggest that the substrate specificity of O-GlcNAcase/OGA does not extend to proteins/peptides modified with S-GlcNAc (an analog of O-GlcNAc); proteins modified with S-GlcNAc appear to be stable against O-GlcNAcase/OGA hydrolysis. (PMID:28627871)
  • Tax interacts with the host OGT/OGA complex and inhibits the activity of OGT-bound OGA. (PMID:28742148)
  • Beta-N-acetylhexosaminidase substrate recognition and specificity (PMID:28939839)
  • OGT promotes carcinogenesis and metastasis of cervical cancer cells. OGT’s expression is significantly upregulated in cervical cancer, and low OGT level is correlated with improved prognosis (PMID:30052810)
  • role of the tubular biomarkers NAG, kidney injury molecule-1 and neutrophil gelatinase-associated lipocalin in patients with chest pain before contrast media exposition (PMID:30920848)
  • Study reports that OGA is upregulated in a wide range of human cancers and drives aerobic glycolysis and tumor growth by inhibiting pyruvate kinase M2 (PKM2). PKM2 is dynamically O-GlcNAcylated in response to changes in glucose availability. Under high glucose conditions, PKM2 is a target of OGA-associated acetyltransferase activity, which facilitates O-GlcNAcylation of PKM2 by O-GlcNAc transferase (OGT). (PMID:31501520)
  • Pharmacological inhibition and knockdown of O-GlcNAcase reduces cellular internalization of alpha-synuclein preformed fibrils. (PMID:32365408)
  • Involvement of NDPK-B in Glucose Metabolism-Mediated Endothelial Damage via Activation of the Hexosamine Biosynthesis Pathway and Suppression of O-GlcNAcase Activity. (PMID:33086728)
  • Bacterial O-GlcNAcase genes abundance decreases in ulcerative colitis patients and its administration ameliorates colitis in mice. (PMID:33310751)
  • Elucidating the protein substrate recognition of O-GlcNAc transferase (OGT) toward O-GlcNAcase (OGA) using a GlcNAc electrophilic probe. (PMID:33333092)
  • OGA is associated with deglycosylation of NONO and the KU complex during DNA damage repair. (PMID:34135314)
  • Inhibition of O-GlcNAcase Inhibits Hematopoietic and Leukemic Stem Cell Self-Renewal and Drives Dendritic Cell Differentiation via STAT3/5 Signaling. (PMID:36124999)
  • Cryo-EM structure of human O-GlcNAcylation enzyme pair OGT-OGA complex. (PMID:37907462)
  • E3 ubiquitin ligase UBR5 promotes gemcitabine resistance in pancreatic cancer by inducing O-GlcNAcylation-mediated EMT via destabilization of OGA. (PMID:38755129)

Cross-species orthologs

5 orthologs

OrganismSymbolGene ID
danio_rerioogaENSDARG00000074686
mus_musculusOgaENSMUSG00000025220
rattus_norvegicusOgaENSRNOG00000017822
drosophila_melanogasterOgaFBGN0038870
caenorhabditis_elegansWBGENE00020596

Protein

Protein identifiers

Protein O-GlcNAcaseO60502 (reviewed: O60502)

Alternative names: Beta-N-acetylglucosaminidase, Beta-N-acetylhexosaminidase, Beta-hexosaminidase, Meningioma-expressed antigen 5, N-acetyl-beta-D-glucosaminidase, N-acetyl-beta-glucosaminidase, Nuclear cytoplasmic O-GlcNAcase and acetyltransferase

All UniProt accessions (2): O60502, H7C3X0

UniProt curated annotations — full annotation on UniProt →

Function. Cleaves GlcNAc but not GalNAc from O-glycosylated proteins. Deglycosylates a large and diverse number of proteins, such as CRYAB, ELK1, GSDMD, LMNB1 and TAB1. Can use p-nitrophenyl-beta-GlcNAc and 4-methylumbelliferone-GlcNAc as substrates but not p-nitrophenyl-beta-GalNAc or p-nitrophenyl-alpha-GlcNAc (in vitro). Does not bind acetyl-CoA and does not have histone acetyltransferase activity. Cleaves GlcNAc but not GalNAc from O-glycosylated proteins. Can use p-nitrophenyl-beta-GlcNAc as substrate but not p-nitrophenyl-beta-GalNAc or p-nitrophenyl-alpha-GlcNAc (in vitro), but has about six times lower specific activity than isoform 1.

Subunit / interactions. Monomer. Interacts with CLOCK. (Microbial infection) Interacts with human T-cell leukemia virus 1/HTLV-1 protein Tax; this interaction increases Tax interacting partner CREB1 O-GlcNAcylation.

Subcellular location. Nucleus Cytoplasm.

Tissue specificity. Ubiquitous. Shows highest expression in the brain, placenta and pancreas.

Post-translational modifications. Proteolytically cleaved by caspase-3 during apoptosis. The fragments interact with each other; cleavage does not decrease enzyme activity.

Activity regulation. Inhibited by N-acetylglucosamine and not N-acetylgalactosamine.

Similarity. Belongs to the glycosyl hydrolase 84 family.

Isoforms (4)

UniProt IDNamesCanonical?
O60502-11yes
O60502-22
O60502-33, MGEA5s
O60502-44

RefSeq proteins (2): NP_001135906, NP_036347* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR011496O-GlcNAcase_catDomain
IPR016181Acyl_CoA_acyltransferaseHomologous_superfamily
IPR017853GH_hydrolase_sfHomologous_superfamily
IPR051822Glycosyl_Hydrolase_84Family

Pfam: PF07555

Enzyme classification (BRENDA):

  • EC 3.2.1.169 — protein O-GlcNAcase (BRENDA: 10 organisms, 123 substrates, 118 inhibitors, 78 Km, 29 kcat entries)
  • EC 3.2.1.35 — hyaluronoglucosaminidase (BRENDA: 70 organisms, 156 substrates, 263 inhibitors, 27 Km, 1 kcat entries)

Substrate kinetics (BRENDA)

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

SubstrateKm (mM)Measurements
4-NITROPHENYL N-ACETYL-BETA-D-GLUCOSAMINIDE0.016–3638
4-METHYLUMBELLIFERYL N-ACETYL-BETA-D-GLUCOSAMINI0.0029–1.412
HYALURONAN0.038–0.36711
3,4-DINITROPHENYL N-ACETYL-BETA-D-GLUCOSAMINIDE0.21–0.564
3-FLUORO-4-NITROPHENYL N-ACETYL-BETA-D-GLUCOSAMI0.3–0.734
4-METHYLUMBELLIFERYL-N-ACETYL-BETA-D-GLUCOSAMINI0.0029–0.13
3-NITROPHENYL N-ACETYL-BETA-D-GLUCOSAMINIDE0.47–0.952
4-METHYLUMBELLIFERYL 2-ACETAMIDO-2-DEOXY-BETA-D-0.08–12
FLUORESCEIN DI(N-ACETYL-BETA-D-GLUCOSAMINIDE)0.0849–2.12
N-ACETYL-BETA-D-GLUCOSAMINE1.5–3.62
PHENYL N-ACETYL-BETA-D-GLUCOSAMINIDE0.62–0.952
4-CHLOROPHENYL N-ACETYL-BETA-D-GLUCOSAMINIDE0.561
4-METHYLUMBELLIFERYL N-DIFLUOROACETYL-BETA-D-GLU0.451
4-METHYLUMBELLIFERYL N-FLUOROACETYL-BETA-D-GLUCO0.491
4-METHYLUMBELLIFERYL N-TRIFLUOROACETYL-BETA-D-GL0.381

Catalyzed reactions (Rhea), 2 shown:

  • 3-O-(N-acetyl-beta-D-glucosaminyl)-L-seryl-[protein] + H2O = N-acetyl-D-glucosamine + L-seryl-[protein] (RHEA:48876)
  • 3-O-(N-acetyl-beta-D-glucosaminyl)-L-threonyl-[protein] + H2O = L-threonyl-[protein] + N-acetyl-D-glucosamine (RHEA:48892)

UniProt features (77 total): helix 20, turn 13, strand 13, mutagenesis site 10, binding site 7, splice variant 4, sequence variant 2, region of interest 2, chain 1, domain 1, site 1, modified residue 1, compositionally biased region 1, active site 1

Structure

Experimental structures (PDB)

28 structures.

PDBMethodResolution (Å)
5UN8X-RAY DIFFRACTION2.13
5M7UX-RAY DIFFRACTION2.3
5M7RX-RAY DIFFRACTION2.35
5M7SX-RAY DIFFRACTION2.4
7OU6X-RAY DIFFRACTION2.41
5TKEX-RAY DIFFRACTION2.48
5UN9X-RAY DIFFRACTION2.5
8P0LX-RAY DIFFRACTION2.5
9BA8X-RAY DIFFRACTION2.54
2YDQX-RAY DIFFRACTION2.6
5M7TX-RAY DIFFRACTION2.6
5VVOX-RAY DIFFRACTION2.6
5VVUX-RAY DIFFRACTION2.7
9BA9X-RAY DIFFRACTION2.75
5UHPX-RAY DIFFRACTION2.79
5VVTX-RAY DIFFRACTION2.8
5VVVX-RAY DIFFRACTION2.8
6PM9X-RAY DIFFRACTION2.86
5VVXX-RAY DIFFRACTION2.9
5UHKX-RAY DIFFRACTION2.97
9NE4ELECTRON MICROSCOPY2.98
9NE5ELECTRON MICROSCOPY3.05
9QENELECTRON MICROSCOPY3.08
5UHLX-RAY DIFFRACTION3.14
5UHOX-RAY DIFFRACTION3.21
6HKIX-RAY DIFFRACTION3.3
9NE2ELECTRON MICROSCOPY3.63
7YEHELECTRON MICROSCOPY3.92

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-O60502-F176.020.55

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 (2): 413–414 (cleavage; by caspase-3); 175 (proton donor)

Ligand- & substrate-binding residues (7): 219; 285; 313; 67; 98; 174; 175

Post-translational modifications (1): 364

Mutagenesis-validated functional residues (10):

PositionPhenotype
69strongly reduces affinity for glycopeptide substrates. nearly abolishes enzyme activity.
174nearly abolishes enzyme activity.
175nearly abolishes enzyme activity.
255nearly abolishes enzyme activity.
286nearly abolishes enzyme activity.
287nearly abolishes enzyme activity.
413abrogates cleavage by caspase-3.
679nearly abolishes enzyme activity.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 209 (showing top): TGCGCANK_UNKNOWN, BASSO_B_LYMPHOCYTE_NETWORK, PEREZ_TP63_TARGETS, LFA1_Q6, MAZ_Q6, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, GOBP_CARBOHYDRATE_DERIVATIVE_CATABOLIC_PROCESS, AP2_Q3, GGGTGGRR_PAX4_03, MODULE_229, GOBP_CARBOHYDRATE_DERIVATIVE_METABOLIC_PROCESS, UEDA_PERIFERAL_CLOCK, DEURIG_T_CELL_PROLYMPHOCYTIC_LEUKEMIA_DN, JIANG_TIP30_TARGETS_UP, GOBP_CARBOHYDRATE_DERIVATIVE_BIOSYNTHETIC_PROCESS

GO Biological Process (6): N-acetylglucosamine metabolic process (GO:0006044), protein O-linked glycosylation (GO:0006493), glycoprotein catabolic process (GO:0006516), protein deglycosylation (GO:0006517), glycoprotein metabolic process (GO:0009100), carbohydrate derivative metabolic process (GO:1901135)

GO Molecular Function (8): hyalurononglucosaminidase activity (GO:0004415), hexosaminidase activity (GO:0015929), identical protein binding (GO:0042802), [protein]-3-O-(N-acetyl-D-glucosaminyl)-L-serine/L-threonine O-N-acetyl-alpha-D-glucosaminase activity (GO:0102571), acyltransferase activity, transferring groups other than amino-acyl groups (GO:0016747), hydrolase activity (GO:0016787), hydrolase activity, acting on glycosyl bonds (GO:0016798), catalytic activity, acting on a protein (GO:0140096)

GO Cellular Component (4): nucleus (GO:0005634), cytosol (GO:0005829), membrane (GO:0016020), cytoplasm (GO:0005737)

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure3
glycoprotein metabolic process2
hydrolase activity, hydrolyzing O-glycosyl compounds2
catalytic activity2
amino sugar metabolic process1
glycoprotein biosynthetic process1
protein catabolic process1
carbohydrate derivative catabolic process1
protein modification process1
protein metabolic process1
carbohydrate derivative metabolic process1
metabolic process1
hexosaminidase activity1
protein binding1
catalytic activity, acting on a protein1
acyltransferase activity1
hydrolase activity1
intracellular membrane-bounded organelle1
cytoplasm1
intracellular anatomical structure1

Protein interactions and networks

STRING

1752 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
OGAOGTO15294952
OGAAURKBQ96GD4927
OGAGM2AP17900857
OGAGUSBP08236830
OGAHEXBP07686814
OGAB2MP01884775
OGAHAVCR1Q96D42773
OGAARSBP15848761
OGAGFPT2O94808758
OGAGFPT1Q06210758
OGAAMBPP00977728
OGAALBP02768720
OGALCN2P30150720
OGACST3P01034718
OGAEP300Q09472712

IntAct

86 interactions, top by confidence:

ABTypeScore
EIF4EEIF4G3psi-mi:“MI:0914”(association)0.810
C1QTNF9C1QTNF9Bpsi-mi:“MI:0914”(association)0.780
CNOT3CNOT1psi-mi:“MI:0914”(association)0.740
CFTRESYT2psi-mi:“MI:2364”(proximity)0.710
OGAOGApsi-mi:“MI:0407”(direct interaction)0.610
OGAOGApsi-mi:“MI:0915”(physical association)0.610
STN1SMCO3psi-mi:“MI:0914”(association)0.530
SAMTORPER1psi-mi:“MI:0914”(association)0.530
LPAR1TMEM223psi-mi:“MI:0914”(association)0.530
SPSB4ARHGEF10psi-mi:“MI:0914”(association)0.530
OGATP53psi-mi:“MI:0407”(direct interaction)0.440
TNFAIP3LRRIQ3psi-mi:“MI:2364”(proximity)0.420
XPO7OGApsi-mi:“MI:0915”(physical association)0.400
LACTB2OGApsi-mi:“MI:0915”(physical association)0.400
OGAFKBP5psi-mi:“MI:0915”(physical association)0.400
OGANUDCD3psi-mi:“MI:0915”(physical association)0.400
OGApsi-mi:“MI:0915”(physical association)0.400
A2MOGApsi-mi:“MI:0915”(physical association)0.370
OGACDC37psi-mi:“MI:0915”(physical association)0.370
MAST1OGApsi-mi:“MI:0915”(physical association)0.370
RNF32OGApsi-mi:“MI:0915”(physical association)0.370
CSNK2BOGApsi-mi:“MI:0915”(physical association)0.370
GSK3BOGApsi-mi:“MI:0915”(physical association)0.370
E7COPEpsi-mi:“MI:0914”(association)0.350
Xpo7HAT1psi-mi:“MI:0914”(association)0.350
LRRK2psi-mi:“MI:0914”(association)0.350
CYLDOGApsi-mi:“MI:0914”(association)0.350

BioGRID (160): MGEA5 (Affinity Capture-MS), MGEA5 (Affinity Capture-MS), MGEA5 (Affinity Capture-MS), MGEA5 (Affinity Capture-MS), MGEA5 (Affinity Capture-MS), CDC37 (Co-fractionation), PITHD1 (Co-fractionation), MGEA5 (Affinity Capture-MS), MGEA5 (Proximity Label-MS), MGEA5 (Affinity Capture-MS), MGEA5 (Affinity Capture-MS), MGEA5 (Affinity Capture-MS), MGEA5 (Affinity Capture-MS), MGEA5 (Affinity Capture-MS), MGEA5 (Affinity Capture-MS)

ESM2 similar proteins: A0JMD0, A1A535, A1ZAB5, A2AIV2, A8E7C5, A8PJX4, A8XAA9, B0W2S0, B3MIW0, B3NPV8, B4GAM1, B4JW99, B4KT50, B4LQ23, B4MY63, B4P6P7, D3YVL2, E9PXF8, F4HS99, F4HZK4, F4J5S1, F4JKH6, O60502, O75153, O88379, P34466, P69735, Q0IHW8, Q0VA04, Q15042, Q17N71, Q291J5, Q5PQS3, Q5SW19, Q5TYW4, Q5U430, Q69YN4, Q6NTN5, Q6ZT12, Q7PZD5

Diamond homologs: O60502, Q0TR53, Q2CEE2, Q2CEE3, Q89ZI2, Q8VIJ5, Q8XL08, Q9EQQ9, B3TLD6, P0DTR4, P29767, Q02834

SIGNOR signaling

5 interactions.

AEffectBMechanism
OGA“down-regulates activity”G6PDdeglycosylation
OGA“up-regulates activity”PFKPdeglycosylation
OGA“up-regulates activity”PFKMdeglycosylation
OGA“up-regulates activity”PFKLdeglycosylation
OGA“up-regulates activity”PFKdeglycosylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance66
Likely benign3
Benign1

Top pathogenic / likely-pathogenic (0)

SpliceAI

3028 predictions. Top by Δscore:

VariantEffectΔscore
10:101787358:ACTC:Adonor_loss1.0000
10:101787360:TCA:Tdonor_loss1.0000
10:101787361:CA:Cdonor_loss1.0000
10:101787362:A:ACdonor_gain1.0000
10:101787363:C:CCdonor_gain1.0000
10:101787363:C:CGdonor_loss1.0000
10:101787452:C:CTacceptor_gain1.0000
10:101787453:A:Tacceptor_gain1.0000
10:101787520:TTTT:Tacceptor_gain1.0000
10:101787524:C:CCacceptor_gain1.0000
10:101791344:TATC:Tdonor_gain1.0000
10:101791345:A:ACdonor_gain1.0000
10:101791345:AT:Adonor_gain1.0000
10:101791345:ATCA:Adonor_gain1.0000
10:101791346:T:Cdonor_gain1.0000
10:101791352:A:ACdonor_gain1.0000
10:101791353:C:CCdonor_gain1.0000
10:101792942:CG:Cacceptor_gain1.0000
10:101793574:CTAT:Cdonor_gain1.0000
10:101793688:AGAG:Adonor_gain1.0000
10:101798061:T:TAdonor_gain1.0000
10:101798840:A:ACdonor_gain1.0000
10:101798841:C:CCdonor_gain1.0000
10:101800240:A:ACdonor_gain1.0000
10:101800241:C:CTdonor_gain1.0000
10:101800241:CT:Cdonor_gain1.0000
10:101800241:CTG:Cdonor_gain1.0000
10:101800241:CTGCT:Cdonor_gain1.0000
10:101800271:TGCA:Tdonor_gain1.0000
10:101800398:CAG:Cacceptor_gain1.0000

AlphaMissense

6069 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
10:101791044:A:TV769D1.000
10:101793946:C:AW679C1.000
10:101793946:C:GW679C1.000
10:101793948:A:GW679R1.000
10:101793948:A:TW679R1.000
10:101798031:A:GW645R1.000
10:101798031:A:TW645R1.000
10:101798145:A:GW607R1.000
10:101798145:A:TW607R1.000
10:101798897:A:GL585P1.000
10:101798951:A:GL567P1.000
10:101800278:A:GW387R1.000
10:101800278:A:TW387R1.000
10:101803778:C:AW331C1.000
10:101803778:C:GW331C1.000
10:101803780:A:GW331R1.000
10:101803780:A:TW331R1.000
10:101803808:G:CN321K1.000
10:101803808:G:TN321K1.000
10:101803826:A:CN315K1.000
10:101803826:A:TN315K1.000
10:101803830:G:CP314R1.000
10:101803830:G:TP314Q1.000
10:101803832:A:CN313K1.000
10:101803832:A:TN313K1.000
10:101803834:T:CN313D1.000
10:101803839:A:GL311P1.000
10:101803842:A:TV310D1.000
10:101803845:C:TG309E1.000
10:101803846:C:GG309R1.000

dbSNP variants (sampled 300 via entrez): RS1000059290 (10:101817285 G>A), RS1000224430 (10:101804565 G>A,T), RS1000234527 (10:101810934 G>A,T), RS1000349212 (10:101798596 T>C), RS1000403832 (10:101810630 C>T), RS1000468334 (10:101803445 T>A,C), RS1000514804 (10:101785269 C>T), RS1000605470 (10:101808107 C>CTG), RS1000681943 (10:101809508 G>A,C), RS1000808867 (10:101798409 T>C,G), RS1000914572 (10:101785083 C>A), RS1001140684 (10:101784439 CACG>C), RS1001162679 (10:101815692 A>C), RS1001170440 (10:101784242 C>T), RS1001197606 (10:101791793 A>G)

Disease associations

OMIM: gene MIM:604039 | 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):

StudyTraitp-value
GCST009524_180Household income (MTAG)1.000000e-08
GCST010138_11Raw vegetable consumption3.000000e-08

EFO canonical traits (2, from GWAS)

EFO IDTrait name
EFO:0009695household income
EFO:0008111diet measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5921 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 21 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL5095251CEPEROGNASTAT221

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Hydrolases & Lipases

Most potent curated ligand interactions (3 total), top 3:

LigandActionAffinityParameter
ceperognastatInhibition8.63pIC50
MK-8719Inhibition8.1pKi
thiamet-GInhibition7.68pKi

Binding affinities (BindingDB)

309 measured of 373 human assays (373 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
US8901087, 2KI0.05 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
US9695197, 4KI0.11 nMUS-9695197: Glycosidase inhibitors and uses thereof
US8901087, 27KI0.12 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,4R,5R,6R,7aS)-2-(azetidin-1-yl)-6-(hydroxymethyl)-3a,4,5,6,7,7a-hexahydro-1,3-benzoxazole-4,5-diolKI0.13 nMUS-9120781: Selective glycosidase inhibitors and uses thereof
US8901087, 191KI0.14 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aS,4S,5S,6S,7aR)-2-(dimethylamino)-6-[(1R)-1-hydroxyethyl]-3a,4,5,6,7,7a-hexahydro-1,3-benzothiazole-4,5-diolKI0.14 nMUS-9126957: Selective glycosidase inhibitors and uses thereof
US8901087, 95KI0.16 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-5-((R)-1-(4- benzylbenzyloxy)-2,2,2- trifluoroethyl)-2-(methylamino)- 5,6,7,7a-tetrahydro-3aH- pyrano[3,2-d]thiazole-6,7-diolKI0.16 nMUS-9611275: Permeable glycosidase inhibitors and uses thereof
(3aR,5R,6S,7R,7aR)-2-(dimethylamino)-5-[(1S)-1-hydroxyethyl]-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diolKI0.17 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
US8901087, 97KI0.17 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,5R,6S,7R,7aR)-2-(azetidin-1-yl)-5-[(1S)-1-hydroxyethyl]-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diolKI0.18 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-2-(dimethylamino)-5-((R)-1-methoxyethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diol & (3aR,5S,6S,7R,7aR)-2-(dimethylamino)-5-((S)-1-methoxyethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diolKI0.19 nMUS-9611275: Permeable glycosidase inhibitors and uses thereof
[(3aR,5S,6S,7S,7aR)-2-(dimethylamino)-7-phenylmethoxy-6-(phenylmethoxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazol-5-yl]-(1,3-dithian-2-yl)methanolKI0.19 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
US9120781, 26KI0.2 nMUS-9120781: Selective glycosidase inhibitors and uses thereof
(3aR,5R,6S,7R,7aR)-2-(dimethylamino)-5-[(1S)-1-hydroxyprop-2-enyl]-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diolKI0.22 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,4R,5R,6R,7aS)-2-(dimethylamino)-6-[(1S)-1-hydroxyethyl]-3a,4,5,6,7,7a-hexahydro-1,3-benzoxazole-4,5-diolKI0.26 nMUS-9126957: Selective glycosidase inhibitors and uses thereof
US9126957, 6KI0.26 nMUS-9126957: Selective glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-2-(dimethylamino)-5-[(1R)-2,2,2-trifluoro-1-hydroxyethyl]-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diolKI0.3 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,5R,6S,7R,7aR)-2-(dimethylamino)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diolKI0.3 nMUS-9815861: Selective glycosidase inhibitors and uses thereof
(3aR,5R,6R,7S,7aR)-2-(dimethylamino)-7-fluoro-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazol-6-olKI0.3 nMUS-9409924: Selective glycosidase inhibitors and uses thereof
US9409924, 34KI0.3 nMUS-9409924: Selective glycosidase inhibitors and uses thereof
(3aR,5R,6S,7R,7aR)-2-[ethyl(methyl)amino]-5-(1-hydroxyethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diolKI0.33 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
US8901087, 13KI0.4 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
US9409924, (3aR,5R,6R,7S,7aR)-2-(ethylamino)-7-fluoro-5-(hydroxymethyl)-3aH,5H,6H,7H,7aH-pyrano[3,2-d][1,3]thiazol-6-olKI0.4 nMUS-9409924: Selective glycosidase inhibitors and uses thereof
(3AR,5R,6S,7R,7AR)-2-(ETHYLAMINO)-5-(HYDROXYMETHYL)-5,6,7,7A-TETRAHYDRO-3AH-PYRANO[3,2-D][1,3]THIAZOLE-6,7-DIOLKI0.4 nMUS-9243020: Selective glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-2-[ethyl(methyl)amino]-5-[(1R)-2,2,2-trifluoro-1-hydroxyethyl]-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diolKI0.44 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,5R,6S,7R,7aR)-2-(dimethylamino)-5-[(1S)-1-hydroxy-2-methylprop-2-enyl]-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diolKI0.45 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-2- (dimethylamino)-5-((R)-2,2,2- trifluoro-1-(4-methoxy-3,5- dimethylbenzyloxy)ethyl)- 5,6,7,7a-tetrahydro-3aH- pyrano[3,2-d]thiazole-6,7-diolKI0.45 nMUS-9611275: Permeable glycosidase inhibitors and uses thereof
(3aR,5R,6S,7R,7aR)-2-(azetidin-1-yl)-5-[(1S)-1-hydroxyprop-2-enyl]-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diolKI0.5 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,4R,5R,6R,7aS)-2-(dimethylamino)-6-(hydroxymethyl)-3a,4,5,6,7,7a-hexahydro-1,3-benzothiazole-4,5-diolKI0.5 nMUS-9120781: Selective glycosidase inhibitors and uses thereof
US9243020, 17KI0.5 nMUS-9815861: Selective glycosidase inhibitors and uses thereof
(3aR,5R,6S,7R,7aR)-5-[(1S)-1-hydroxyethyl]-2-pyrrolidin-1-yl-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diolKI0.53 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-2- (methylamino)-5-((R)-2,2,2- trifluoro-1-(4-(3- fluoropropyl)benzyloxy)ethyl)- 5,6,7,7a-tetrahydro-3aH- pyrano[3,2-d]thiazole-6,7-diolKI0.59 nMUS-9611275: Permeable glycosidase inhibitors and uses thereof
US9120781, 9KI0.6 nMUS-9120781: Selective glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-2- (dimethylamino)-5-((R)-2,2,2- trifluoro-1-(4-(2- fluoroethyl)benzyloxy)ethyl)- 5,6,7,7a-tetrahydro-3aH- pyrano[3,2-d]thiazole-6,7-diolKI0.61 nMUS-9611275: Permeable glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-2- (dimethylamino)-5-((R)-2,2,2- trifluoro-1-(4-(2- fluoroethoxy)benzyloxy)ethyl)- 5,6,7,7a-tetrahydro-3aH- pyrano[3,2-d]thiazole-6,7-diolKI0.65 nMUS-9611275: Permeable glycosidase inhibitors and uses thereof
US8901087, 8KI0.68 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
N-[1-(7-{bis[(4-methoxyphenyl)methyl]amino}heptyl)-4,5-dihydroxy-6-(hydroxymethyl)piperidin-3-yl]acetamide, 4KI0.69 nM
US8901087, 25KI0.7 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
US8901087, 53KI0.7 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,4R,5R,6S,7aS)-2-(azetidin-1-yl)-6-(difluoromethyl)-3a,4,5,6,7,7a-hexahydro-1,3-benzoxazole-4,5-diolKI0.7 nMUS-9199949: Selective glycosidase inhibitors and uses thereof
US9409924, 38KI0.7 nMUS-9409924: Selective glycosidase inhibitors and uses thereof
(3aR,5R,6S,7S,7aR)-5- (hydroxymethyl)-2-(methylamino)- 5,6,7,7a-tetrahydro-3aH-pyrano[3,2- d]thiazole-6,7-diolKI0.7 nMUS-9701693: Selective glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-2- (methylamino)-5-((R)-2,2,2- trifluoro-1-(4-(2- fluoroethyl)benzyloxy)ethyl)- 5,6,7,7a-tetrahydro-3aH- pyrano[3,2-d]thiazole-6,7-diolKI0.71 nMUS-9611275: Permeable glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-2- (dimethylamino)-5-((R)-2,2,2- trifluoro-1-(4-(3- fluoropropyl)benzyloxy)ethyl)- 5,6,7,7a-tetrahydro-3aH- pyrano[3,2-d]thiazole-6,7-diolKI0.78 nMUS-9611275: Permeable glycosidase inhibitors and uses thereof
US8901087, 181KI0.8 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
US8901087, 141KI0.82 nMUS-8901087: Selective glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-5-((R)-1-(4-(allyloxy)benzyloxy)-2,2,2-trifluoroethyl)-2-(dimethylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diolKI0.82 nMUS-9611275: Permeable glycosidase inhibitors and uses thereof
(3aR,5S,6S,7R,7aR)-2- (dimethylamino)-5-((R)-2,2,2- trifluoro-1-(4-methoxy-3- (trifluoromethyl)benzyloxy)ethyl)- 5,6,7,7a-tetrahydro-3aH- pyrano[3,2-d]thiazole-6,7-diolKI0.84 nMUS-9611275: Permeable glycosidase inhibitors and uses thereof
US8901087, 3KI0.9 nMUS-8901087: Selective glycosidase inhibitors and uses thereof

ChEMBL bioactivities

985 potent at pChembl≥5 of 991 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
10.30Ki0.05nMCHEMBL3647355
10.12Ki0.075nMCHEMBL5978885
10.02Ki0.095nMCHEMBL5982879
9.96Ki0.11nMCHEMBL6019753
9.93Ki0.117nMCHEMBL5833418
9.92Ki0.12nMCHEMBL3647362
9.89Ki0.13nMCHEMBL4109135
9.85Ki0.14nMCHEMBL3647388
9.85Ki0.14nMCHEMBL3952267
9.80Ki0.16nMCHEMBL3647380
9.80Ki0.16nMCHEMBL6029490
9.78Ki0.167nMCHEMBL5978885
9.77Ki0.17nMCHEMBL3647354
9.77Ki0.17nMCHEMBL3647381
9.74Ki0.18nMCHEMBL3647375
9.72Ki0.19nMCHEMBL3647392
9.72Ki0.19nMCHEMBL5906193
9.70Ki0.2nMCHEMBL4115664
9.67IC500.214nMCHEMBL4779747
9.66Ki0.22nMCHEMBL3647370
9.62Ki0.241nMCHEMBL6064515
9.59Ki0.26nMCHEMBL3986688
9.59Ki0.26nMCHEMBL3931073
9.57Ki0.268nMCHEMBL6057396
9.54Ki0.287nMCHEMBL5828721
9.53Ki0.294nMCHEMBL5782940
9.52Ki0.3nMCHEMBL3647359
9.52Ki0.3nMCHEMBL4112819
9.52Ki0.3nMCHEMBL4110353
9.52Ki0.3nMCHEMBL3929320
9.49Ki0.324nMCHEMBL5944832
9.48Ki0.33nMCHEMBL3647368
9.47IC500.34nMCHEMBL5591488
9.44Ki0.36nMCHEMBL4443587
9.41IC500.385nMCHEMBL4759587
9.41Ki0.392nMCHEMBL5783742
9.41Ki0.387nMCHEMBL5861625
9.41Ki0.389nMCHEMBL5752657
9.40Ki0.4nMCHEMBL3647360
9.40Ki0.4nMCHEMBL1213603
9.40Ki0.4nMCHEMBL4108448
9.39IC500.41nMCHEMBL1213603
9.39Ki0.41nMCHEMBL1213603
9.39Ki0.411nMCHEMBL5879675
9.37IC500.43nMCHEMBL5591695
9.37Ki0.427nMCHEMBL5789908
9.37Ki0.43nMCHEMBL5777939
9.36Ki0.44nMCHEMBL3647390
9.35Ki0.45nMCHEMBL3647371
9.35Ki0.45nMCHEMBL5763051

PubChem BioAssay actives

255 with measured affinity, of 400 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.

CompoundAssayTypeValueUnit
1-[2-[(3R,5S)-1-[(6-fluoro-2-methyl-1,3-benzothiazol-5-yl)methyl]-5-methylpyrrolidin-3-yl]oxy-5,7-dihydropyrrolo[3,4-b]pyridin-6-yl]ethanone1710173: Inhibition of full-length human N-terminal poly-His tagged OGA expressed in baculovirus infected Sf9 cells using FD-GlcNAc as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assayic500.0002uM
N-[5-[[4-[2-(1,2,3,4-tetrahydro-1,7-naphthyridin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0003uM
(3aR,5R,6S,7R,7aR)-2-ethylimino-5-(hydroxymethyl)-1,3a,5,6,7,7a-hexahydropyrano[3,2-d][1,3]thiazole-6,7-diol1527147: Inhibition of human O-GlcNAcaseic500.0004uM
1-[2-[(3R,5S)-1-[(1S)-1-(6-fluoro-2-methyl-1,3-benzothiazol-5-yl)ethyl]-5-methylpyrrolidin-3-yl]oxy-5,7-dihydropyrrolo[3,4-b]pyridin-6-yl]ethanone1710173: Inhibition of full-length human N-terminal poly-His tagged OGA expressed in baculovirus infected Sf9 cells using FD-GlcNAc as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assayic500.0004uM
N-[5-[[4-[2-[2-(dimethylamino)pyrimidin-5-yl]ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0004uM
(3aR,5S,6S,7R,7aR)-5-(difluoromethyl)-2-(methylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol1558062: Inhibition of recombinant human OGAki0.0004uM
1-[2-[(3R,5S)-1-[(6-fluoro-2-methyl-1,3-benzothiazol-5-yl)methyl]-5-methylpyrrolidin-3-yl]oxy-5,7-dihydropyrrolo[3,4-d]pyrimidin-6-yl]ethanone1710173: Inhibition of full-length human N-terminal poly-His tagged OGA expressed in baculovirus infected Sf9 cells using FD-GlcNAc as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assayic500.0005uM
1-[2-[(3R,5S)-1-[(1S)-1-(6-fluoro-2-methyl-1,3-benzothiazol-5-yl)ethyl]-5-methylpyrrolidin-3-yl]oxy-5,7-dihydropyrrolo[3,4-d]pyrimidin-6-yl]ethanone1710173: Inhibition of full-length human N-terminal poly-His tagged OGA expressed in baculovirus infected Sf9 cells using FD-GlcNAc as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assayic500.0005uM
(3aR,5R,6R,7S,7aR)-7-fluoro-5-(hydroxymethyl)-2-(methylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazol-6-ol1558062: Inhibition of recombinant human OGAki0.0005uM
(3aR,5S,6S,7R,7aR)-5-(fluoromethyl)-2-methylimino-1,3a,5,6,7,7a-hexahydropyrano[3,2-d][1,3]thiazole-6,7-diol1558062: Inhibition of recombinant human OGAki0.0006uM
1-[3-[(3R,5S)-1-[(6-fluoro-2-methyl-1,3-benzothiazol-5-yl)methyl]-5-methylpyrrolidin-3-yl]oxy-5,7-dihydropyrrolo[3,4-b]pyridin-6-yl]ethanone1710173: Inhibition of full-length human N-terminal poly-His tagged OGA expressed in baculovirus infected Sf9 cells using FD-GlcNAc as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assayic500.0006uM
N-[5-[[4-[2-(8-methylquinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0007uM
1-[6-[(3R,5S)-1-[(6-fluoro-2-methyl-1,3-benzothiazol-5-yl)methyl]-5-methylpyrrolidin-3-yl]oxy-1,3-dihydropyrrolo[3,4-c]pyridin-2-yl]ethanone1710173: Inhibition of full-length human N-terminal poly-His tagged OGA expressed in baculovirus infected Sf9 cells using FD-GlcNAc as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assayic500.0008uM
N-[5-[[4-[2-(1,2,3,4-tetrahydroquinolin-7-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0008uM
N-[5-[[4-[2-(7-methylquinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0015uM
N-[5-[[4-[2-(2-oxo-3,4-dihydro-1H-quinolin-5-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0017uM
N-[5-[[4-[2-(1-benzofuran-7-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0018uM
N-[4-fluoro-5-[[(2S,4S)-2-methyl-4-[(5-methyl-1,3,4-oxadiazol-2-yl)methoxy]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0021uM
N-[4-fluoro-5-[[(2S,4S)-2-methyl-4-[(5-methyl-1,2,4-oxadiazol-3-yl)methoxy]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114327: Inhibition of full length N-terminal his-tagged human OGA expressed in baculovirus expression system preincubated for for 30 mins followed by substrate addition and measured after 60 mins by fluorescence based analysisic500.0024uM
(3aR,5S,6S,7R,7aR)-5-(difluoromethyl)-2-(dimethylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol1558062: Inhibition of recombinant human OGAki0.0024uM
(3aR,5R,6S,7R,7aR)-5-(hydroxymethyl)-2-[methyl(prop-2-enyl)amino]-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol1558062: Inhibition of recombinant human OGAki0.0028uM
(3aR,5R,6R,7R,7aR)-7-fluoro-5-(hydroxymethyl)-2-methylimino-1,3a,5,6,7,7a-hexahydropyrano[3,2-d][1,3]thiazol-6-ol1558062: Inhibition of recombinant human OGAki0.0030uM
N-[5-[[4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0030uM
N-[5-[[4-[2-(8-fluoro-1,2,3,4-tetrahydroquinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0032uM
(3aR,5R,6S,7R,7aR)-2-(azetidin-1-yl)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol1558062: Inhibition of recombinant human OGAki0.0033uM
N-[5-[[4-[2-[6-(dimethylamino)-3-pyridinyl]ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0035uM
N-[5-[[4-[2-[6-(trifluoromethyl)pyrimidin-4-yl]ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0036uM
N-[5-[[(5S)-2-(2,6-dimethyl-4-pyridinyl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide1537422: Inhibition of recombinant human full length OGA using FM-GlcNAc as substrate preincubated for 60 mins followed by substrate addition and measured after 6 hrs by fluorescence assayic500.0037uM
N-[5-[[4-[2-(2-pyrrolidin-1-ylpyrimidin-5-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0037uM
N-[5-[[2-(3,5-dimethyl-2-pyridinyl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide1537422: Inhibition of recombinant human full length OGA using FM-GlcNAc as substrate preincubated for 60 mins followed by substrate addition and measured after 6 hrs by fluorescence assayic500.0039uM
(2E)-N-[(5R,6R,7R,8S)-6,7-dihydroxy-5-(hydroxymethyl)-2-(2-phenylethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridin-8-yl]penta-2,4-dienamide1378936: Competitive inhibition of human O-GlcNAcase by Lineweaver-Burk analysiski0.0041uM
N-[5-[[4-[2-(2,6-dimethyl-3-pyridinyl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0044uM
N-[5-[[4-[2-(5,6,7,8-tetrahydro-1,5-naphthyridin-2-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0046uM
N-[5-[[4-[2-(1,2,3,4-tetrahydroquinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0049uM
(3aR,5S,6S,7R,7aR)-5-(difluoromethyl)-2-(propylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol1558062: Inhibition of recombinant human OGAki0.0053uM
N-[5-[[4-[2-(4,6-dimethyl-2-pyridinyl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0054uM
(3aR,5R,6S,7R,7aR)-2-[ethyl(methyl)amino]-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol1558062: Inhibition of recombinant human OGAki0.0055uM
(3aR,5R,6S,7R,7aR)-2-(2-fluoroethylamino)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol1558062: Inhibition of recombinant human OGAki0.0056uM
N-[5-[[2-(2,6-dimethyl-4-pyridinyl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide1537422: Inhibition of recombinant human full length OGA using FM-GlcNAc as substrate preincubated for 60 mins followed by substrate addition and measured after 6 hrs by fluorescence assayic500.0060uM
(3aR,5S,6S,7R,7aR)-5-(difluoromethyl)-2-ethylimino-1,3a,5,6,7,7a-hexahydropyrano[3,2-d][1,3]thiazole-6,7-diol1527147: Inhibition of human O-GlcNAcaseic500.0079uM
N-[5-[[4-[2-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0080uM
N-[5-[[4-[2-[2-(trifluoromethyl)pyrimidin-5-yl]ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0087uM
N-[5-[[4-[2-(6-pyrrolidin-1-yl-3-pyridinyl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0088uM
N-[5-[[4-[2-(2,3-dihydro-1-benzofuran-5-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0089uM
N-[5-[[4-[2-(7-fluoro-1,2,3,4-tetrahydroquinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0089uM
(3aR,5S,6S,7R,7aR)-2-(dimethylamino)-5-(fluoromethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol1558062: Inhibition of recombinant human OGAki0.0090uM
(3aR,5R,6S,7aR)-5-(hydroxymethyl)-2-(methylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazol-6-ol1558062: Inhibition of recombinant human OGAki0.0094uM
N-[5-[[4-[2-(1,3-benzodioxol-5-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide2114285: Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysisic500.0095uM
(3aR,5R,6S,7R,7aR)-5-(hydroxymethyl)-2-methyl-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol515842: Inhibition of human O-GlcNAcase after 5 mins by Lineweaver-Burke plot analysiski0.0100uM
N-[5-[4-[(1S)-1-(1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl]-1,3,4-thiadiazol-2-yl]acetamide2114326: Inhibition of human OGAic500.0102uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Valproic Acidaffects cotreatment, increases expression, decreases expression, affects expression6
bisphenol Adecreases expression, increases expression, increases methylation4
sodium arsenitedecreases expression, increases expression4
Acetaminophenaffects expression, increases expression3
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxideaffects expression, decreases expression3
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamideaffects cotreatment, increases expression, decreases expression2
bisphenol Sincreases expression, affects cotreatment, decreases expression2
Leflunomideincreases expression2
Rotenonedecreases expression2
Tretinoindecreases expression, increases expression2
aristolochic acid Idecreases expression1
GSK-J4increases expression1
FR900359affects phosphorylation1
bisphenol Faffects cotreatment, decreases expression1
dicrotophosdecreases expression1
beauvericinincreases expression1
triphenyl phosphateaffects expression1
deoxynivalenolincreases expression1
quercitrinincreases expression1
trichostatin Aaffects expression1
methylparabenincreases expression1
sulforaphaneincreases expression1
tris(1,3-dichloro-2-propyl)phosphateincreases expression1
nickel chlorideincreases expression1
beta-methylcholineaffects expression1
epigallocatechin gallatedecreases expression1
tamibarotenedecreases expression1
di-n-butylphosphoric acidaffects expression1
chloropicrinincreases expression1
K 7174increases expression1

ChEMBL screening assays

89 unique, capped per target: 89 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1218573BindingInhibition of human O-GlcNAcaseA potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. — Nat Chem Biol

Cellosaurus cell lines

3 cell lines: 3 cancer cell line

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

CellosaurusNameCategorySex
CVCL_B1ZHAbcam HeLa OGA KOCancer cell lineFemale
CVCL_SY28HAP1 MGEA5 (-) 1Cancer cell lineMale
CVCL_XQ53HAP1 MGEA5 (-) 2Cancer cell lineMale

Clinical trials (associated diseases)

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

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.