GUSB
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Summary
GUSB (glucuronidase beta, HGNC:4696) is a protein-coding gene on chromosome 7q11.21, encoding Beta-glucuronidase (P08236). Plays an important role in the degradation of dermatan and keratan sulfates.
This gene encodes a hydrolase that degrades glycosaminoglycans, including heparan sulfate, dermatan sulfate, and chondroitin-4,6-sulfate. The enzyme forms a homotetramer that is localized to the lysosome. Mutations in this gene result in mucopolysaccharidosis type VII. Alternative splicing results in multiple transcript variants. There are many pseudogenes of this locus in the human genome.
Source: NCBI Gene 2990 — RefSeq curated summary.
At a glance
- Gene–disease (curated): mucopolysaccharidosis type 7 (Definitive, ClinGen)
- GWAS associations: 1
- Clinical variants (ClinVar): 771 total — 55 pathogenic, 40 likely-pathogenic
- Phenotypes (HPO): 82
- Druggable target: yes — 2 molecules with ChEMBL bioactivity
- Dosage sensitivity (ClinGen): haploinsufficiency autosomal recessive, triplosensitivity no evidence
- MANE Select transcript:
NM_000181
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:4696 |
| Approved symbol | GUSB |
| Name | glucuronidase beta |
| Location | 7q11.21 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000169919 |
| Ensembl biotype | protein_coding |
| OMIM | 611499 |
| Entrez | 2990 |
Gene structure
Transcript identifiers
Ensembl transcripts: 49 — 37 protein_coding, 5 protein_coding_CDS_not_defined, 4 retained_intron, 3 nonsense_mediated_decay
ENST00000304895, ENST00000421103, ENST00000430730, ENST00000446111, ENST00000447929, ENST00000461622, ENST00000462371, ENST00000465785, ENST00000466883, ENST00000475316, ENST00000476486, ENST00000478118, ENST00000479038, ENST00000489482, ENST00000864776, ENST00000864777, ENST00000864778, ENST00000864779, ENST00000864780, ENST00000864781, ENST00000864782, ENST00000864783, ENST00000864784, ENST00000864785, ENST00000864786, ENST00000864787, ENST00000864788, ENST00000864789, ENST00000864790, ENST00000864791, ENST00000864792, ENST00000864793, ENST00000864794, ENST00000864795, ENST00000864796, ENST00000864797, ENST00000864798, ENST00000912571, ENST00000912572, ENST00000912573, ENST00000912574, ENST00000912575, ENST00000912576, ENST00000912577, ENST00000912578, ENST00000952458, ENST00000952459, ENST00000952460, ENST00000952461
RefSeq mRNA: 4 — MANE Select: NM_000181
NM_000181, NM_001284290, NM_001293104, NM_001293105
CCDS: CCDS5530, CCDS64665
Canonical transcript exons
ENST00000304895 — 12 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001131491 | 65960684 | 65961063 |
| ENSE00001554367 | 65981974 | 65982213 |
| ENSE00003467512 | 65974526 | 65974704 |
| ENSE00003502074 | 65970282 | 65970366 |
| ENSE00003534535 | 65979727 | 65979911 |
| ENSE00003569314 | 65967731 | 65967907 |
| ENSE00003569679 | 65976015 | 65976202 |
| ENSE00003607665 | 65979399 | 65979541 |
| ENSE00003630799 | 65974295 | 65974441 |
| ENSE00003638618 | 65974919 | 65975071 |
| ENSE00003683385 | 65964323 | 65964458 |
| ENSE00003687473 | 65980224 | 65980409 |
Expression profiles
Bgee: expression breadth ubiquitous, 297 present calls, max score 98.96.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 28.3209 / max 245.7589, expressed in 1812 samples.
FANTOM5 promoters (4 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 84213 | 25.4000 | 1808 |
| 84212 | 1.9217 | 1035 |
| 84211 | 0.8995 | 527 |
| 84210 | 0.0997 | 24 |
Top tissues by expression
299 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| endometrium epithelium | UBERON:0004811 | 98.96 | gold quality |
| tendon of biceps brachii | UBERON:0008188 | 98.75 | gold quality |
| tibia | UBERON:0000979 | 98.38 | gold quality |
| visceral pleura | UBERON:0002401 | 97.62 | gold quality |
| pleura | UBERON:0000977 | 96.66 | gold quality |
| parietal pleura | UBERON:0002400 | 96.56 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 96.17 | gold quality |
| palpebral conjunctiva | UBERON:0001812 | 96.15 | gold quality |
| right lobe of liver | UBERON:0001114 | 96.11 | gold quality |
| granulocyte | CL:0000094 | 96.03 | gold quality |
| layer of synovial tissue | UBERON:0007616 | 95.93 | gold quality |
| spleen | UBERON:0002106 | 95.85 | gold quality |
| liver | UBERON:0002107 | 95.82 | gold quality |
| placenta | UBERON:0001987 | 95.62 | gold quality |
| parotid gland | UBERON:0001831 | 95.60 | gold quality |
| eye | UBERON:0000970 | 95.57 | gold quality |
| rectum | UBERON:0001052 | 95.55 | gold quality |
| ileal mucosa | UBERON:0000331 | 95.52 | gold quality |
| pylorus | UBERON:0001166 | 95.17 | gold quality |
| monocyte | CL:0000576 | 95.15 | gold quality |
| colonic mucosa | UBERON:0000317 | 95.15 | gold quality |
| synovial joint | UBERON:0002217 | 95.15 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 95.14 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 95.14 | gold quality |
| mononuclear cell | CL:0000842 | 95.07 | gold quality |
| periodontal ligament | UBERON:0008266 | 95.04 | gold quality |
| leukocyte | CL:0000738 | 95.03 | gold quality |
| renal glomerulus | UBERON:0000074 | 95.00 | gold quality |
| right lung | UBERON:0002167 | 94.98 | gold quality |
| metanephric glomerulus | UBERON:0004736 | 94.91 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-7303 | no | 895.60 |
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): ERF, NR1I2, NR4A3, TFAP2A, VSX2
miRNA regulators (miRDB)
7 targeting GUSB, 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-3692-3P | 99.98 | 70.27 | 2139 |
| HSA-MIR-4255 | 99.72 | 67.70 | 1541 |
| HSA-MIR-4527 | 99.66 | 67.43 | 714 |
| HSA-MIR-587 | 99.64 | 70.86 | 2611 |
| HSA-MIR-6503-5P | 99.62 | 66.96 | 597 |
| HSA-MIR-6071 | 99.16 | 67.77 | 1780 |
| HSA-MIR-6889-5P | 90.26 | 64.13 | 291 |
Functional genomics
ClinGen dosage: haploinsufficiency 30 (autosomal recessive), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map
Literature-anchored findings (GeneRIF, showing 19)
- beta-glucuronidase mutations are associated with mucopolysaccharidosis type VII (PMID:12522561)
- Recombinant adeno-associated virus encoding human GUSB injected into the vitreous humor of young adult MPS VII mice increased GUSB activity and reduced lysosomal distension in regions of the thalamus and tectum (PMID:12716937)
- beta glucuronidase present in the synovial fluid of rheumatoid arthritis patients, may contribute to the depletion of glycosaminoglycans from cartilage allowing invasion of synovial cells. (PMID:12905469)
- Over-expression of beta-glucuronidase was related to the degree of cancer differentiation, but not to lymph node metastasis. (PMID:14612292)
- These results indicate that beta-glucuronidase transport into brain parenchyma in early postnatal life is mediated by the mannose 6-phosphate/insulin-like growth factor II receptor. (PMID:15314220)
- The genes GUS and PMM1 are recommended for normalization purposes in gene expression studies of liver tissue from patients with chronic hepatitis. (PMID:18591914)
- Study summarized information on the 49 unique, disease-causing mutations determined so far in the GUS gene. (PMID:19224584)
- Liver disease affects the expression of common HKGs; beta-glucuronidase and splicing factor arginine/serine-rich 4 are the most stable HKGs for studies of gene expression in HCV-infected human liver. (PMID:21073651)
- GUSB and ATP2B4 have been validated as a reliable gene combination for Cystic Fibrosis Transmembrane Conductance Regulator gene qPCR data normalization. (PMID:22525089)
- This assessment demonstrated that although butyrate dramatically increased beta-glucuronidase production in bioreactors, it adversely impacted the mannose-6-phosphorylation of this lysosomal storage diseasestherapeutic enzyme (PMID:24033810)
- expression of CES2, UGTA1A1, and GUSB varies in colorectal pathology tissues and that the expression of CES2 is somewhat related to tumor staging. (PMID:24195516)
- the efficacy of a helper-dependent (HD) canine adenovirus (CAV-2) vector harboring a human GUSB expression cassette (HD-RIGIE) in the MPS VII dog brain was tested (PMID:24343103)
- the use of in silico approaches provided a useful understanding of the effect of single point mutations on the structure-function relationship of GUSBp (PMID:26415878)
- Selective and amplified bG expression together with the prodrug DOXGA3 had an increased antitumor effect, showing great potential for prostate cancer therapy. (PMID:26648021)
- Results show that GUS mRNA changes in blood are significantly correlated with gait step length variability in premutation (PM) females patients with fragile X tremor ataxia syndrome . (PMID:27387142)
- We produced GUS from a CHO cell line grown in suspension in a 15 L perfused bioreactor and developed a three step purification procedure that yields approximately 99% pure enzyme with a recovery of more than 40%. (PMID:28734840)
- the beta-d-galactosidase, beta-d-glucuronidase and alpha-l-fucosidase activities in serums from hemolyzed blood, were determined. (PMID:29885630)
- Over-Expression of GUSB Leads to Primary Resistance of Anti-PD1 Therapy in Hepatocellular Carcinoma. (PMID:35812439)
- Macrophages and derived-TNF-alpha promote lipopolysaccharide-induced upregulation of endogenous beta-glucuronidase in the epithelial cells of the bile duct: A possible facilitator of hepatolithiasis formation. (PMID:36473630)
Cross-species orthologs
6 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | gusb | ENSDARG00000063126 |
| mus_musculus | Gusb | ENSMUSG00000025534 |
| rattus_norvegicus | Gusb | ENSRNOG00000000913 |
| drosophila_melanogaster | CG15117 | FBGN0034417 |
| drosophila_melanogaster | betaGlu | FBGN0270927 |
| caenorhabditis_elegans | Y105E8B.9 | WBGENE00013693 |
Paralogs (1): MANBA (ENSG00000109323)
Protein
Protein identifiers
Beta-glucuronidase — P08236 (reviewed: P08236)
Alternative names: Beta-G1
All UniProt accessions (3): P08236, F2Z3L6, F8WBK6
UniProt curated annotations — full annotation on UniProt →
Function. Plays an important role in the degradation of dermatan and keratan sulfates.
Subunit / interactions. Homotetramer.
Subcellular location. Lysosome.
Post-translational modifications. N-linked glycosylated with 3 to 4 oligosaccharide chains.
Disease relevance. Mucopolysaccharidosis 7 (MPS7) [MIM:253220] A form of mucopolysaccharidosis, a group of lysosomal storage diseases characterized by defective degradation of glycosaminoglycans, resulting in their excessive accumulation and secretion. The diseases are progressive and often display a wide spectrum of clinical severity. MPS7 is an autosomal recessive form with a highly variable phenotype, ranging from severe lethal hydrops fetalis to mild forms with survival into adulthood. Most patients with the intermediate phenotype show hepatomegaly, skeletal anomalies, coarse facies, and variable degrees of mental impairment. The disease is caused by variants affecting the gene represented in this entry.
Activity regulation. Inhibited by L-aspartic acid.
Similarity. Belongs to the glycosyl hydrolase 2 family.
Isoforms (3)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P08236-1 | 1, Long | yes |
| P08236-2 | 2, Short | |
| P08236-3 | 3 |
RefSeq proteins (4): NP_000172, NP_001271219, NP_001280033, NP_001280034 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR006101 | Glyco_hydro_2 | Family |
| IPR006102 | Ig-like_GH2 | Domain |
| IPR006103 | Glyco_hydro_2_cat | Domain |
| IPR006104 | Glyco_hydro_2_N | Domain |
| IPR008979 | Galactose-bd-like_sf | Homologous_superfamily |
| IPR013783 | Ig-like_fold | Homologous_superfamily |
| IPR017853 | GH_hydrolase_sf | Homologous_superfamily |
| IPR023230 | Glyco_hydro_2_CS | Conserved_site |
| IPR023232 | Glyco_hydro_2_AS | Active_site |
| IPR036156 | Beta-gal/glucu_dom_sf | Homologous_superfamily |
Pfam: PF00703, PF02836, PF02837
Enzyme classification (BRENDA):
- EC 3.2.1.31 — beta-glucuronidase (BRENDA: 70 organisms, 139 substrates, 75 inhibitors, 71 Km, 35 kcat entries)
Substrate kinetics (BRENDA)
33 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| GLYCYRRHIZIN | 0.78–7.72 | 9 |
| 4-METHYLUMBELLIFERYL-BETA-D-GLUCURONIDE | 1.04–2.76 | 7 |
| 4-NITROPHENYL BETA-D-GLUCURONIDE | 0.0046–0.36 | 5 |
| GLYCYRRHETINIC ACID 3-O-MONO-BETA-D-GLUCURONIDE | 0.91–1.1 | 4 |
| 4-NITROPHENYL BETA-D-GLUCOSIDE | 0.0304–145 | 3 |
| 4-NITROPHENYL-BETA-D-GLUCURONIDE | 0.208–1.4 | 3 |
| 4-METHYLUMBELLIFERYL BETA-D-GLUCURONIDE | 0.54–0.58 | 2 |
| GLCABETA(1-6)GAL | 0.378–0.422 | 2 |
| P-NITROPHENYL-BETA-D-GLUCURONIDE | 0.22–0.23 | 2 |
| 1-DEOXY-1-(6-THIOPURINYL)-BETA-D-GLUCOPYRANOSIDE | 1.49 | 1 |
| 1-DEOXY-1-(6-THIOPURINYL)-BETA-D-GLUCOPYRANOSIDU | 9.25 | 1 |
| 4-ME-BETA-GLCA-(1-6)-BETA-GAL-(1-6)-BETA-GAL-(1- | 1.4 | 1 |
| 4-ME-BETA-GLCA-(1-6)-BETA-GAL-(1-6)-GAL | 1.9 | 1 |
| 4-ME-BETA-GLCA-(1-6)-GAL | 3.6 | 1 |
| 4-METHYLUMBELLIFERYL-BETA-D-GLUCURONIC ACID | 1.25 | 1 |
Catalyzed reactions (Rhea), 1 shown:
- a beta-D-glucuronoside + H2O = D-glucuronate + an alcohol (RHEA:17633)
UniProt features (108 total): sequence variant 40, strand 36, helix 16, turn 7, glycosylation site 4, splice variant 2, signal peptide 1, chain 1, active site 1
Structure
Experimental structures (PDB)
2 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 3HN3 | X-RAY DIFFRACTION | 1.7 |
| 1BHG | X-RAY DIFFRACTION | 2.53 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P08236-F1 | 94.35 | 0.93 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (1): 451 (proton donor)
Glycosylation sites (4): 173, 272, 420, 631
Function
Pathways and Gene Ontology
Reactome pathways
17 pathways
| ID | Pathway |
|---|---|
| R-HSA-2024101 | CS/DS degradation |
| R-HSA-2160916 | Hyaluronan degradation |
| R-HSA-2206292 | MPS VII - Sly syndrome (Hyaluronan metabolism) |
| R-HSA-6798695 | Neutrophil degranulation |
| R-HSA-9953080 | MPS VII - Sly syndrome (CS/DS degradation) |
| R-HSA-1430728 | Metabolism |
| R-HSA-1630316 | Glycosaminoglycan metabolism |
| R-HSA-1638091 | Heparan sulfate/heparin (HS-GAG) metabolism |
| R-HSA-1643685 | Disease |
| R-HSA-168249 | Innate Immune System |
| R-HSA-168256 | Immune System |
| R-HSA-2024096 | HS-GAG degradation |
| R-HSA-2142845 | Hyaluronan metabolism |
| R-HSA-2206281 | Mucopolysaccharidoses |
| R-HSA-5663084 | Diseases of carbohydrate metabolism |
| R-HSA-5668914 | Diseases of metabolism |
| R-HSA-71387 | Metabolism of carbohydrates and carbohydrate derivatives |
MSigDB gene sets: 505 (showing top):
GOBP_MYELOID_CELL_DIFFERENTIATION, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, REACTOME_INNATE_IMMUNE_SYSTEM, GOBP_PHOSPHATIDYLINOSITOL_METABOLIC_PROCESS, GOBP_CARTILAGE_DEVELOPMENT, GOBP_VACUOLE_ORGANIZATION, GOBP_SKELETAL_SYSTEM_DEVELOPMENT, GOBP_INFLAMMATORY_RESPONSE, PAL_PRMT5_TARGETS_UP, GOCC_SECRETORY_GRANULE, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, GOBP_GROWTH
GO Biological Process (35): retinoid metabolic process (GO:0001523), in utero embryonic development (GO:0001701), endochondral ossification (GO:0001958), muscle system process (GO:0003012), chondrocyte hypertrophy (GO:0003415), growth plate cartilage morphogenesis (GO:0003422), carbohydrate metabolic process (GO:0005975), glycosaminoglycan catabolic process (GO:0006027), autophagy (GO:0006914), inflammatory response (GO:0006954), lysosome organization (GO:0007040), cell population proliferation (GO:0008283), protein secretion (GO:0009306), gene expression (GO:0010467), heparan sulfate proteoglycan catabolic process (GO:0030200), chondroitin sulfate proteoglycan catabolic process (GO:0030207), hyaluronan catabolic process (GO:0030214), protein localization to nucleus (GO:0034504), multicellular organism growth (GO:0035264), aorta development (GO:0035904), phosphatidylinositol-3-phosphate biosynthetic process (GO:0036092), TORC1 signaling (GO:0038202), response to peptide hormone (GO:0043434), bone resorption (GO:0045453), homeostasis of number of cells (GO:0048872), articular cartilage development (GO:0061975), energy homeostasis (GO:0097009), cranial skeletal system development (GO:1904888), skeletal system development (GO:0001501), ossification (GO:0001503), growth plate cartilage development (GO:0003417), protein catabolic process (GO:0030163), bone development (GO:0060348), bone morphogenesis (GO:0060349), bone growth (GO:0098868)
GO Molecular Function (7): beta-glucuronidase activity (GO:0004566), signaling receptor binding (GO:0005102), protein domain specific binding (GO:0019904), carbohydrate binding (GO:0030246), hydrolase activity, hydrolyzing O-glycosyl compounds (GO:0004553), hydrolase activity (GO:0016787), hydrolase activity, acting on glycosyl bonds (GO:0016798)
GO Cellular Component (9): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), endoplasmic reticulum (GO:0005783), membrane (GO:0016020), azurophil granule lumen (GO:0035578), lysosomal lumen (GO:0043202), extracellular exosome (GO:0070062), ficolin-1-rich granule lumen (GO:1904813), lysosome (GO:0005764)
Reactome top-level categories
Rollup of top-12 pathways:
| Category | Pathways |
|---|---|
| Mucopolysaccharidoses | 2 |
| Glycosaminoglycan metabolism | 2 |
| Chondroitin sulfate/dermatan sulfate metabolism | 1 |
| Hyaluronan metabolism | 1 |
| Innate Immune System | 1 |
| Metabolism of carbohydrates and carbohydrate derivatives | 1 |
| Immune System | 1 |
| Heparan sulfate/heparin (HS-GAG) metabolism | 1 |
| Diseases of carbohydrate metabolism | 1 |
| Diseases of metabolism | 1 |
| Disease | 1 |
| Metabolism | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| proteoglycan catabolic process | 2 |
| protein binding | 2 |
| cellular anatomical structure | 2 |
| vacuolar lumen | 2 |
| diterpenoid metabolic process | 1 |
| chordate embryonic development | 1 |
| replacement ossification | 1 |
| endochondral bone morphogenesis | 1 |
| system process | 1 |
| chondrocyte development | 1 |
| developmental cell growth | 1 |
| growth plate cartilage development | 1 |
| cartilage morphogenesis | 1 |
| primary metabolic process | 1 |
| aminoglycan catabolic process | 1 |
| glycosaminoglycan metabolic process | 1 |
| catabolic process | 1 |
| transmembrane transport | 1 |
| process utilizing autophagic mechanism | 1 |
| defense response | 1 |
| lytic vacuole organization | 1 |
| cellular process | 1 |
| protein transport | 1 |
| secretion by cell | 1 |
| establishment of protein localization to extracellular region | 1 |
| protein localization to extracellular region | 1 |
| macromolecule biosynthetic process | 1 |
| heparan sulfate proteoglycan metabolic process | 1 |
| chondroitin sulfate proteoglycan metabolic process | 1 |
| glycosaminoglycan catabolic process | 1 |
| hyaluronan metabolic process | 1 |
| protein localization to organelle | 1 |
| multicellular organismal process | 1 |
| developmental growth | 1 |
| artery development | 1 |
| glucuronidase activity | 1 |
| binding | 1 |
| hydrolase activity, acting on glycosyl bonds | 1 |
| catalytic activity | 1 |
| hydrolase activity | 1 |
Protein interactions and networks
STRING
3476 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| GUSB | KL | Q9UEF7 | 869 |
| GUSB | ARSA | P15289 | 838 |
| GUSB | OGA | O60502 | 830 |
| GUSB | GAPDH | P00354 | 766 |
| GUSB | MPI | P34949 | 758 |
| GUSB | CES1 | P23141 | 756 |
| GUSB | IGF2R | P11717 | 744 |
| GUSB | TRPV5 | Q9NQA5 | 741 |
| GUSB | HPRT1 | P00492 | 735 |
| GUSB | B2M | P01884 | 733 |
| GUSB | ARSB | P15848 | 729 |
| GUSB | MPO | P05164 | 728 |
| GUSB | POTEF | A5A3E0 | 718 |
| GUSB | IDUA | P35475 | 717 |
| GUSB | TBP | P20226 | 715 |
IntAct
95 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CDK4 | HSP90AA1 | psi-mi:“MI:0914”(association) | 0.640 |
| CANX | PGRMC1 | psi-mi:“MI:0914”(association) | 0.570 |
| GUSB | psi-mi:“MI:0915”(physical association) | 0.550 | |
| FBXO2 | TMEM131L | psi-mi:“MI:0914”(association) | 0.530 |
| ZBTB42 | MID1 | psi-mi:“MI:0914”(association) | 0.530 |
| ADAMTS4 | MANBA | psi-mi:“MI:0914”(association) | 0.530 |
| C1orf54 | EXTL3 | psi-mi:“MI:0914”(association) | 0.530 |
| CDK4 | GUSB | psi-mi:“MI:0914”(association) | 0.530 |
| DNAJC3 | DEDD | psi-mi:“MI:0914”(association) | 0.530 |
| GUSB | BRAF | psi-mi:“MI:2364”(proximity) | 0.470 |
| BRAF | GUSB | psi-mi:“MI:0915”(physical association) | 0.470 |
| GUSB | GUSB | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| VRK1 | GUSB | psi-mi:“MI:0915”(physical association) | 0.400 |
| GUSB | GIT2 | psi-mi:“MI:0915”(physical association) | 0.370 |
| HSCB | RBP5 | psi-mi:“MI:0914”(association) | 0.350 |
| FBXO6 | GNS | psi-mi:“MI:0914”(association) | 0.350 |
| DENND11 | psi-mi:“MI:0914”(association) | 0.350 | |
| VPS37C | psi-mi:“MI:0914”(association) | 0.350 | |
| P4HA2 | psi-mi:“MI:0914”(association) | 0.350 | |
| MFAP4 | CRLF1 | psi-mi:“MI:0914”(association) | 0.350 |
| SCGB2A2 | RTL8C | psi-mi:“MI:0914”(association) | 0.350 |
| CEACAM8 | PRRT4 | psi-mi:“MI:0914”(association) | 0.350 |
| SLURP1 | MANBA | psi-mi:“MI:0914”(association) | 0.350 |
| TMEM25 | NME4 | psi-mi:“MI:0914”(association) | 0.350 |
| GUSB | HOXA3 | psi-mi:“MI:0914”(association) | 0.350 |
| IDS | COCH | psi-mi:“MI:0914”(association) | 0.350 |
| BTNL2 | TMEM131L | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (88): GUSB (Affinity Capture-MS), GUSB (Affinity Capture-MS), GUSB (Affinity Capture-MS), GUSB (Affinity Capture-MS), FAHD1 (Co-fractionation), HOXA3 (Affinity Capture-MS), PMEL (Affinity Capture-MS), GUSB (Affinity Capture-MS), GUSB (Affinity Capture-MS), GUSB (Affinity Capture-MS), GUSB (Affinity Capture-MS), GUSB (Affinity Capture-MS), GUSB (Affinity Capture-MS), CES1 (Affinity Capture-Western), GUSB (Proximity Label-MS)
ESM2 similar proteins: A0JMP0, A4IG42, A5PJN5, A6QLU7, A6QQ07, F1N2K1, O00462, O18835, O43280, O77695, O95479, O97524, P08236, P10253, P12265, P19813, P70699, P82450, Q3U4H6, Q4FAT7, Q4FZV0, Q5E985, Q5FVF9, Q5R5N6, Q5R7A9, Q5R8R3, Q5RFU0, Q5XHI4, Q641Z7, Q6P6V7, Q6P7A9, Q6QR59, Q6RHW4, Q76HN1, Q865R1, Q8BFW6, Q8BNE1, Q8BP56, Q8C0L6, Q8CFX1
Diamond homologs: A0A089LCJ8, O18835, O77695, O97524, P05804, P06760, P08236, P12265, Q4FAT7, Q5R5N6, Q6P575, Q8E0N2, Q8XP19, Q15486, P06219, Q9K9C6, A6T8X0, A7LXS9, B5XQY2, Q56307
SIGNOR signaling
2 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| TFEB | “up-regulates quantity by expression” | GUSB | “transcriptional regulation” |
| ACSS2 | “up-regulates quantity by expression” | GUSB | “transcriptional regulation” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
771 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 55 |
| Likely pathogenic | 40 |
| Uncertain significance | 221 |
| Likely benign | 369 |
| Benign | 20 |
Top pathogenic / likely-pathogenic (30)
| Variant ID | HGVS | Classification |
|---|---|---|
| 100722 | NM_000181.4(GUSB):c.530C>T (p.Thr177Ile) | Pathogenic |
| 1027384 | NM_000181.4(GUSB):c.1651C>T (p.Gln551Ter) | Pathogenic |
| 2087077 | NM_000181.4(GUSB):c.932dup (p.Ser312fs) | Pathogenic |
| 2111403 | NM_000181.4(GUSB):c.24del (p.Trp9fs) | Pathogenic |
| 2117122 | NM_000181.4(GUSB):c.604C>T (p.Gln202Ter) | Pathogenic |
| 2231212 | NM_000181.4(GUSB):c.1583G>A (p.Trp528Ter) | Pathogenic |
| 2431204 | NM_000181.4(GUSB):c.1874del (p.Arg625fs) | Pathogenic |
| 2431211 | NM_000181.4(GUSB):c.7del (p.Arg3fs) | Pathogenic |
| 2698405 | NM_000181.4(GUSB):c.867_871del (p.Trp289_Tyr291delinsTer) | Pathogenic |
| 2701335 | NM_000181.4(GUSB):c.643C>T (p.Gln215Ter) | Pathogenic |
| 2728754 | NM_000181.4(GUSB):c.74dup (p.Gly26fs) | Pathogenic |
| 2731024 | NM_000181.4(GUSB):c.1455dup (p.Asn486Ter) | Pathogenic |
| 2735027 | NM_000181.4(GUSB):c.1457_1460del (p.Asn486fs) | Pathogenic |
| 2736760 | NM_000181.4(GUSB):c.1047del (p.Asn349fs) | Pathogenic |
| 2755268 | NM_000181.4(GUSB):c.190del (p.Tyr64fs) | Pathogenic |
| 2757736 | NM_000181.4(GUSB):c.1809dup (p.Asn604fs) | Pathogenic |
| 2766408 | NM_000181.4(GUSB):c.1872_1875dup (p.Tyr626fs) | Pathogenic |
| 2797791 | NM_000181.4(GUSB):c.320del (p.Leu107fs) | Pathogenic |
| 2799488 | NM_000181.4(GUSB):c.916C>T (p.Gln306Ter) | Pathogenic |
| 2803581 | NM_000181.4(GUSB):c.739C>T (p.Gln247Ter) | Pathogenic |
| 2806625 | NM_000181.4(GUSB):c.11_12del (p.Gly4fs) | Pathogenic |
| 2841797 | NM_000181.4(GUSB):c.76_79dup (p.Met27fs) | Pathogenic |
| 2847045 | NM_000181.4(GUSB):c.1865T>A (p.Leu622Ter) | Pathogenic |
| 2848108 | NC_000007.14:g.65974442del | Pathogenic |
| 2852702 | NM_000181.4(GUSB):c.325G>T (p.Glu109Ter) | Pathogenic |
| 2863642 | NM_000181.4(GUSB):c.507dup (p.Ile170fs) | Pathogenic |
| 2867424 | NM_000181.4(GUSB):c.1872_1875del (p.Glu624fs) | Pathogenic |
| 2869792 | NM_000181.4(GUSB):c.527_530del (p.Leu176fs) | Pathogenic |
| 2891880 | NM_000181.4(GUSB):c.434del (p.Gly145fs) | Pathogenic |
| 2903068 | NM_000181.4(GUSB):c.1756dup (p.Ile586fs) | Pathogenic |
SpliceAI
2134 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 7:65961059:CGGTG:C | acceptor_gain | 1.0000 |
| 7:65961061:GTGC:G | acceptor_loss | 1.0000 |
| 7:65961062:TGC:T | acceptor_loss | 1.0000 |
| 7:65961063:GC:G | acceptor_loss | 1.0000 |
| 7:65961064:C:CC | acceptor_gain | 1.0000 |
| 7:65964318:CTTAC:C | donor_loss | 1.0000 |
| 7:65964320:TACAC:T | donor_loss | 1.0000 |
| 7:65964321:A:AC | donor_gain | 1.0000 |
| 7:65964322:C:CC | donor_gain | 1.0000 |
| 7:65964322:CA:C | donor_gain | 1.0000 |
| 7:65964322:CACT:C | donor_gain | 1.0000 |
| 7:65964322:CACTG:C | donor_gain | 1.0000 |
| 7:65964454:GGATC:G | acceptor_gain | 1.0000 |
| 7:65964455:GATC:G | acceptor_gain | 1.0000 |
| 7:65964456:ATC:A | acceptor_gain | 1.0000 |
| 7:65964457:TC:T | acceptor_gain | 1.0000 |
| 7:65964458:CC:C | acceptor_gain | 1.0000 |
| 7:65964459:C:CC | acceptor_gain | 1.0000 |
| 7:65964459:C:T | acceptor_gain | 1.0000 |
| 7:65964464:A:AC | acceptor_gain | 1.0000 |
| 7:65964467:C:CT | acceptor_gain | 1.0000 |
| 7:65964468:A:T | acceptor_gain | 1.0000 |
| 7:65964472:C:CT | acceptor_gain | 1.0000 |
| 7:65964473:A:T | acceptor_gain | 1.0000 |
| 7:65967729:A:AT | donor_loss | 1.0000 |
| 7:65974292:CACTT:C | donor_loss | 1.0000 |
| 7:65974293:A:AC | donor_gain | 1.0000 |
| 7:65974293:A:C | donor_loss | 1.0000 |
| 7:65974293:ACTT:A | donor_gain | 1.0000 |
| 7:65974294:C:CC | donor_gain | 1.0000 |
AlphaMissense
4252 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 7:65964353:A:G | W587R | 0.998 |
| 7:65964353:A:T | W587R | 0.998 |
| 7:65974350:A:G | W446R | 0.998 |
| 7:65974350:A:T | W446R | 0.998 |
| 7:65974618:G:C | S384R | 0.997 |
| 7:65974618:G:T | S384R | 0.997 |
| 7:65974620:T:G | S384R | 0.997 |
| 7:65961014:T:A | R613S | 0.996 |
| 7:65961014:T:G | R613S | 0.996 |
| 7:65961015:C:G | R613T | 0.996 |
| 7:65961034:C:A | G607W | 0.996 |
| 7:65961034:C:G | G607R | 0.996 |
| 7:65961034:C:T | G607R | 0.996 |
| 7:65964336:G:C | F592L | 0.996 |
| 7:65964336:G:T | F592L | 0.996 |
| 7:65964338:A:G | F592L | 0.996 |
| 7:65974553:T:A | E406V | 0.996 |
| 7:65974625:C:G | R382P | 0.996 |
| 7:65974626:G:T | R382S | 0.996 |
| 7:65967767:G:C | S539R | 0.995 |
| 7:65967767:G:T | S539R | 0.995 |
| 7:65967769:T:G | S539R | 0.995 |
| 7:65974617:G:C | H385D | 0.995 |
| 7:65974664:T:G | D369A | 0.995 |
| 7:65974665:C:G | D369H | 0.995 |
| 7:65974927:C:G | D353H | 0.995 |
| 7:65976065:A:G | W288R | 0.995 |
| 7:65976065:A:T | W288R | 0.995 |
| 7:65979499:A:C | F208L | 0.995 |
| 7:65979499:A:T | F208L | 0.995 |
dbSNP variants (sampled 300 via entrez): RS1000541273 (7:65962076 T>A), RS1000786397 (7:65983479 G>A), RS1000862844 (7:65978424 G>T), RS1000889798 (7:65977854 A>C), RS1000944410 (7:65983048 G>C), RS1001242154 (7:65962480 G>A,T), RS1001242776 (7:65962807 G>C), RS1001551410 (7:65978000 C>T), RS1001662167 (7:65977874 A>G), RS1001705711 (7:65969555 G>A), RS1001820487 (7:65983286 C>A), RS1001950098 (7:65981780 T>C), RS1002042558 (7:65971174 G>A), RS1002061277 (7:65979048 C>A), RS1002151006 (7:65976880 G>A,T)
Disease associations
OMIM: gene MIM:611499 | disease phenotypes: MIM:253220, MIM:236750, MIM:253200
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| mucopolysaccharidosis type 7 | Definitive | Autosomal recessive |
ClinGen Gene-Disease Validity (1)
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
| Disease | Classification | Inheritance |
|---|---|---|
| mucopolysaccharidosis type 7 | Definitive | AR |
Mondo (5): mucopolysaccharidosis type 7 (MONDO:0009662), prostate cancer (MONDO:0008315), non-immune hydrops fetalis (MONDO:0009369), intellectual disability (MONDO:0001071), mucopolysaccharidosis type 6 (MONDO:0009661)
Orphanet (5): Mucopolysaccharidosis type 7 (Orphanet:584), Familial prostate cancer (Orphanet:1331), Non-immune hydrops fetalis (Orphanet:363999), Mucopolysaccharidosis type 6 (Orphanet:583), NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)
HPO phenotypes
82 total (30 of 82 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000007 | Autosomal recessive inheritance |
| HP:0000023 | Inguinal hernia |
| HP:0000158 | Macroglossia |
| HP:0000212 | Gingival overgrowth |
| HP:0000238 | Hydrocephalus |
| HP:0000256 | Macrocephaly |
| HP:0000280 | Coarse facial features |
| HP:0000286 | Epicanthus |
| HP:0000324 | Facial asymmetry |
| HP:0000365 | Hearing impairment |
| HP:0000403 | Recurrent otitis media |
| HP:0000407 | Sensorineural hearing impairment |
| HP:0000470 | Short neck |
| HP:0000505 | Visual impairment |
| HP:0000574 | Thick eyebrow |
| HP:0000613 | Photophobia |
| HP:0000687 | Widely spaced teeth |
| HP:0000767 | Pectus excavatum |
| HP:0000768 | Pectus carinatum |
| HP:0000926 | Platyspondyly |
| HP:0000943 | Dysostosis multiplex |
| HP:0001004 | Lymphedema |
| HP:0001007 | Hirsutism |
| HP:0001249 | Intellectual disability |
| HP:0001252 | Hypotonia |
| HP:0001270 | Motor delay |
| HP:0001371 | Flexion contracture |
| HP:0001376 | Limitation of joint mobility |
| HP:0001387 | Joint stiffness |
| HP:0001537 | Umbilical hernia |
GWAS associations
1 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST90013406_127 | Liver enzyme levels (alkaline phosphatase) | 3.000000e-15 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004533 | alkaline phosphatase measurement |
MeSH disease descriptors (4)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D008607 | Intellectual Disability | C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539 |
| D009087 | Mucopolysaccharidosis VI | C16.320.565.202.715.670; C16.320.565.595.600.670; C17.300.550.575.670; C18.452.648.202.715.670; C18.452.648.595.600.670 |
| D016538 | Mucopolysaccharidosis VII | C16.320.565.202.715.675; C16.320.565.595.600.675; C17.300.550.575.675; C18.452.648.202.715.675; C18.452.648.595.600.675 |
| D011471 | Prostatic Neoplasms | C04.588.945.440.770; C12.100.500.260.750; C12.100.500.565.625; C12.200.294.260.750; C12.200.294.565.625; C12.200.758.409.750; C12.900.619.750 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL2728 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 49,362 (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 |
|---|---|---|---|
| CHEMBL90593 | PRASTERONE | 4 | 23,422 |
| CHEMBL150 | KAEMPFEROL | 1 | 25,940 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
117 measured of 155 human assays (157 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 4-chloro-N-[(4-chlorophenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 30 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[(3-methylphenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 30 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[(2-chlorophenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 40 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[(3-fluorophenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 40 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-(3-methoxyphenyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 70 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-(3-chlorophenyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 70 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[(3-chlorophenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 90 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-(naphthalen-1-ylmethyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 90 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-(naphthalen-1-ylmethyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 90 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[(4-methoxyphenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 100 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 5-(3-piperazin-1-ylphenoxy)-N-(2-pyrrolidin-1-ylethyl)thiophene-2-sulfonamide | IC50 | 120 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-methyl-N-(naphthalen-1-ylmethyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 120 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[(3,5-dichlorophenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 130 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-[3-(dimethylamino)propyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 150 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-(4-methoxyphenyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 170 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[2-(3,4-dimethoxyphenyl)ethyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 190 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-[2-(N-ethyl-3-methylanilino)ethyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 200 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-[(2-bromophenyl)methyl]-4-chloro-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 210 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-[(2,4-dimethylphenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 210 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-(1,3-benzodioxol-5-ylmethyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 220 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-(4-methoxyphenyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 230 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-[2-(4-chlorophenyl)ethyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 240 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[2-(2-fluorophenyl)ethyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 270 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-(cyclohexylmethyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 270 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-benzyl-4-chloro-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 280 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-[(3,4-dimethoxyphenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 290 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-5-(3-piperazin-1-ylphenoxy)-N-[[3-(trifluoromethyl)phenyl]methyl]thiophene-2-sulfonamide | IC50 | 290 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-(naphthalen-1-ylmethyl)-5-(4-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 300 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[(3,5-dimethoxyphenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 310 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-[3-(2-oxopyrrolidin-1-yl)propyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 320 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-(1,3-benzodioxol-5-ylmethyl)-4-chloro-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 320 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-[2-(2-fluorophenyl)ethyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 330 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 330 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[(3,4-dimethoxyphenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 340 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[(3-methoxyphenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 350 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-(3-methylsulfanylpropyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 390 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[(2,4-dimethylphenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 410 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-(4-phenylbutan-2-yl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 430 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| (E)-5-chloro-N’-(2,4,5-trihydroxybenzylidene)-1H-indole-2-carbohydrazide (10) | IC50 | 500 nM | |
| 4-chloro-N-[2-(4-chlorophenyl)ethyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 500 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-cyclopentyl-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 510 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-[2-(4-methoxyphenyl)ethyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 510 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-cycloheptyl-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 560 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-[(3-methoxyphenyl)methyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 570 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 5-(3-piperazin-1-ylphenoxy)-N-(thiophen-2-ylmethyl)thiophene-2-sulfonamide | IC50 | 600 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 5-(3-piperazin-1-ylphenoxy)-N-(2-thiophen-2-ylethyl)thiophene-2-sulfonamide | IC50 | 630 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-(oxolan-2-ylmethyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 710 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| 4-chloro-N-[3-(2-oxopyrrolidin-1-yl)propyl]-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 730 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| ethyl 4-[[5-(3-piperazin-1-ylphenoxy)thiophen-2-yl]sulfonylamino]piperidine-1-carboxylate | IC50 | 730 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| N-cyclohexyl-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | IC50 | 750 nM | US-9617239: Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
ChEMBL bioactivities
278 potent at pChembl≥5 of 416 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.01 | IC50 | 0.984 | nM | CHEMBL3980115 |
| 8.93 | IC50 | 1.17 | nM | CHEMBL3980115 |
| 8.47 | EC50 | 3.41 | nM | CHEMBL3980115 |
| 8.45 | EC50 | 3.58 | nM | CHEMBL3980115 |
| 8.10 | IC50 | 8 | nM | CHEMBL5409470 |
| 8.01 | IC50 | 9.75 | nM | CHEMBL5273557 |
| 7.75 | EC50 | 17.7 | nM | CHEMBL3903683 |
| 7.70 | IC50 | 20 | nM | CHEMBL4635113 |
| 7.55 | EC50 | 28.3 | nM | CHEMBL1236932 |
| 7.54 | EC50 | 29 | nM | CHEMBL3903683 |
| 7.52 | IC50 | 30 | nM | CHEMBL4635884 |
| 7.52 | IC50 | 30 | nM | CHEMBL4633508 |
| 7.48 | EC50 | 33.2 | nM | CHEMBL1236932 |
| 7.40 | IC50 | 40 | nM | CHEMBL4649028 |
| 7.40 | IC50 | 40 | nM | CHEMBL4647420 |
| 7.16 | IC50 | 70 | nM | CHEMBL3289121 |
| 7.16 | IC50 | 70 | nM | CHEMBL5863393 |
| 7.16 | IC50 | 70 | nM | CHEMBL5915942 |
| 7.05 | IC50 | 90 | nM | CHEMBL4648659 |
| 7.05 | IC50 | 90 | nM | CHEMBL4635113 |
| 7.05 | IC50 | 90 | nM | CHEMBL4634028 |
| 7.03 | EC50 | 92.4 | nM | CHEMBL2335167 |
| 7.00 | EC50 | 99.9 | nM | CHEMBL2335167 |
| 7.00 | IC50 | 100 | nM | CHEMBL4165927 |
| 7.00 | IC50 | 100 | nM | CHEMBL4168635 |
| 7.00 | IC50 | 100 | nM | CHEMBL4642327 |
| 7.00 | IC50 | 100 | nM | CHEMBL4644220 |
| 6.93 | IC50 | 118 | nM | CHEMBL4642420 |
| 6.92 | IC50 | 120 | nM | CHEMBL4632976 |
| 6.92 | IC50 | 120 | nM | CHEMBL6014082 |
| 6.92 | IC50 | 120 | nM | CHEMBL4642704 |
| 6.89 | IC50 | 130 | nM | CHEMBL4643487 |
| 6.85 | IC50 | 142 | nM | CHEMBL4641808 |
| 6.82 | IC50 | 150 | nM | CHEMBL5950647 |
| 6.77 | IC50 | 170 | nM | CHEMBL5965722 |
| 6.72 | IC50 | 190 | nM | CHEMBL5864563 |
| 6.70 | IC50 | 200 | nM | CHEMBL4177204 |
| 6.70 | IC50 | 200 | nM | CHEMBL4643914 |
| 6.70 | IC50 | 200 | nM | CHEMBL5840028 |
| 6.68 | IC50 | 210 | nM | CHEMBL5992833 |
| 6.68 | IC50 | 210 | nM | CHEMBL5953913 |
| 6.67 | IC50 | 212.6 | nM | CHEMBL2335167 |
| 6.66 | EC50 | 221.2 | nM | CHEMBL1236933 |
| 6.66 | IC50 | 220 | nM | CHEMBL5907131 |
| 6.64 | IC50 | 230.6 | nM | CHEMBL2335167 |
| 6.64 | IC50 | 230 | nM | CHEMBL5866010 |
| 6.63 | EC50 | 233.2 | nM | CHEMBL1236933 |
| 6.62 | IC50 | 240 | nM | CHEMBL6031655 |
| 6.57 | IC50 | 270 | nM | CHEMBL5928918 |
| 6.57 | IC50 | 270 | nM | CHEMBL5956299 |
PubChem BioAssay actives
201 with measured affinity, of 502 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 |
|---|---|---|---|---|
| 4-(13-piperazin-1-yl-11-thia-9,14,15,16-tetrazatetracyclo[8.7.0.02,7.012,17]heptadeca-1(10),2(7),8,12(17),13,15-hexaen-8-yl)morpholine | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.0012 | uM |
| (5S,6R,7S,8S)-6,7,8-trihydroxy-2-[2-(3-phenoxyphenyl)ethyl]-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid | 2018409: Inhibition of recombinant human GUSbeta using 4-MUG as substrate pre-incubated for 10 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | ic50 | 0.0080 | uM |
| (5S,6R,7S,8S)-6,7,8-trihydroxy-2-[2-[4-(trifluoromethyl)phenyl]ethyl]-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid | 1922231: Inhibition of human beta-glucuronidase | ic50 | 0.0097 | uM |
| 4-chloro-N-(naphthalen-1-ylmethyl)-5-(3-piperazin-1-ylphenoxy)thiophene-2-sulfonamide | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.0200 | uM |
| 2-(2-ethoxyphenyl)-3H-quinazolin-4-one | 1656455: Inhibition of beta-glucuronidase (unknown origin) using p-nitrophenyl-beta-d-glucuronide as substrate after 30 mins | ic50 | 0.0700 | uM |
| 1-[[4-[bis(1H-indol-3-yl)methyl]benzoyl]amino]-3-(2-fluorophenyl)thiourea | 1656455: Inhibition of beta-glucuronidase (unknown origin) using p-nitrophenyl-beta-d-glucuronide as substrate after 30 mins | ic50 | 0.1000 | uM |
| N-[(E)-(2,3-dihydroxyphenyl)methylideneamino]-3-[[5-[[(E)-(2,3-dihydroxyphenyl)methylideneamino]carbamoyl]-1H-indol-3-yl]-(4-methylphenyl)methyl]-1H-indole-5-carboxamide | 1494144: Inhibition of human beta-glucuronidase | ic50 | 0.1000 | uM |
| 3-[(4-methylphenyl)-[5-[[(E)-(2,4,5-trihydroxyphenyl)methylideneamino]carbamoyl]-1H-indol-3-yl]methyl]-N-[(E)-(2,4,5-trihydroxyphenyl)methylideneamino]-1H-indole-5-carboxamide | 1494144: Inhibition of human beta-glucuronidase | ic50 | 0.1000 | uM |
| 1-[(6,8-dimethyl-2-oxo-1H-quinolin-3-yl)methyl]-1-(2-hydroxyethyl)-3-(2-methylphenyl)urea | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.1180 | uM |
| 1-[[4-[bis(1H-indol-3-yl)methyl]benzoyl]amino]-3-(3,4-dichlorophenyl)thiourea | 1801941: β-Glucuronidase Bioassay from Article 10.1016/j.bioorg.2016.07.008: “Synthesis, ß-glucuronidase inhibition and molecular docking studies of hybrid bisindole-thiosemicarbazides analogs.” | ic50 | 0.1200 | uM |
| 1-[[4-[bis(1H-indol-3-yl)methyl]benzoyl]amino]-3-[4-(trifluoromethyl)phenyl]thiourea | 1656455: Inhibition of beta-glucuronidase (unknown origin) using p-nitrophenyl-beta-d-glucuronide as substrate after 30 mins | ic50 | 0.1200 | uM |
| 1-[(6,8-dimethyl-2-oxo-1H-quinolin-3-yl)methyl]-3-(4-fluoro-2-methylphenyl)-1-(2-hydroxyethyl)urea | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.1420 | uM |
| 3-[(4-methylphenyl)-[5-[[(E)-(2,4,6-trihydroxyphenyl)methylideneamino]carbamoyl]-1H-indol-3-yl]methyl]-N-[(E)-(2,4,6-trihydroxyphenyl)methylideneamino]-1H-indole-5-carboxamide | 1494144: Inhibition of human beta-glucuronidase | ic50 | 0.2000 | uM |
| 1-[(6,8-dimethyl-2-oxo-1H-quinolin-3-yl)methyl]-3-(4-ethoxyphenyl)-1-(2-hydroxyethyl)thiourea | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.2800 | uM |
| N-[(E)-(3,4-dihydroxyphenyl)methylideneamino]-3-[[5-[[(E)-(3,4-dihydroxyphenyl)methylideneamino]carbamoyl]-1H-indol-3-yl]-(4-methylphenyl)methyl]-1H-indole-5-carboxamide | 1494144: Inhibition of human beta-glucuronidase | ic50 | 0.3000 | uM |
| N-[(E)-(2,4-dihydroxyphenyl)methylideneamino]-3-[[5-[[(E)-(2,4-dihydroxyphenyl)methylideneamino]carbamoyl]-1H-indol-3-yl]-(4-methylphenyl)methyl]-1H-indole-5-carboxamide | 1494144: Inhibition of human beta-glucuronidase | ic50 | 0.3000 | uM |
| 3-(2-bromophenyl)-1-[(6,8-dimethyl-2-oxo-1H-quinolin-3-yl)methyl]-1-(2-hydroxyethyl)urea | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.3470 | uM |
| N,N-diethyl-6-methyl-2-sulfanylidene-4-thiophen-2-yl-3,4-dihydro-1H-pyrimidine-5-carboxamide | 1667339: Inhibition of beta-glucuronidase (unknown origin) using p-nitrophenyl-beta-D-glucuronide as substrate pre-incubated for 30 mins followed by substrate addition by spectrophotometric method | ic50 | 0.3500 | uM |
| 1-[(6,8-dimethyl-2-oxo-1H-quinolin-3-yl)methyl]-1-(2-hydroxyethyl)-3-(4-methoxyphenyl)thiourea | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.3700 | uM |
| 1-[(6,8-dimethyl-2-oxo-1H-quinolin-3-yl)methyl]-1-(2-hydroxyethyl)-3-(2-propan-2-ylphenyl)urea | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.4680 | uM |
| 1-[[4-[bis(1H-indol-3-yl)methyl]benzoyl]amino]-3-(2-chlorophenyl)thiourea | 1656455: Inhibition of beta-glucuronidase (unknown origin) using p-nitrophenyl-beta-d-glucuronide as substrate after 30 mins | ic50 | 0.5000 | uM |
| 5-chloro-N-[(E)-(2,4,5-trihydroxyphenyl)methylideneamino]-1H-indole-2-carboxamide | 1656455: Inhibition of beta-glucuronidase (unknown origin) using p-nitrophenyl-beta-d-glucuronide as substrate after 30 mins | ic50 | 0.5000 | uM |
| 3-[5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-yl]benzene-1,2-diol | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.5000 | uM |
| 2,7-dimethyl-4-piperazin-1-yl-4b,5,6,7,8,8a-hexahydro-[1]benzothiolo[2,3-d]pyrimidine | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.5400 | uM |
| 9-[[1-(pyridin-3-ylmethyl)triazol-4-yl]methyl]carbazole | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.5500 | uM |
| (E)-3-(4-chlorophenyl)-1-(2,5-dihydroxyphenyl)prop-2-en-1-one | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.6000 | uM |
| 2-(3,4-dimethoxyphenyl)-3H-quinazolin-4-one | 1153850: Inhibition of beta-glucuronidase activity (unknown origin) assessed as p-nitrophenol formation after 30 mins using p-nitrophenyl-beta-D-glucuronide as substrate by spectrophotometry | ic50 | 0.6000 | uM |
| N,N-diethyl-6-methyl-4-(3-nitrophenyl)-2-sulfanylidene-3,4-dihydro-1H-pyrimidine-5-carboxamide | 1667339: Inhibition of beta-glucuronidase (unknown origin) using p-nitrophenyl-beta-D-glucuronide as substrate pre-incubated for 30 mins followed by substrate addition by spectrophotometric method | ic50 | 0.6000 | uM |
| N,N-diethyl-4-(3-hydroxyphenyl)-6-methyl-2-sulfanylidene-3,4-dihydro-1H-pyrimidine-5-carboxamide | 1667339: Inhibition of beta-glucuronidase (unknown origin) using p-nitrophenyl-beta-D-glucuronide as substrate pre-incubated for 30 mins followed by substrate addition by spectrophotometric method | ic50 | 0.7200 | uM |
| 1-(3-bromo-4-hydroxyphenyl)-2-[4-(carbazol-9-ylmethyl)triazol-1-yl]ethanone | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.7500 | uM |
| 3-(2-cyclopropylphenyl)-1-[(6,8-dimethyl-2-oxo-1H-quinolin-3-yl)methyl]-1-(2-hydroxyethyl)urea | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.7590 | uM |
| 4,4-dimethyl-14-sulfanylidene-5-oxa-8-thia-10,12,13,15-tetrazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2(7),10-trien-16-one | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.7590 | uM |
| N,N-diethyl-4-(3-hydroxy-4-methoxyphenyl)-6-methyl-2-sulfanylidene-3,4-dihydro-1H-pyrimidine-5-carboxamide | 1667339: Inhibition of beta-glucuronidase (unknown origin) using p-nitrophenyl-beta-D-glucuronide as substrate pre-incubated for 30 mins followed by substrate addition by spectrophotometric method | ic50 | 0.7600 | uM |
| 2-[4-[5-(2-fluorophenyl)-1,3,4-oxadiazol-2-yl]phenyl]chromen-4-one | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.8000 | uM |
| (5S,6R,7R,8S)-7,8-dihydroxy-6-methoxy-2-[2-(3-phenoxyphenyl)ethyl]-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid | 2018409: Inhibition of recombinant human GUSbeta using 4-MUG as substrate pre-incubated for 10 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | ic50 | 0.8390 | uM |
| 1-(3-bromo-4-methoxyphenyl)-2-[4-(carbazol-9-ylmethyl)triazol-1-yl]ethanone | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.8500 | uM |
| (E)-4,4,4-triethoxy-1-[3-methyl-4-phenyl-5-[(E)-4,4,4-triethoxybut-2-enoyl]thieno[2,3-b]thiophen-2-yl]but-2-en-1-one | 1165427: Inhibition of beta-glucuronidase (unknown origin) using p-nitrophenyl-beta-D-glucuronide substrate incubated for 30 mins by spectrophotometry | ic50 | 0.9000 | uM |
| 3-[5-(1H-indol-2-ylmethyl)-1,3,4-oxadiazol-2-yl]benzene-1,2-diol | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 0.9000 | uM |
| 3-methoxy-4-[5-[4-[5-(2,4,6-trichlorophenyl)-1,3,4-thiadiazol-2-yl]phenyl]-1,3,4-oxadiazol-2-yl]phenol | 1545107: Inhibition of human beta-glucuronidase pre-incubated for 30 mins before p-nitrophenyl-beta-D-glucuronide substrate addition by spectrophotometry | ic50 | 0.9600 | uM |
| methyl 2-[[2-hydroxyethyl-[(6-methyl-2-oxo-1H-quinolin-3-yl)methyl]carbamothioyl]amino]benzoate | 1656455: Inhibition of beta-glucuronidase (unknown origin) using p-nitrophenyl-beta-d-glucuronide as substrate after 30 mins | ic50 | 1.0600 | uM |
| 2-(4-methoxyphenyl)-3H-quinazolin-4-one | 1153850: Inhibition of beta-glucuronidase activity (unknown origin) assessed as p-nitrophenol formation after 30 mins using p-nitrophenyl-beta-D-glucuronide as substrate by spectrophotometry | ic50 | 1.1000 | uM |
| 4-[5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-yl]benzene-1,2-diol | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 1.1000 | uM |
| N-[(E)-(2,4-dichlorophenyl)methylideneamino]-3-[[5-[[(E)-(2,4-dichlorophenyl)methylideneamino]carbamoyl]-1H-indol-3-yl]-(4-methylphenyl)methyl]-1H-indole-5-carboxamide | 1494144: Inhibition of human beta-glucuronidase | ic50 | 1.1000 | uM |
| 2-[4-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]phenyl]chromen-4-one | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 1.1000 | uM |
| N-[(E)-(2,5-dihydroxyphenyl)methylideneamino]-3-[[5-[[(E)-(2,5-dihydroxyphenyl)methylideneamino]carbamoyl]-1H-indol-3-yl]-(4-methylphenyl)methyl]-1H-indole-5-carboxamide | 1494144: Inhibition of human beta-glucuronidase | ic50 | 1.1400 | uM |
| 2-(3-ethoxy-4-hydroxyphenyl)-3H-quinazolin-4-one | 1153850: Inhibition of beta-glucuronidase activity (unknown origin) assessed as p-nitrophenol formation after 30 mins using p-nitrophenyl-beta-D-glucuronide as substrate by spectrophotometry | ic50 | 1.1700 | uM |
| 2-(2-methyl-5-nitroimidazol-1-yl)ethyl 2-chloro-4,5-difluorobenzoate | 1667338: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 1.2000 | uM |
| N-[(E)-(2-fluorophenyl)methylideneamino]-3-[[5-[[(E)-(2-fluorophenyl)methylideneamino]carbamoyl]-1H-indol-3-yl]-(4-methylphenyl)methyl]-1H-indole-5-carboxamide | 1494144: Inhibition of human beta-glucuronidase | ic50 | 1.2000 | uM |
| 3-[(5-bromo-1H-indol-3-yl)-(6-bromo-1H-indol-3-yl)methyl]benzene-1,2-diol | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 1.2000 | uM |
| 4-[5-(1H-indol-2-ylmethyl)-1,3,4-oxadiazol-2-yl]benzene-1,2-diol | 1656436: Inhibition of beta-glucuronidase (unknown origin) | ic50 | 1.2000 | uM |
CTD chemical–gene interactions
48 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| bisphenol A | increases expression, affects cotreatment | 3 |
| sodium arsenite | increases abundance, affects expression, decreases expression | 3 |
| Ozone | increases oxidation, increases abundance, affects expression, affects cotreatment, increases expression | 3 |
| Valproic Acid | increases expression, increases methylation | 3 |
| methacrylaldehyde | affects cotreatment, increases expression, increases oxidation, increases abundance | 2 |
| epigallocatechin gallate | increases secretion, affects cotreatment, increases expression, decreases reaction | 2 |
| Acetaminophen | increases expression | 2 |
| Acrolein | affects cotreatment, increases expression, increases oxidation, increases abundance | 2 |
| Air Pollutants | increases oxidation, affects expression, affects cotreatment, increases abundance, increases expression | 2 |
| Benzo(a)pyrene | decreases methylation, affects reaction, increases expression, increases reaction | 2 |
| Doxorubicin | decreases expression, affects response to substance | 2 |
| bisphenol F | increases expression | 1 |
| PF-06840003 | decreases expression, decreases reaction | 1 |
| ginger extract | increases abundance, increases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| alpha-pinene | affects cotreatment, increases expression, increases oxidation, increases abundance | 1 |
| benoxaprofen | increases secretion | 1 |
| potassium chromate(VI) | affects cotreatment, increases expression | 1 |
| mannose-6-phosphate | affects reaction, increases expression | 1 |
| Am 580 | increases expression | 1 |
| 6-((2-(4-imidazolyl)ethyl)amino)heptanoic acid 4-toluidide | increases expression, increases reaction | 1 |
| fexofenadine | affects binding, decreases reaction, increases activity, increases expression | 1 |
| ICG 001 | increases expression | 1 |
| bisphenol B | increases expression | 1 |
| jinfukang | increases expression | 1 |
| picoxystrobin | increases expression | 1 |
| bisphenol AF | increases expression | 1 |
| Rosiglitazone | increases expression | 1 |
| Sunitinib | decreases expression | 1 |
| Arsenic | decreases expression, increases abundance | 1 |
ChEMBL screening assays
41 unique, capped per target: 38 binding, 3 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1071205 | Binding | Inhibition of beta-glucuronidase at 10 uM | Synthesis and biological evaluation of nitrogen-containing chalcones as possible anti-inflammatory and antioxidant agents. — Bioorg Med Chem Lett |
| CHEMBL4026921 | ADMET | Inhibition of N-terminal His-tagged human beta-glucuronidase expressed in Escherichia coli BL21 (DE3) assessed as residual activity using pNPG as substrate at 10 uM preincubated for 30 mins followed by substrate addition measured after 1 hr | Specific Inhibition of Bacterial β-Glucuronidase by Pyrazolo[4,3-c]quinoline Derivatives via a pH-Dependent Manner To Suppress Chemotherapy-Induced Intestinal Toxicity. — J Med Chem |
Cellosaurus cell lines
9 cell lines: 6 cancer cell line, 3 finite cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_0P00 | GM02074 | Finite cell line | Female |
| CVCL_D1MZ | Abcam K-562 GUSB KO | Cancer cell line | Female |
| CVCL_D2JJ | Abcam Raji GUSB KO | Cancer cell line | Male |
| CVCL_D5ET | HeLa::TMEM192-3xHA GUSB KO | Cancer cell line | Female |
| CVCL_M988 | GM01850 | Finite cell line | Male |
| CVCL_SQ73 | HAP1 GUSB (-) 1 | Cancer cell line | Male |
| CVCL_SQ74 | HAP1 GUSB (-) 2 | Cancer cell line | Male |
| CVCL_UQ66 | Abcam Jurkat GUSB KO | Cancer cell line | Male |
| CVCL_V751 | GM00121 | Finite cell line | Male |
Clinical trials (associated diseases)
300 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00029224 | PHASE4 | COMPLETED | Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions |
| NCT00035997 | PHASE4 | COMPLETED | Open-label Trial on the Effect of I.V. Zoledronic Acid 4 mg on Bone Density in Hormone Sensitive Prostate Cancer Patients With Bone Metastasis |
| NCT00063609 | PHASE4 | COMPLETED | The Effect of Zoledronic Acid on Bone Loss in Prostate Cancer Patients Undergoing Androgen Deprivation Therapy |
| NCT00103623 | PHASE4 | SUSPENDED | The Plenaxis® Experience Study |
| NCT00106392 | PHASE4 | COMPLETED | A Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy |
| NCT00185029 | PHASE4 | UNKNOWN | MR-Lymphography and Lymph Node Staging in Prostate Cancer |
| NCT00199485 | PHASE4 | COMPLETED | Angelica Sinensis for the Treatment of Hot Flashes in Men Undergoing LHRH Therapy for Prostate Cancer |
| NCT00219219 | PHASE4 | COMPLETED | Zoledronic Acid in the Prevention of Skeletal-related Events in Hormone Refractory and Hormone-sensitive Prostate Cancer Patients With Bone Metastases |
| NCT00219271 | PHASE4 | COMPLETED | Effect Of Zoledronic Acid On Circulating And Bone Marrow-Residing Prostate Cancer Cells In Patients With Clinically Localized Prostate Cancer |
| NCT00237146 | PHASE4 | COMPLETED | Study to Evaluate Zoledronic Acid on Quality of Life and Skeletal-related Events as Adjuvant Treatment in Patients With Hormone-naïve Prostate Cancer and Bone Metastasis Who Have Undergone Orchiectomy |
| NCT00242554 | PHASE4 | COMPLETED | Open-label Phase IV Clinical Trial to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Prostate Cancer and Bone Metastases |
| NCT00280098 | PHASE4 | COMPLETED | Docetaxel in the Treatment of Hormone Refractory Prostate Cancer |
| NCT00293696 | PHASE4 | COMPLETED | Casodex/Zoladex Biomarkers in Localised Prostate Cancer |
| NCT00334139 | PHASE4 | COMPLETED | Effect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer |
| NCT00375765 | PHASE4 | COMPLETED | Effects On Dihydrotestosterone Regulated Gene Expression In Benign Prostatic Hyperplasia Or Prostate Cancer |
| NCT00391690 | PHASE4 | COMPLETED | Evaluation of Bone Markers as Diagnostic Tools for Early Detection of Bone Metastases in Patients With High Risk Prostate Cancer |
| NCT00422708 | PHASE4 | COMPLETED | Local Anesthesia for Prostate Biopsy |
| NCT00526331 | PHASE4 | COMPLETED | Evaluation of Arterial Pressure Based Cardiac Output for Goal-Directed Perioperative Therapy |
| NCT00590213 | PHASE4 | COMPLETED | Compare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX |
| NCT00629330 | PHASE4 | TERMINATED | Dissemination of Prostate Cancer Screening to PCP’s in African American Communities |
| NCT00771966 | PHASE4 | COMPLETED | Radical Prostatectomy and Perioperative Fluid Therapy |
| NCT00805701 | PHASE4 | COMPLETED | Study Assessing The Efficacy And Safety Of Avodart (Dutasteride) At Improving Urinary Symptoms In Men With Prostate Cancer Who Are Undergoing Seed Implantation |
| NCT00859027 | PHASE4 | COMPLETED | Effect Of Risedronate On Bone Mass In Older Men Receiving Neoadjuvant Therapy For Prostate Cancer |
| NCT00906269 | PHASE4 | UNKNOWN | Can Hyperbaric Oxygen Improve Erectile Function Following Surgery for Prostate Cancer |
| NCT00953277 | PHASE4 | COMPLETED | Study of Nerve Reconstruction Using AVANCE in Subjects Who Undergo Robotic Assisted Prostatectomy for Treatment of Prostate Cancer |
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| NCT01161563 | PHASE4 | COMPLETED | Randomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue Administration |
| NCT01230905 | PHASE4 | COMPLETED | Study to Monitor the Effects of Androgen Suppression Treatment on the Heart |
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| NCT01365143 | PHASE4 | TERMINATED | Prospective Randomized Trial Comparing Robotic Versus Open Radical Prostatectomy |
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| NCT01512472 | PHASE4 | TERMINATED | Firmagon (Degarelix) Intermittent Therapy |
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Related Atlas pages
- Associated diseases: mucopolysaccharidosis type 7
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): mucopolysaccharidosis type 6, mucopolysaccharidosis type 7, non-immune hydrops fetalis