OGA
gene geneOn this page
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
| Field | Value |
|---|---|
| HGNC ID | HGNC:7056 |
| Approved symbol | OGA |
| Name | O-GlcNAcase |
| Location | 10q24.32 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | MEA5, NCOAT |
| Ensembl gene | ENSG00000198408 |
| Ensembl biotype | protein_coding |
| OMIM | 604039 |
| Entrez | 10724 |
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
| Exon | Start | End |
|---|---|---|
| ENSE00000721914 | 101798842 | 101799455 |
| ENSE00000721926 | 101810184 | 101810314 |
| ENSE00000721929 | 101813030 | 101813127 |
| ENSE00000721932 | 101813555 | 101813606 |
| ENSE00000811427 | 101793913 | 101793998 |
| ENSE00000811428 | 101800242 | 101800400 |
| ENSE00000811429 | 101803735 | 101804019 |
| ENSE00000811430 | 101806045 | 101806143 |
| ENSE00003471052 | 101792839 | 101792943 |
| ENSE00003531550 | 101807730 | 101807901 |
| ENSE00003533549 | 101787364 | 101787523 |
| ENSE00003538234 | 101791354 | 101791439 |
| ENSE00003640803 | 101797980 | 101798154 |
| ENSE00003691121 | 101790896 | 101791088 |
| ENSE00003847848 | 101817824 | 101818444 |
| ENSE00003848061 | 101784450 | 101786587 |
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 ID | TPM avg | Samples expressed |
|---|---|---|
| 111108 | 36.4853 | 1807 |
| 111105 | 2.0225 | 904 |
| 111107 | 1.7255 | 970 |
| 111104 | 1.5539 | 618 |
Top tissues by expression
294 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| sperm | CL:0000019 | 99.10 | gold quality |
| skin of abdomen | UBERON:0001416 | 98.64 | gold quality |
| skin of leg | UBERON:0001511 | 98.64 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 98.58 | gold quality |
| cerebellar cortex | UBERON:0002129 | 98.56 | gold quality |
| tibial nerve | UBERON:0001323 | 98.54 | gold quality |
| right uterine tube | UBERON:0001302 | 98.49 | gold quality |
| mucosa of stomach | UBERON:0001199 | 98.47 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 98.46 | gold quality |
| left ovary | UBERON:0002119 | 98.44 | gold quality |
| ventricular zone | UBERON:0003053 | 98.43 | gold quality |
| colonic epithelium | UBERON:0000397 | 98.39 | gold quality |
| cortical plate | UBERON:0005343 | 98.38 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 98.31 | gold quality |
| ganglionic eminence | UBERON:0004023 | 98.30 | gold quality |
| right ovary | UBERON:0002118 | 98.28 | gold quality |
| calcaneal tendon | UBERON:0003701 | 98.28 | gold quality |
| endocervix | UBERON:0000458 | 98.27 | gold quality |
| male germ cell | CL:0000015 | 98.25 | gold quality |
| cerebellum | UBERON:0002037 | 98.23 | gold quality |
| ectocervix | UBERON:0012249 | 98.20 | gold quality |
| right coronary artery | UBERON:0001625 | 98.11 | gold quality |
| right lung | UBERON:0002167 | 98.10 | gold quality |
| body of uterus | UBERON:0009853 | 98.10 | gold quality |
| vagina | UBERON:0000996 | 98.03 | gold quality |
| granulocyte | CL:0000094 | 97.99 | gold quality |
| tendon | UBERON:0000043 | 97.99 | gold quality |
| popliteal artery | UBERON:0002250 | 97.99 | gold quality |
| tibial artery | UBERON:0007610 | 97.98 | gold quality |
| nipple | UBERON:0002030 | 97.97 | gold quality |
Single-cell (SCXA)
Detected in 4 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-GEOD-75367 | no | 2938.59 |
| E-MTAB-6075 | no | 1398.35 |
| E-GEOD-106540 | no | 593.49 |
| E-ANND-3 | no | 0.00 |
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):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-7110-3P | 100.00 | 73.18 | 2486 |
| HSA-MIR-3064-3P | 100.00 | 70.09 | 1254 |
| HSA-MIR-6873-3P | 100.00 | 71.42 | 2626 |
| HSA-MIR-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-30A-5P | 100.00 | 76.31 | 3233 |
| HSA-MIR-30B-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30C-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30D-5P | 100.00 | 76.32 | 3233 |
| HSA-MIR-30E-5P | 100.00 | 76.32 | 3242 |
| HSA-MIR-513B-5P | 99.99 | 69.96 | 2150 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-520G-5P | 99.99 | 66.76 | 658 |
| HSA-MIR-371B-5P | 99.99 | 75.34 | 4759 |
| HSA-MIR-520D-5P | 99.98 | 73.34 | 4883 |
| HSA-MIR-524-5P | 99.98 | 73.43 | 4882 |
| HSA-MIR-27A-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-27B-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-9985 | 99.98 | 72.11 | 2939 |
| HSA-MIR-5696 | 99.98 | 72.36 | 4487 |
| HSA-MIR-373-5P | 99.98 | 75.36 | 4753 |
| HSA-MIR-616-5P | 99.98 | 75.58 | 4775 |
| HSA-MIR-3148 | 99.97 | 75.06 | 6478 |
| HSA-MIR-548AJ-3P | 99.96 | 73.38 | 5345 |
| HSA-MIR-548X-3P | 99.96 | 73.38 | 5345 |
| HSA-MIR-548AA | 99.96 | 70.64 | 3753 |
| HSA-MIR-548AP-3P | 99.96 | 70.64 | 3753 |
| HSA-MIR-548T-3P | 99.96 | 70.64 | 3753 |
| HSA-MIR-128-3P | 99.95 | 71.17 | 2484 |
| HSA-MIR-216A-3P | 99.95 | 71.19 | 2505 |
| HSA-MIR-9718 | 99.94 | 68.91 | 918 |
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
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | oga | ENSDARG00000074686 |
| mus_musculus | Oga | ENSMUSG00000025220 |
| rattus_norvegicus | Oga | ENSRNOG00000017822 |
| drosophila_melanogaster | Oga | FBGN0038870 |
| caenorhabditis_elegans | WBGENE00020596 |
Protein
Protein identifiers
Protein O-GlcNAcase — O60502 (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 ID | Names | Canonical? |
|---|---|---|
| O60502-1 | 1 | yes |
| O60502-2 | 2 | |
| O60502-3 | 3, MGEA5s | |
| O60502-4 | 4 |
RefSeq proteins (2): NP_001135906, NP_036347* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR011496 | O-GlcNAcase_cat | Domain |
| IPR016181 | Acyl_CoA_acyltransferase | Homologous_superfamily |
| IPR017853 | GH_hydrolase_sf | Homologous_superfamily |
| IPR051822 | Glycosyl_Hydrolase_84 | Family |
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.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| 4-NITROPHENYL N-ACETYL-BETA-D-GLUCOSAMINIDE | 0.016–36 | 38 |
| 4-METHYLUMBELLIFERYL N-ACETYL-BETA-D-GLUCOSAMINI | 0.0029–1.4 | 12 |
| HYALURONAN | 0.038–0.367 | 11 |
| 3,4-DINITROPHENYL N-ACETYL-BETA-D-GLUCOSAMINIDE | 0.21–0.56 | 4 |
| 3-FLUORO-4-NITROPHENYL N-ACETYL-BETA-D-GLUCOSAMI | 0.3–0.73 | 4 |
| 4-METHYLUMBELLIFERYL-N-ACETYL-BETA-D-GLUCOSAMINI | 0.0029–0.1 | 3 |
| 3-NITROPHENYL N-ACETYL-BETA-D-GLUCOSAMINIDE | 0.47–0.95 | 2 |
| 4-METHYLUMBELLIFERYL 2-ACETAMIDO-2-DEOXY-BETA-D- | 0.08–1 | 2 |
| FLUORESCEIN DI(N-ACETYL-BETA-D-GLUCOSAMINIDE) | 0.0849–2.1 | 2 |
| N-ACETYL-BETA-D-GLUCOSAMINE | 1.5–3.6 | 2 |
| PHENYL N-ACETYL-BETA-D-GLUCOSAMINIDE | 0.62–0.95 | 2 |
| 4-CHLOROPHENYL N-ACETYL-BETA-D-GLUCOSAMINIDE | 0.56 | 1 |
| 4-METHYLUMBELLIFERYL N-DIFLUOROACETYL-BETA-D-GLU | 0.45 | 1 |
| 4-METHYLUMBELLIFERYL N-FLUOROACETYL-BETA-D-GLUCO | 0.49 | 1 |
| 4-METHYLUMBELLIFERYL N-TRIFLUOROACETYL-BETA-D-GL | 0.38 | 1 |
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.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 5UN8 | X-RAY DIFFRACTION | 2.13 |
| 5M7U | X-RAY DIFFRACTION | 2.3 |
| 5M7R | X-RAY DIFFRACTION | 2.35 |
| 5M7S | X-RAY DIFFRACTION | 2.4 |
| 7OU6 | X-RAY DIFFRACTION | 2.41 |
| 5TKE | X-RAY DIFFRACTION | 2.48 |
| 5UN9 | X-RAY DIFFRACTION | 2.5 |
| 8P0L | X-RAY DIFFRACTION | 2.5 |
| 9BA8 | X-RAY DIFFRACTION | 2.54 |
| 2YDQ | X-RAY DIFFRACTION | 2.6 |
| 5M7T | X-RAY DIFFRACTION | 2.6 |
| 5VVO | X-RAY DIFFRACTION | 2.6 |
| 5VVU | X-RAY DIFFRACTION | 2.7 |
| 9BA9 | X-RAY DIFFRACTION | 2.75 |
| 5UHP | X-RAY DIFFRACTION | 2.79 |
| 5VVT | X-RAY DIFFRACTION | 2.8 |
| 5VVV | X-RAY DIFFRACTION | 2.8 |
| 6PM9 | X-RAY DIFFRACTION | 2.86 |
| 5VVX | X-RAY DIFFRACTION | 2.9 |
| 5UHK | X-RAY DIFFRACTION | 2.97 |
| 9NE4 | ELECTRON MICROSCOPY | 2.98 |
| 9NE5 | ELECTRON MICROSCOPY | 3.05 |
| 9QEN | ELECTRON MICROSCOPY | 3.08 |
| 5UHL | X-RAY DIFFRACTION | 3.14 |
| 5UHO | X-RAY DIFFRACTION | 3.21 |
| 6HKI | X-RAY DIFFRACTION | 3.3 |
| 9NE2 | ELECTRON MICROSCOPY | 3.63 |
| 7YEH | ELECTRON MICROSCOPY | 3.92 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O60502-F1 | 76.02 | 0.55 |
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):
| Position | Phenotype |
|---|---|
| 69 | strongly reduces affinity for glycopeptide substrates. nearly abolishes enzyme activity. |
| 174 | nearly abolishes enzyme activity. |
| 175 | nearly abolishes enzyme activity. |
| 255 | nearly abolishes enzyme activity. |
| 286 | nearly abolishes enzyme activity. |
| 287 | nearly abolishes enzyme activity. |
| 413 | abrogates cleavage by caspase-3. |
| 679 | nearly 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:
| Category | Terms |
|---|---|
| cellular anatomical structure | 3 |
| glycoprotein metabolic process | 2 |
| hydrolase activity, hydrolyzing O-glycosyl compounds | 2 |
| catalytic activity | 2 |
| amino sugar metabolic process | 1 |
| glycoprotein biosynthetic process | 1 |
| protein catabolic process | 1 |
| carbohydrate derivative catabolic process | 1 |
| protein modification process | 1 |
| protein metabolic process | 1 |
| carbohydrate derivative metabolic process | 1 |
| metabolic process | 1 |
| hexosaminidase activity | 1 |
| protein binding | 1 |
| catalytic activity, acting on a protein | 1 |
| acyltransferase activity | 1 |
| hydrolase activity | 1 |
| intracellular membrane-bounded organelle | 1 |
| cytoplasm | 1 |
| intracellular anatomical structure | 1 |
Protein interactions and networks
STRING
1752 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| OGA | OGT | O15294 | 952 |
| OGA | AURKB | Q96GD4 | 927 |
| OGA | GM2A | P17900 | 857 |
| OGA | GUSB | P08236 | 830 |
| OGA | HEXB | P07686 | 814 |
| OGA | B2M | P01884 | 775 |
| OGA | HAVCR1 | Q96D42 | 773 |
| OGA | ARSB | P15848 | 761 |
| OGA | GFPT2 | O94808 | 758 |
| OGA | GFPT1 | Q06210 | 758 |
| OGA | AMBP | P00977 | 728 |
| OGA | ALB | P02768 | 720 |
| OGA | LCN2 | P30150 | 720 |
| OGA | CST3 | P01034 | 718 |
| OGA | EP300 | Q09472 | 712 |
IntAct
86 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| EIF4E | EIF4G3 | psi-mi:“MI:0914”(association) | 0.810 |
| C1QTNF9 | C1QTNF9B | psi-mi:“MI:0914”(association) | 0.780 |
| CNOT3 | CNOT1 | psi-mi:“MI:0914”(association) | 0.740 |
| CFTR | ESYT2 | psi-mi:“MI:2364”(proximity) | 0.710 |
| OGA | OGA | psi-mi:“MI:0407”(direct interaction) | 0.610 |
| OGA | OGA | psi-mi:“MI:0915”(physical association) | 0.610 |
| STN1 | SMCO3 | psi-mi:“MI:0914”(association) | 0.530 |
| SAMTOR | PER1 | psi-mi:“MI:0914”(association) | 0.530 |
| LPAR1 | TMEM223 | psi-mi:“MI:0914”(association) | 0.530 |
| SPSB4 | ARHGEF10 | psi-mi:“MI:0914”(association) | 0.530 |
| OGA | TP53 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| TNFAIP3 | LRRIQ3 | psi-mi:“MI:2364”(proximity) | 0.420 |
| XPO7 | OGA | psi-mi:“MI:0915”(physical association) | 0.400 |
| LACTB2 | OGA | psi-mi:“MI:0915”(physical association) | 0.400 |
| OGA | FKBP5 | psi-mi:“MI:0915”(physical association) | 0.400 |
| OGA | NUDCD3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| OGA | psi-mi:“MI:0915”(physical association) | 0.400 | |
| A2M | OGA | psi-mi:“MI:0915”(physical association) | 0.370 |
| OGA | CDC37 | psi-mi:“MI:0915”(physical association) | 0.370 |
| MAST1 | OGA | psi-mi:“MI:0915”(physical association) | 0.370 |
| RNF32 | OGA | psi-mi:“MI:0915”(physical association) | 0.370 |
| CSNK2B | OGA | psi-mi:“MI:0915”(physical association) | 0.370 |
| GSK3B | OGA | psi-mi:“MI:0915”(physical association) | 0.370 |
| E7 | COPE | psi-mi:“MI:0914”(association) | 0.350 |
| Xpo7 | HAT1 | psi-mi:“MI:0914”(association) | 0.350 |
| LRRK2 | psi-mi:“MI:0914”(association) | 0.350 | |
| CYLD | OGA | psi-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.
| A | Effect | B | Mechanism |
|---|---|---|---|
| OGA | “down-regulates activity” | G6PD | deglycosylation |
| OGA | “up-regulates activity” | PFKP | deglycosylation |
| OGA | “up-regulates activity” | PFKM | deglycosylation |
| OGA | “up-regulates activity” | PFKL | deglycosylation |
| OGA | “up-regulates activity” | PFK | deglycosylation |
Disease & clinical
Clinical variants and AI predictions
ClinVar
88 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 66 |
| Likely benign | 3 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
3028 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 10:101787358:ACTC:A | donor_loss | 1.0000 |
| 10:101787360:TCA:T | donor_loss | 1.0000 |
| 10:101787361:CA:C | donor_loss | 1.0000 |
| 10:101787362:A:AC | donor_gain | 1.0000 |
| 10:101787363:C:CC | donor_gain | 1.0000 |
| 10:101787363:C:CG | donor_loss | 1.0000 |
| 10:101787452:C:CT | acceptor_gain | 1.0000 |
| 10:101787453:A:T | acceptor_gain | 1.0000 |
| 10:101787520:TTTT:T | acceptor_gain | 1.0000 |
| 10:101787524:C:CC | acceptor_gain | 1.0000 |
| 10:101791344:TATC:T | donor_gain | 1.0000 |
| 10:101791345:A:AC | donor_gain | 1.0000 |
| 10:101791345:AT:A | donor_gain | 1.0000 |
| 10:101791345:ATCA:A | donor_gain | 1.0000 |
| 10:101791346:T:C | donor_gain | 1.0000 |
| 10:101791352:A:AC | donor_gain | 1.0000 |
| 10:101791353:C:CC | donor_gain | 1.0000 |
| 10:101792942:CG:C | acceptor_gain | 1.0000 |
| 10:101793574:CTAT:C | donor_gain | 1.0000 |
| 10:101793688:AGAG:A | donor_gain | 1.0000 |
| 10:101798061:T:TA | donor_gain | 1.0000 |
| 10:101798840:A:AC | donor_gain | 1.0000 |
| 10:101798841:C:CC | donor_gain | 1.0000 |
| 10:101800240:A:AC | donor_gain | 1.0000 |
| 10:101800241:C:CT | donor_gain | 1.0000 |
| 10:101800241:CT:C | donor_gain | 1.0000 |
| 10:101800241:CTG:C | donor_gain | 1.0000 |
| 10:101800241:CTGCT:C | donor_gain | 1.0000 |
| 10:101800271:TGCA:T | donor_gain | 1.0000 |
| 10:101800398:CAG:C | acceptor_gain | 1.0000 |
AlphaMissense
6069 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 10:101791044:A:T | V769D | 1.000 |
| 10:101793946:C:A | W679C | 1.000 |
| 10:101793946:C:G | W679C | 1.000 |
| 10:101793948:A:G | W679R | 1.000 |
| 10:101793948:A:T | W679R | 1.000 |
| 10:101798031:A:G | W645R | 1.000 |
| 10:101798031:A:T | W645R | 1.000 |
| 10:101798145:A:G | W607R | 1.000 |
| 10:101798145:A:T | W607R | 1.000 |
| 10:101798897:A:G | L585P | 1.000 |
| 10:101798951:A:G | L567P | 1.000 |
| 10:101800278:A:G | W387R | 1.000 |
| 10:101800278:A:T | W387R | 1.000 |
| 10:101803778:C:A | W331C | 1.000 |
| 10:101803778:C:G | W331C | 1.000 |
| 10:101803780:A:G | W331R | 1.000 |
| 10:101803780:A:T | W331R | 1.000 |
| 10:101803808:G:C | N321K | 1.000 |
| 10:101803808:G:T | N321K | 1.000 |
| 10:101803826:A:C | N315K | 1.000 |
| 10:101803826:A:T | N315K | 1.000 |
| 10:101803830:G:C | P314R | 1.000 |
| 10:101803830:G:T | P314Q | 1.000 |
| 10:101803832:A:C | N313K | 1.000 |
| 10:101803832:A:T | N313K | 1.000 |
| 10:101803834:T:C | N313D | 1.000 |
| 10:101803839:A:G | L311P | 1.000 |
| 10:101803842:A:T | V310D | 1.000 |
| 10:101803845:C:T | G309E | 1.000 |
| 10:101803846:C:G | G309R | 1.000 |
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):
| Study | Trait | p-value |
|---|---|---|
| GCST009524_180 | Household income (MTAG) | 1.000000e-08 |
| GCST010138_11 | Raw vegetable consumption | 3.000000e-08 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0009695 | household income |
| EFO:0008111 | diet 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).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL5095251 | CEPEROGNASTAT | 2 | 21 |
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:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| ceperognastat | Inhibition | 8.63 | pIC50 |
| MK-8719 | Inhibition | 8.1 | pKi |
| thiamet-G | Inhibition | 7.68 | pKi |
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.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| US8901087, 2 | KI | 0.05 nM | US-8901087: Selective glycosidase inhibitors and uses thereof |
| US9695197, 4 | KI | 0.11 nM | US-9695197: Glycosidase inhibitors and uses thereof |
| US8901087, 27 | KI | 0.12 nM | US-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-diol | KI | 0.13 nM | US-9120781: Selective glycosidase inhibitors and uses thereof |
| US8901087, 191 | KI | 0.14 nM | US-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-diol | KI | 0.14 nM | US-9126957: Selective glycosidase inhibitors and uses thereof |
| US8901087, 95 | KI | 0.16 nM | US-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-diol | KI | 0.16 nM | US-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-diol | KI | 0.17 nM | US-8901087: Selective glycosidase inhibitors and uses thereof |
| US8901087, 97 | KI | 0.17 nM | US-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-diol | KI | 0.18 nM | US-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-diol | KI | 0.19 nM | US-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)methanol | KI | 0.19 nM | US-8901087: Selective glycosidase inhibitors and uses thereof |
| US9120781, 26 | KI | 0.2 nM | US-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-diol | KI | 0.22 nM | US-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-diol | KI | 0.26 nM | US-9126957: Selective glycosidase inhibitors and uses thereof |
| US9126957, 6 | KI | 0.26 nM | US-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-diol | KI | 0.3 nM | US-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-diol | KI | 0.3 nM | US-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-ol | KI | 0.3 nM | US-9409924: Selective glycosidase inhibitors and uses thereof |
| US9409924, 34 | KI | 0.3 nM | US-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-diol | KI | 0.33 nM | US-8901087: Selective glycosidase inhibitors and uses thereof |
| US8901087, 13 | KI | 0.4 nM | US-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-ol | KI | 0.4 nM | US-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-DIOL | KI | 0.4 nM | US-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-diol | KI | 0.44 nM | US-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-diol | KI | 0.45 nM | US-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-diol | KI | 0.45 nM | US-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-diol | KI | 0.5 nM | US-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-diol | KI | 0.5 nM | US-9120781: Selective glycosidase inhibitors and uses thereof |
| US9243020, 17 | KI | 0.5 nM | US-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-diol | KI | 0.53 nM | US-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-diol | KI | 0.59 nM | US-9611275: Permeable glycosidase inhibitors and uses thereof |
| US9120781, 9 | KI | 0.6 nM | US-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-diol | KI | 0.61 nM | US-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-diol | KI | 0.65 nM | US-9611275: Permeable glycosidase inhibitors and uses thereof |
| US8901087, 8 | KI | 0.68 nM | US-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, 4 | KI | 0.69 nM | |
| US8901087, 25 | KI | 0.7 nM | US-8901087: Selective glycosidase inhibitors and uses thereof |
| US8901087, 53 | KI | 0.7 nM | US-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-diol | KI | 0.7 nM | US-9199949: Selective glycosidase inhibitors and uses thereof |
| US9409924, 38 | KI | 0.7 nM | US-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-diol | KI | 0.7 nM | US-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-diol | KI | 0.71 nM | US-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-diol | KI | 0.78 nM | US-9611275: Permeable glycosidase inhibitors and uses thereof |
| US8901087, 181 | KI | 0.8 nM | US-8901087: Selective glycosidase inhibitors and uses thereof |
| US8901087, 141 | KI | 0.82 nM | US-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-diol | KI | 0.82 nM | US-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-diol | KI | 0.84 nM | US-9611275: Permeable glycosidase inhibitors and uses thereof |
| US8901087, 3 | KI | 0.9 nM | US-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).
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.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 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]ethanone | 1710173: 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 assay | ic50 | 0.0002 | uM |
| N-[5-[[4-[2-(1,2,3,4-tetrahydro-1,7-naphthyridin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0003 | uM |
| (3aR,5R,6S,7R,7aR)-2-ethylimino-5-(hydroxymethyl)-1,3a,5,6,7,7a-hexahydropyrano[3,2-d][1,3]thiazole-6,7-diol | 1527147: Inhibition of human O-GlcNAcase | ic50 | 0.0004 | uM |
| 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]ethanone | 1710173: 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 assay | ic50 | 0.0004 | uM |
| N-[5-[[4-[2-[2-(dimethylamino)pyrimidin-5-yl]ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0004 | uM |
| (3aR,5S,6S,7R,7aR)-5-(difluoromethyl)-2-(methylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol | 1558062: Inhibition of recombinant human OGA | ki | 0.0004 | uM |
| 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]ethanone | 1710173: 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 assay | ic50 | 0.0005 | uM |
| 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]ethanone | 1710173: 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 assay | ic50 | 0.0005 | uM |
| (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-ol | 1558062: Inhibition of recombinant human OGA | ki | 0.0005 | uM |
| (3aR,5S,6S,7R,7aR)-5-(fluoromethyl)-2-methylimino-1,3a,5,6,7,7a-hexahydropyrano[3,2-d][1,3]thiazole-6,7-diol | 1558062: Inhibition of recombinant human OGA | ki | 0.0006 | uM |
| 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]ethanone | 1710173: 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 assay | ic50 | 0.0006 | uM |
| N-[5-[[4-[2-(8-methylquinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0007 | uM |
| 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]ethanone | 1710173: 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 assay | ic50 | 0.0008 | uM |
| N-[5-[[4-[2-(1,2,3,4-tetrahydroquinolin-7-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0008 | uM |
| N-[5-[[4-[2-(7-methylquinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0015 | uM |
| N-[5-[[4-[2-(2-oxo-3,4-dihydro-1H-quinolin-5-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0017 | uM |
| N-[5-[[4-[2-(1-benzofuran-7-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0018 | uM |
| 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]acetamide | 2114285: 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 analysis | ic50 | 0.0021 | uM |
| 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]acetamide | 2114327: 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 analysis | ic50 | 0.0024 | uM |
| (3aR,5S,6S,7R,7aR)-5-(difluoromethyl)-2-(dimethylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol | 1558062: Inhibition of recombinant human OGA | ki | 0.0024 | uM |
| (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-diol | 1558062: Inhibition of recombinant human OGA | ki | 0.0028 | uM |
| (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-ol | 1558062: Inhibition of recombinant human OGA | ki | 0.0030 | uM |
| N-[5-[[4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0030 | uM |
| N-[5-[[4-[2-(8-fluoro-1,2,3,4-tetrahydroquinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0032 | uM |
| (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-diol | 1558062: Inhibition of recombinant human OGA | ki | 0.0033 | uM |
| N-[5-[[4-[2-[6-(dimethylamino)-3-pyridinyl]ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0035 | uM |
| N-[5-[[4-[2-[6-(trifluoromethyl)pyrimidin-4-yl]ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0036 | uM |
| N-[5-[[(5S)-2-(2,6-dimethyl-4-pyridinyl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide | 1537422: 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 assay | ic50 | 0.0037 | uM |
| N-[5-[[4-[2-(2-pyrrolidin-1-ylpyrimidin-5-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0037 | uM |
| N-[5-[[2-(3,5-dimethyl-2-pyridinyl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide | 1537422: 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 assay | ic50 | 0.0039 | uM |
| (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-dienamide | 1378936: Competitive inhibition of human O-GlcNAcase by Lineweaver-Burk analysis | ki | 0.0041 | uM |
| N-[5-[[4-[2-(2,6-dimethyl-3-pyridinyl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0044 | uM |
| N-[5-[[4-[2-(5,6,7,8-tetrahydro-1,5-naphthyridin-2-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0046 | uM |
| N-[5-[[4-[2-(1,2,3,4-tetrahydroquinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0049 | uM |
| (3aR,5S,6S,7R,7aR)-5-(difluoromethyl)-2-(propylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol | 1558062: Inhibition of recombinant human OGA | ki | 0.0053 | uM |
| N-[5-[[4-[2-(4,6-dimethyl-2-pyridinyl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0054 | uM |
| (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-diol | 1558062: Inhibition of recombinant human OGA | ki | 0.0055 | uM |
| (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-diol | 1558062: Inhibition of recombinant human OGA | ki | 0.0056 | uM |
| N-[5-[[2-(2,6-dimethyl-4-pyridinyl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide | 1537422: 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 assay | ic50 | 0.0060 | uM |
| (3aR,5S,6S,7R,7aR)-5-(difluoromethyl)-2-ethylimino-1,3a,5,6,7,7a-hexahydropyrano[3,2-d][1,3]thiazole-6,7-diol | 1527147: Inhibition of human O-GlcNAcase | ic50 | 0.0079 | uM |
| N-[5-[[4-[2-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0080 | uM |
| N-[5-[[4-[2-[2-(trifluoromethyl)pyrimidin-5-yl]ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0087 | uM |
| N-[5-[[4-[2-(6-pyrrolidin-1-yl-3-pyridinyl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0088 | uM |
| N-[5-[[4-[2-(2,3-dihydro-1-benzofuran-5-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0089 | uM |
| N-[5-[[4-[2-(7-fluoro-1,2,3,4-tetrahydroquinolin-6-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0089 | uM |
| (3aR,5S,6S,7R,7aR)-2-(dimethylamino)-5-(fluoromethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol | 1558062: Inhibition of recombinant human OGA | ki | 0.0090 | uM |
| (3aR,5R,6S,7aR)-5-(hydroxymethyl)-2-(methylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazol-6-ol | 1558062: Inhibition of recombinant human OGA | ki | 0.0094 | uM |
| N-[5-[[4-[2-(1,3-benzodioxol-5-yl)ethynyl]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide | 2114285: 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 analysis | ic50 | 0.0095 | uM |
| (3aR,5R,6S,7R,7aR)-5-(hydroxymethyl)-2-methyl-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol | 515842: Inhibition of human O-GlcNAcase after 5 mins by Lineweaver-Burke plot analysis | ki | 0.0100 | uM |
| N-[5-[4-[(1S)-1-(1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl]-1,3,4-thiadiazol-2-yl]acetamide | 2114326: Inhibition of human OGA | ic50 | 0.0102 | uM |
CTD chemical–gene interactions
74 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects cotreatment, increases expression, decreases expression, affects expression | 6 |
| bisphenol A | decreases expression, increases expression, increases methylation | 4 |
| sodium arsenite | decreases expression, increases expression | 4 |
| Acetaminophen | affects expression, increases expression | 3 |
| 7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide | affects expression, decreases expression | 3 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, increases expression, decreases expression | 2 |
| bisphenol S | increases expression, affects cotreatment, decreases expression | 2 |
| Leflunomide | increases expression | 2 |
| Rotenone | decreases expression | 2 |
| Tretinoin | decreases expression, increases expression | 2 |
| aristolochic acid I | decreases expression | 1 |
| GSK-J4 | increases expression | 1 |
| FR900359 | affects phosphorylation | 1 |
| bisphenol F | affects cotreatment, decreases expression | 1 |
| dicrotophos | decreases expression | 1 |
| beauvericin | increases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| deoxynivalenol | increases expression | 1 |
| quercitrin | increases expression | 1 |
| trichostatin A | affects expression | 1 |
| methylparaben | increases expression | 1 |
| sulforaphane | increases expression | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | increases expression | 1 |
| nickel chloride | increases expression | 1 |
| beta-methylcholine | affects expression | 1 |
| epigallocatechin gallate | decreases expression | 1 |
| tamibarotene | decreases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| chloropicrin | increases expression | 1 |
| K 7174 | increases expression | 1 |
ChEMBL screening assays
89 unique, capped per target: 89 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1218573 | Binding | Inhibition of human O-GlcNAcase | A 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):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B1ZH | Abcam HeLa OGA KO | Cancer cell line | Female |
| CVCL_SY28 | HAP1 MGEA5 (-) 1 | Cancer cell line | Male |
| CVCL_XQ53 | HAP1 MGEA5 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.