MGAT2
gene geneOn this page
Also known as GNT-II
Summary
MGAT2 (alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase, HGNC:7045) is a protein-coding gene on chromosome 14q21.3, encoding Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase (Q10469). Plays an essential role in protein N-glycosylation.
The product of this gene is a Golgi enzyme catalyzing an essential step in the conversion of oligomannose to complex N-glycans. The enzyme has the typical glycosyltransferase domains: a short N-terminal cytoplasmic domain, a hydrophobic non-cleavable signal-anchor domain, and a C-terminal catalytic domain. Mutations in this gene may lead to carbohydrate-deficient glycoprotein syndrome, type II. The coding region of this gene is intronless. Transcript variants with a spliced 5’ UTR may exist, but their biological validity has not been determined.
Source: NCBI Gene 4247 — RefSeq curated summary.
At a glance
- Gene–disease (curated): MGAT2-congenital disorder of glycosylation (Definitive, GenCC)
- Clinical variants (ClinVar): 166 total — 6 pathogenic, 6 likely-pathogenic
- Phenotypes (HPO): 99
- Druggable target: yes — 2 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_002408
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:7045 |
| Approved symbol | MGAT2 |
| Name | alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase |
| Location | 14q21.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | GNT-II |
| Ensembl gene | ENSG00000168282 |
| Ensembl biotype | protein_coding |
| OMIM | 602616 |
| Entrez | 4247 |
Gene structure
Transcript identifiers
Ensembl transcripts: 1 — 1 protein_coding
ENST00000305386
RefSeq mRNA: 1 — MANE Select: NM_002408
NM_002408
CCDS: CCDS9690
Canonical transcript exons
ENST00000305386 — 1 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001175172 | 49620799 | 49623481 |
Expression profiles
Bgee: expression breadth ubiquitous, 278 present calls, max score 96.44.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 21.2176 / max 125.4906, expressed in 1814 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 139438 | 20.7873 | 1813 |
| 139437 | 0.4304 | 209 |
Top tissues by expression
294 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| jejunal mucosa | UBERON:0000399 | 96.44 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 94.96 | gold quality |
| colonic mucosa | UBERON:0000317 | 94.64 | gold quality |
| decidua | UBERON:0002450 | 93.90 | gold quality |
| periodontal ligament | UBERON:0008266 | 92.87 | gold quality |
| corpus epididymis | UBERON:0004359 | 92.10 | gold quality |
| caput epididymis | UBERON:0004358 | 91.94 | gold quality |
| bronchial epithelial cell | CL:0002328 | 91.74 | gold quality |
| cauda epididymis | UBERON:0004360 | 91.66 | gold quality |
| seminal vesicle | UBERON:0000998 | 91.08 | gold quality |
| adult organism | UBERON:0007023 | 90.70 | gold quality |
| skin of hip | UBERON:0001554 | 90.60 | gold quality |
| epithelium of bronchus | UBERON:0002031 | 90.07 | gold quality |
| superficial temporal artery | UBERON:0001614 | 90.05 | gold quality |
| choroid plexus epithelium | UBERON:0003911 | 89.90 | gold quality |
| pericardium | UBERON:0002407 | 89.80 | gold quality |
| bronchus | UBERON:0002185 | 89.75 | gold quality |
| granulocyte | CL:0000094 | 89.71 | gold quality |
| duodenum | UBERON:0002114 | 89.32 | gold quality |
| monocyte | CL:0000576 | 89.25 | gold quality |
| mononuclear cell | CL:0000842 | 89.13 | gold quality |
| parotid gland | UBERON:0001831 | 89.11 | gold quality |
| leukocyte | CL:0000738 | 89.10 | gold quality |
| cartilage tissue | UBERON:0002418 | 88.80 | gold quality |
| bone marrow cell | CL:0002092 | 88.53 | gold quality |
| pigmented layer of retina | UBERON:0001782 | 88.43 | gold quality |
| retina | UBERON:0000966 | 88.40 | gold quality |
| oral cavity | UBERON:0000167 | 88.25 | gold quality |
| mammary duct | UBERON:0001765 | 88.22 | gold quality |
| heart right ventricle | UBERON:0002080 | 88.00 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 6.67 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): NR1I2
miRNA regulators (miRDB)
89 targeting MGAT2, 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-200B-3P | 100.00 | 73.31 | 2693 |
| HSA-MIR-200C-3P | 100.00 | 73.35 | 2685 |
| HSA-MIR-429 | 100.00 | 73.44 | 2698 |
| HSA-MIR-4262 | 100.00 | 73.26 | 3931 |
| HSA-MIR-5692A | 100.00 | 74.40 | 6850 |
| HSA-LET-7A-3P | 100.00 | 74.03 | 3932 |
| HSA-LET-7B-3P | 100.00 | 74.08 | 3913 |
| HSA-LET-7F-1-3P | 100.00 | 74.02 | 3928 |
| HSA-MIR-98-3P | 100.00 | 74.08 | 3907 |
| 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-548AW | 99.99 | 72.57 | 3559 |
| HSA-MIR-181A-5P | 99.99 | 72.96 | 2995 |
| HSA-MIR-181B-5P | 99.99 | 72.97 | 2996 |
| HSA-MIR-181C-5P | 99.99 | 72.95 | 2996 |
| HSA-MIR-181D-5P | 99.99 | 73.04 | 2997 |
| HSA-MIR-3662 | 99.99 | 73.82 | 5684 |
| HSA-MIR-150-5P | 99.99 | 66.69 | 1976 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-371B-5P | 99.99 | 75.34 | 4759 |
| HSA-MIR-12136 | 99.98 | 72.81 | 5713 |
| HSA-MIR-373-5P | 99.98 | 75.36 | 4753 |
| HSA-MIR-616-5P | 99.98 | 75.58 | 4775 |
| HSA-MIR-520D-5P | 99.98 | 73.34 | 4883 |
| HSA-MIR-524-5P | 99.98 | 73.43 | 4882 |
| HSA-MIR-570-3P | 99.96 | 72.41 | 4910 |
| HSA-MIR-5688 | 99.96 | 73.23 | 4504 |
Literature-anchored findings (GeneRIF, showing 5)
- Golgi N-glycosyltransferases beta-1,2-N-acetylglucosaminyltransferase I, beta-1,2-N-acetylglucosaminyltransferase II, 1,4-galactosyltransferase I, and alpha-2,6-sialyltransferase I form both homo- and heterodimeric enzyme complexes in live cells (PMID:20378551)
- UDP-galactose (SLC35A2) and UDP-N-acetylglucosamine (SLC35A3) Transporters Form Glycosylation-related Complexes with Mannoside Acetylglucosaminyltransferases (Mgats). (PMID:25944901)
- The recombinant hGnTII was purified from silkworm larval hemolymph in two steps by using tandem affinity purification tags, with a yield of approximately 120 mug from 10 mL hemolymph, and exhibited glycosyltransferase activity and strict substrate specificity. The enzyme was found to be N-glycosylated by the enzymatic cleavage of glycans, while hGnTII expressed in insect cells had not been reported to be glycosylated. (PMID:29409697)
- These data suggest that substrate binding by MGAT2 employs both conserved and convergent catalytic subsite modules to provide substrate selectivity and catalysis. More broadly, the MGAT2 active-site architecture demonstrates how glycosyltransferases create complementary modular templates for regiospecific extension of glycan structures in mammalian cells. (PMID:29666272)
- Immune dysfunction in MGAT2-CDG: A clinical report and review of the literature. (PMID:33044030)
Cross-species orthologs
5 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | mgat2 | ENSDARG00000052408 |
| mus_musculus | Mgat2 | ENSMUSG00000043998 |
| rattus_norvegicus | Mgat2 | ENSRNOG00000004234 |
| drosophila_melanogaster | Mgat2 | FBGN0039738 |
| caenorhabditis_elegans | WBGENE00001645 |
Protein
Protein identifiers
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase — Q10469 (reviewed: Q10469)
Alternative names: Beta-1,2-N-acetylglucosaminyltransferase II, GlcNAc-T II, Mannoside acetylglucosaminyltransferase 2, N-glycosyl-oligosaccharide-glycoprotein N-acetylglucosaminyltransferase II
All UniProt accessions (1): Q10469
UniProt curated annotations — full annotation on UniProt →
Function. Plays an essential role in protein N-glycosylation. Catalyzes the transfer of N-acetylglucosamine (GlcNAc) onto the free terminal mannose moiety in the core structure of the nascent N-linked glycan chain, giving rise to the second branch in complex glycans.
Subunit / interactions. Homodimer.
Subcellular location. Golgi apparatus membrane.
Disease relevance. Congenital disorder of glycosylation 2A (CDG2A) [MIM:212066] A multisystem disorder caused by a defect in glycoprotein biosynthesis and characterized by under-glycosylated serum glycoproteins. Congenital disorders of glycosylation result in a wide variety of clinical features, such as defects in the nervous system development, psychomotor retardation, dysmorphic features, hypotonia, coagulation disorders, and immunodeficiency. The broad spectrum of features reflects the critical role of N-glycoproteins during embryonic development, differentiation, and maintenance of cell functions. The disease is caused by variants affecting the gene represented in this entry.
Pathway. Protein modification; protein glycosylation.
Similarity. Belongs to the glycosyltransferase 16 (GT16) protein family.
RefSeq proteins (1): NP_002399* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR007754 | GlcNAc_II | Family |
| IPR029044 | Nucleotide-diphossugar_trans | Homologous_superfamily |
Pfam: PF05060
Enzyme classification (BRENDA):
- EC 2.4.1.143 — alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase (BRENDA: 19 organisms, 41 substrates, 17 inhibitors, 35 Km, 16 kcat entries)
Substrate kinetics (BRENDA)
17 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| BETA-D-GLCNAC-(1->2)-ALPHA-D-MAN-(1->3)-[ALPHA-D | 0.062–0.557 | 8 |
| UDP-ALPHA-D-GLCNAC | 0.295–4.3 | 8 |
| ALPHA-D-MANNOSYL-1,6-(N-ACETYL-D-GLUCOSAMINYL-1, | 0.0166–0.19 | 3 |
| UDP-N-ACETYLGLUCOSAMINE | 0.018–0.96 | 3 |
| 3-DEOXY-MANALPHA(1-6)(GLCNACBETA(1-2)MANALPHA(1- | 3.7 | 1 |
| 3-O-METHYL-MANALPHA(1-6)(GLCNACBETA(1-2)MANALPHA | 0.26 | 1 |
| 4-DEOXY-MANALPHA(1-6)(GLCNACBETA(1-2)MANALPHA(1- | 0.22 | 1 |
| 4-O-METHYL-ALPHA-D-MANNOSYL-1,6-(N-ACETYL-BETA-D | 0.16 | 1 |
| 4-O-METHYL-MANALPHA(1-6)(GLCNACBETA(1-2)MANALPHA | 0.26 | 1 |
| 6-DEOXY-MANALPHA(1-6)(GLCNACBETA(1-2)MANALPHA(1- | 0.25 | 1 |
| 6-O-METHYL-MANALPHA(1-6)(GLCNACBETA(1-2)MANALPHA | 0.2 | 1 |
| ALPHA-D-MANNOSYL-1,6-(N-ACETYL-BETA-D-GLUCOSAMIN | 0.55 | 1 |
| ALPHA-D-MANNOSYL-1,6-(N-ACETYL-BETA-D-GLUCOSAMIN | 0.13 | 1 |
| MANALPHA(1-6)(GLCNACBETA(1-2)-6-DEOXY-MANALPHA(1 | 0.55 | 1 |
| MANALPHA(1-6)(GLCNACBETA(1-2)4-O-METHYL-MANALPHA | 0.16 | 1 |
Catalyzed reactions (Rhea), 1 shown:
- an N(4)-{beta-D-GlcNAc-(1->2)-alpha-D-Man-(1->3)-[alpha-D-Man-(1->6)]-beta-D-Man-(1->4)-beta-D-GlcNAc-(1->4)-beta-D-GlcNAc}-L-asparaginyl-[protein] + UDP-N-acetyl-alpha-D-glucosamine = N(4)-{beta-D-GlcNAc-(1->2)-alpha-D-Man-(1->3)-[beta-D-GlcNAc-(1->2)-alpha-D-Man-(1->6)]-beta-D-Man-(1->4)-beta-D-GlcNAc-(1->4)-beta-D-GlcNAc}-L-asparaginyl-[protein] + UDP + H(+) (RHEA:12941)
UniProt features (63 total): helix 15, strand 14, mutagenesis site 8, binding site 6, disulfide bond 5, turn 5, sequence variant 3, topological domain 2, glycosylation site 2, chain 1, transmembrane region 1, sequence conflict 1
Structure
Experimental structures (PDB)
3 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 5VCM | X-RAY DIFFRACTION | 1.6 |
| 5VCR | X-RAY DIFFRACTION | 1.99 |
| 5VCS | X-RAY DIFFRACTION | 2.8 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q10469-F1 | 86.01 | 0.75 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Ligand- & substrate-binding residues (6): 123–127; 154; 229–233; 261; 298; 374
Disulfide bonds (5): 196–210, 283–286, 334–357, 339–440, 378–386
Glycosylation sites (2): 69, 86
Mutagenesis-validated functional residues (8):
| Position | Phenotype |
|---|---|
| 198 | strongly decreased catalytic activity and affinity for udp-glcnac. |
| 217 | nearly abolishes catalytic activity. |
| 259 | loss of catalytic activity. |
| 294 | strongly decreased catalytic activity and affinity for udp-glcnac. |
| 318 | strongly decreased catalytic activity and affinity for udp-glcnac. |
| 344 | nearly abolishes catalytic activity and strongly decreases affinity for udp-glcnac. |
| 346 | loss of catalytic activity. |
| 347 | loss of catalytic activity. |
Function
Pathways and Gene Ontology
Reactome pathways
18 pathways
| ID | Pathway |
|---|---|
| R-HSA-4793952 | Defective MGAT2 causes CDG-2a |
| R-HSA-9694548 | Maturation of spike protein |
| R-HSA-975578 | Reactions specific to the complex N-glycan synthesis pathway |
| R-HSA-1643685 | Disease |
| R-HSA-3781860 | Diseases associated with N-glycosylation of proteins |
| R-HSA-3781865 | Diseases of glycosylation |
| R-HSA-392499 | Metabolism of proteins |
| R-HSA-446203 | Asparagine N-linked glycosylation |
| R-HSA-5663205 | Infectious disease |
| R-HSA-5668914 | Diseases of metabolism |
| R-HSA-597592 | Post-translational protein modification |
| R-HSA-948021 | Transport to the Golgi and subsequent modification |
| R-HSA-9679506 | SARS-CoV Infections |
| R-HSA-9694516 | SARS-CoV-2 Infection |
| R-HSA-9694635 | Translation of Structural Proteins |
| R-HSA-975576 | N-glycan antennae elongation in the medial/trans-Golgi |
| R-HSA-9772573 | Late SARS-CoV-2 Infection Events |
| R-HSA-9824446 | Viral Infection Pathways |
MSigDB gene sets: 469 (showing top):
GSE18804_SPLEEN_MACROPHAGE_VS_TUMORAL_MACROPHAGE_UP, GSE45365_NK_CELL_VS_CD8A_DC_UP, RNGTGGGC_UNKNOWN, GOBP_OLIGOSACCHARIDE_METABOLIC_PROCESS, GOBP_PROTEIN_N_LINKED_GLYCOSYLATION, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, KEGG_N_GLYCAN_BIOSYNTHESIS, GOBP_CARBOHYDRATE_DERIVATIVE_METABOLIC_PROCESS, MARTINEZ_RB1_TARGETS_UP, ONKEN_UVEAL_MELANOMA_UP, GOBP_CARBOHYDRATE_DERIVATIVE_BIOSYNTHETIC_PROCESS, FISCHER_G2_M_CELL_CYCLE, GROSS_HYPOXIA_VIA_ELK3_UP, GROSS_HYPOXIA_VIA_HIF1A_UP, GROSS_HYPOXIA_VIA_ELK3_AND_HIF1A_DN
GO Biological Process (5): protein N-linked glycosylation (GO:0006487), oligosaccharide biosynthetic process (GO:0009312), obsolete protein N-linked glycosylation via asparagine (GO:0018279), viral protein processing (GO:0019082), obsolete protein glycosylation (GO:0006486)
GO Molecular Function (6): alpha-1,6-mannosylglycoprotein 2-beta-N-acetylglucosaminyltransferase activity (GO:0008455), manganese ion binding (GO:0030145), protein homodimerization activity (GO:0042803), transferase activity (GO:0016740), glycosyltransferase activity (GO:0016757), metal ion binding (GO:0046872)
GO Cellular Component (4): Golgi membrane (GO:0000139), Golgi apparatus (GO:0005794), Golgi stack (GO:0005795), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-15 pathways:
| Category | Pathways |
|---|---|
| Disease | 2 |
| Diseases associated with N-glycosylation of proteins | 1 |
| Translation of Structural Proteins | 1 |
| N-glycan antennae elongation in the medial/trans-Golgi | 1 |
| Diseases of glycosylation | 1 |
| Diseases of metabolism | 1 |
| Post-translational protein modification | 1 |
| Metabolism of proteins | 1 |
| Asparagine N-linked glycosylation | 1 |
| Viral Infection Pathways | 1 |
| SARS-CoV Infections | 1 |
| Late SARS-CoV-2 Infection Events | 1 |
| Transport to the Golgi and subsequent modification | 1 |
| SARS-CoV-2 Infection | 1 |
| Infectious disease | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| glycoprotein biosynthetic process | 1 |
| oligosaccharide metabolic process | 1 |
| carbohydrate biosynthetic process | 1 |
| viral process | 1 |
| viral gene expression | 1 |
| acetylglucosaminyltransferase activity | 1 |
| catalytic activity, acting on a glycoprotein | 1 |
| transition metal ion binding | 1 |
| identical protein binding | 1 |
| protein dimerization activity | 1 |
| catalytic activity | 1 |
| transferase activity | 1 |
| cation binding | 1 |
| Golgi apparatus | 1 |
| bounding membrane of organelle | 1 |
| cytoplasm | 1 |
| endomembrane system | 1 |
| intracellular membrane-bounded organelle | 1 |
| Golgi apparatus subcompartment | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
550 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| MGAT2 | MGAT1 | P26572 | 943 |
| MGAT2 | MAN2A1 | Q16706 | 790 |
| MGAT2 | MGAT5 | Q09328 | 785 |
| MGAT2 | MAN2A2 | P49641 | 726 |
| MGAT2 | MGAT3 | Q09327 | 716 |
| MGAT2 | MGAT4A | Q9UM21 | 692 |
| MGAT2 | MGAT4B | Q9UQ53 | 692 |
| MGAT2 | FUT8 | Q9BYC5 | 677 |
| MGAT2 | POMGNT1 | Q8WZA1 | 654 |
| MGAT2 | GUSB | P08236 | 647 |
| MGAT2 | GCNT2 | Q8N0V5 | 646 |
| MGAT2 | ALG3 | Q92685 | 625 |
| MGAT2 | EXTL3 | O43909 | 564 |
| MGAT2 | ST3GAL3 | Q11203 | 558 |
| MGAT2 | MGAT5B | Q3V5L5 | 549 |
IntAct
39 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| TOR1AIP2 | TMEM223 | psi-mi:“MI:0914”(association) | 0.530 |
| PEX19 | FAM20B | psi-mi:“MI:0914”(association) | 0.530 |
| PEX19 | MYO1D | psi-mi:“MI:0914”(association) | 0.530 |
| HSCB | RBP5 | psi-mi:“MI:0914”(association) | 0.350 |
| ATAD3A | TMEM223 | psi-mi:“MI:0914”(association) | 0.350 |
| P | psi-mi:“MI:0914”(association) | 0.350 | |
| M | psi-mi:“MI:0914”(association) | 0.350 | |
| PLOD2 | psi-mi:“MI:0914”(association) | 0.350 | |
| SHANK3 | IGKV3D-15 | psi-mi:“MI:0914”(association) | 0.350 |
| PDGFRA | GXYLT2 | psi-mi:“MI:0914”(association) | 0.350 |
| TCTN2 | TMEM131L | psi-mi:“MI:0914”(association) | 0.350 |
| ST14 | LIPT2 | psi-mi:“MI:0914”(association) | 0.350 |
| SCGB2A2 | RTL8C | psi-mi:“MI:0914”(association) | 0.350 |
| BCAP31 | GOLIM4 | psi-mi:“MI:0914”(association) | 0.350 |
| CPQ | COX7A2L | psi-mi:“MI:0914”(association) | 0.350 |
| TMPRSS13 | TOR1A | psi-mi:“MI:0914”(association) | 0.350 |
| MAN1A1 | GPC4 | psi-mi:“MI:0914”(association) | 0.350 |
| MINPP1 | MGAT2 | psi-mi:“MI:0914”(association) | 0.350 |
| REEP5 | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
| TSPAN8 | POTEF | psi-mi:“MI:0914”(association) | 0.350 |
| MAN1A1 | PLOD2 | psi-mi:“MI:0914”(association) | 0.350 |
| PEX19 | KCNN4 | psi-mi:“MI:0914”(association) | 0.350 |
| TOR1AIP2 | XPO1 | psi-mi:“MI:0914”(association) | 0.350 |
| SAAL1 | TMEM223 | psi-mi:“MI:0914”(association) | 0.350 |
| SLC30A1 | PSMD11 | psi-mi:“MI:0914”(association) | 0.350 |
| SLC30A10 | GOLIM4 | psi-mi:“MI:0914”(association) | 0.350 |
| SLC30A7 | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (58): MGAT2 (Affinity Capture-MS), MGAT2 (Affinity Capture-MS), MGAT2 (Affinity Capture-MS), MGAT2 (Affinity Capture-MS), MGAT2 (Affinity Capture-MS), MGAT2 (Affinity Capture-MS), S (Reconstituted Complex), MGAT2 (Proximity Label-MS), MGAT2 (Affinity Capture-MS), MGAT2 (Negative Genetic), MGAT2 (Affinity Capture-MS), MGAT2 (Affinity Capture-MS), MGAT2 (Affinity Capture-MS), MGAT2 (Affinity Capture-MS), MGAT2 (Affinity Capture-MS)
ESM2 similar proteins: A0A4Z3, A1Y9I9, A4FUH1, B6CZ46, B6CZ56, B6CZ62, D3ZNQ3, G3V9Q9, O43505, O60512, O60909, O94766, P14616, P14617, P58158, Q09326, Q10469, Q2NKH9, Q2YDM8, Q3V1N9, Q3V5L5, Q4R5T7, Q5EA01, Q5EB73, Q5JU69, Q5M936, Q5NVN3, Q5R4S2, Q5R868, Q5YB40, Q5ZLK4, Q64716, Q6AYR4, Q765H6, Q7Z4J2, Q8BGT9, Q8BWP8, Q8IXK2, Q8NCL4, Q8R1J9
Diamond homologs: O19071, Q09326, Q10469, Q921V5, Q9FT88
SIGNOR signaling
0 interactions.
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 52 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| Metal ion SLC transporters | 6 | 109.3× | 2e-09 |
| R-HSA-425366 | 5 | 27.5× | 5e-05 |
| SLC-mediated transmembrane transport | 5 | 9.0× | 8e-03 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| zinc ion transmembrane transport | 8 | 122.1× | 3e-13 |
| intracellular zinc ion homeostasis | 7 | 73.3× | 7e-10 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
166 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 6 |
| Likely pathogenic | 6 |
| Uncertain significance | 120 |
| Likely benign | 19 |
| Benign | 6 |
Top pathogenic / likely-pathogenic (12)
| Variant ID | HGVS | Classification |
|---|---|---|
| 617657 | NM_002408.4(MGAT2):c.753dup (p.Ala252fs) | Pathogenic |
| 617658 | NM_002408.4(MGAT2):c.91C>T (p.Gln31Ter) | Pathogenic |
| 617661 | NM_002408.4(MGAT2):c.799G>C (p.Asp267His) | Pathogenic |
| 6990 | NM_002408.4(MGAT2):c.785A>G (p.His262Arg) | Pathogenic |
| 6991 | NM_002408.4(MGAT2):c.952A>G (p.Asn318Asp) | Pathogenic |
| 6992 | NM_002408.4(MGAT2):c.1017T>A (p.Cys339Ter) | Pathogenic |
| 30270 | NM_002408.4(MGAT2):c.711G>C (p.Lys237Asn) | Likely pathogenic |
| 3061920 | NM_002408.4(MGAT2):c.1085G>A (p.Trp362Ter) | Likely pathogenic |
| 3065025 | NM_002408.4(MGAT2):c.1199_1202del (p.Asn400fs) | Likely pathogenic |
| 489288 | NM_002408.4(MGAT2):c.745C>T (p.Arg249Ter) | Likely pathogenic |
| 596219 | NM_002408.4(MGAT2):c.1006_1009del (p.Asp336fs) | Likely pathogenic |
| 817419 | NM_002408.4(MGAT2):c.346dup (p.Arg116fs) | Likely pathogenic |
SpliceAI
0 predictions. Top by Δscore:
AlphaMissense
2939 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 14:49621722:A:C | S152R | 1.000 |
| 14:49621724:C:A | S152R | 1.000 |
| 14:49621724:C:G | S152R | 1.000 |
| 14:49621830:T:C | F188L | 1.000 |
| 14:49621831:T:G | F188C | 1.000 |
| 14:49621832:T:A | F188L | 1.000 |
| 14:49621832:T:G | F188L | 1.000 |
| 14:49621896:T:A | C210S | 1.000 |
| 14:49621897:G:C | C210S | 1.000 |
| 14:49621936:G:C | R223T | 1.000 |
| 14:49621936:G:T | R223I | 1.000 |
| 14:49621937:A:C | R223S | 1.000 |
| 14:49621937:A:T | R223S | 1.000 |
| 14:49621961:A:C | K231N | 1.000 |
| 14:49621961:A:T | K231N | 1.000 |
| 14:49622303:C:A | N345K | 1.000 |
| 14:49622303:C:G | N345K | 1.000 |
| 14:49622306:G:C | W346C | 1.000 |
| 14:49622306:G:T | W346C | 1.000 |
| 14:49622308:A:C | D347A | 1.000 |
| 14:49622308:A:T | D347V | 1.000 |
| 14:49622554:G:A | G429E | 1.000 |
| 14:49622559:T:A | W431R | 1.000 |
| 14:49622559:T:C | W431R | 1.000 |
| 14:49622561:G:C | W431C | 1.000 |
| 14:49622561:G:T | W431C | 1.000 |
| 14:49622572:G:C | R435T | 1.000 |
| 14:49622572:G:T | R435M | 1.000 |
| 14:49621565:C:A | N99K | 0.999 |
| 14:49621565:C:G | N99K | 0.999 |
dbSNP variants (sampled 300 via entrez): RS1000194527 (14:49619782 T>C), RS1000458463 (14:49621556 C>T), RS1000796282 (14:49620645 G>A), RS1000864356 (14:49619362 G>A), RS1000981677 (14:49619604 T>G), RS1001322400 (14:49619685 C>G), RS1002967671 (14:49620548 C>A), RS1003201135 (14:49619697 T>C), RS1003340772 (14:49620385 G>A,C), RS1003647744 (14:49620606 T>C), RS1003705196 (14:49619467 G>C), RS1003833972 (14:49619163 A>G), RS1003910403 (14:49619438 C>A,T), RS1005048070 (14:49618961 A>G,T), RS1005716041 (14:49620833 G>A)
Disease associations
OMIM: gene MIM:602616 | disease phenotypes: MIM:212066
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| MGAT2-congenital disorder of glycosylation | Definitive | Autosomal recessive |
ClinGen Gene-Disease Validity (1)
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
| Disease | Classification | Inheritance |
|---|---|---|
| MGAT2-congenital disorder of glycosylation | Moderate | AR |
Mondo (1): MGAT2-congenital disorder of glycosylation (MONDO:0008908)
Orphanet (1): MGAT2-CDG (Orphanet:79329)
HPO phenotypes
99 total (30 of 99 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000007 | Autosomal recessive inheritance |
| HP:0000154 | Wide mouth |
| HP:0000194 | Open mouth |
| HP:0000212 | Gingival overgrowth |
| HP:0000232 | Everted lower lip vermilion |
| HP:0000233 | Thin vermilion border |
| HP:0000248 | Brachycephaly |
| HP:0000252 | Microcephaly |
| HP:0000253 | Progressive microcephaly |
| HP:0000256 | Macrocephaly |
| HP:0000268 | Dolichocephaly |
| HP:0000278 | Retrognathia |
| HP:0000303 | Mandibular prognathia |
| HP:0000316 | Hypertelorism |
| HP:0000343 | Long philtrum |
| HP:0000358 | Posteriorly rotated ears |
| HP:0000363 | Abnormal earlobe morphology |
| HP:0000369 | Low-set ears |
| HP:0000395 | Prominent antihelix |
| HP:0000400 | Macrotia |
| HP:0000407 | Sensorineural hearing impairment |
| HP:0000426 | Prominent nasal bridge |
| HP:0000444 | Convex nasal ridge |
| HP:0000470 | Short neck |
| HP:0000494 | Downslanted palpebral fissures |
| HP:0000527 | Long eyelashes |
| HP:0000574 | Thick eyebrow |
| HP:0000678 | Dental crowding |
| HP:0000699 | Diastema |
| HP:0000718 | Aggressive behavior |
GWAS associations
0 associations (top):
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| C535752 | Congenital disorder of glycosylation type 2A (supp.) |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL2321630 (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: 35 (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 |
|---|---|---|---|
| CHEMBL3912712 | BMS-963272 | 1 | 25 |
| CHEMBL5418882 | BMS-986172 | 1 | 10 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
593 measured of 596 human assays (596 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| (2S)-2-[2-chloro-4-(4,4,4-trifluorobutoxy)phenyl]-4-(5-cyclopropylthiophen-2-yl)-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 0.2 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| (2S)-4-(5-ethyl-1,3-thiazol-2-yl)-2-[2-fluoro-4-(6,6,6-trifluorohexoxy)phenyl]-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 0.5 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| N-[[(2S)-4-[5-(difluoromethoxy)-2-pyridinyl]-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]methyl]-2-methylsulfonylacetamide | IC50 | 0.62 nM | US-10335401: Non-aromatic heterocyclic derivative having MGAT2 inhibitory activity |
| (2S)-2-[2-chloro-4-(6,6,6-trifluorohexoxy)phenyl]-4-(5-cyclopropyl-1,3-thiazol-2-yl)-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 0.7 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| N-[[(2S)-4-[5-(2-hydroxypropan-2-yl)-2-pyridinyl]-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]methyl]-2-methylsulfonylacetamide | IC50 | 0.73 nM | US-10335401: Non-aromatic heterocyclic derivative having MGAT2 inhibitory activity |
| 4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-N-[4-(trifluoromethoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | IC50 | 1 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-N-[4-(trifluoromethyl)phenyl]-1,3-dihydropyridine-5-carboxamide | IC50 | 1 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| N-(4-hydroxyphenyl)-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | IC50 | 1 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 4-(4-methylphenyl)-N-(1,2-oxazol-5-yl)-6-oxo-2-(trifluoromethyl)-2-[4-(3,3,3-trifluoropropoxy)phenyl]-1,3-dihydropyridine-5-carboxamide | IC50 | 1 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 4-[4-(difluoromethoxy)phenyl]-2-[2-fluoro-4-(6,6,6-trifluorohexoxy)phenyl]-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 1 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 2-[3-fluoro-4-(6,6,6-trifluorohexoxy)phenyl]-4-naphthalen-2-yl-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 1 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| (2S)-4-[4-(difluoromethyl)phenyl]-2-[2-fluoro-4-(6,6,6-trifluorohexoxy)phenyl]-N-methylsulfonyl-6-oxo-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | IC50 | 1 nM | US-9822074: Dihydropyridinone MGAT2 inhibitors |
| (2S)-4-(4-cyclopropylphenyl)-2-[2-fluoro-4-(6,6,6-trifluorohexoxy)phenyl]-N-methylsulfonyl-6-oxo-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | IC50 | 1 nM | US-9822074: Dihydropyridinone MGAT2 inhibitors |
| 2-methylsulfonyl-N-[[(2S)-6-oxo-4-(5-prop-1-en-2-yl-2-pyridinyl)-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]methyl]acetamide | IC50 | 1 nM | US-10335401: Non-aromatic heterocyclic derivative having MGAT2 inhibitory activity |
| (S,E)-2-Methyl-N-(2,2,2-trifluoro-1-(4-((5,5,5-trifluoropentyl)oxy phenyl)ethylidene)propane-2-sulfinamide | IC50 | 1.1 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| (2S)-2-[2-chloro-4-(4,4,4-trifluorobutoxy)phenyl]-4-(5-cyclopropyl-1,3-thiazol-2-yl)-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 1.1 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| N-[[(2S)-4-[5-(difluoromethyl)-2-pyridinyl]-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]methyl]-2-methylsulfonylacetamide | IC50 | 1.1 nM | US-10335401: Non-aromatic heterocyclic derivative having MGAT2 inhibitory activity |
| 1-(5-Cyclopropylthiazol-2-yl)ethanone | IC50 | 1.2 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| (2S)-4-(5-cyclopropylthiophen-2-yl)-2-[2-methoxy-4-(4,4,4-trifluorobutoxy)phenyl]-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 1.4 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| (2S)-4-(5-cyclopropyl-1,3-thiazol-2-yl)-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 1.4 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| 1-(5-Methylthiazol-2-yl)ethanone | IC50 | 1.5 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| (S)—N-(4-(5-Ethylthiophen-2-yl)-2-oxo-6-(4-((6,6,6-trifluorohexyl)oxy)phenyl)-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridin-3-yl)-2-(methylsulfonyl)acetamide | IC50 | 1.5 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| 2-[(1R)-1-(3,5-difluorophenyl)ethyl]-N-[3-(pyrrolidine-1-carbonyl)-1,2,4-oxadiazol-5-yl]-3,4-dihydro-1H-isoquinoline-7-sulfonamide | IC50 | 1.6 nM | US-10065945: Isoquinoline derivatives as MGAT2 inhibitors |
| N-[[(2S)-4-[5-(difluoromethyl)-2-pyridinyl]-6-oxo-2-(trifluoromethyl)-2-[4-(3,3,3-trifluoropropyl)phenyl]-1,3-dihydropyridin-5-yl]methyl]-2-methylsulfonylacetamide | IC50 | 1.9 nM | US-10335401: Non-aromatic heterocyclic derivative having MGAT2 inhibitory activity |
| 4-(2-fluoro-4-methoxyphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carbonitrile | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| N-[4-[4-(difluoromethoxy)phenyl]-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]-1,2-oxazole-5-carboxamide | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 3-bromo-N-[4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]-1,2-oxazole-5-carboxamide | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 4-(5,6,7,8-tetrahydronaphthalen-2-yl)-5-(tetrazolidin-5-yl)-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| N-[4-[4-(difluoromethoxy)phenyl]-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]pyridine-4-carboxamide | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 2-[2-fluoro-4-(6,6,6-trifluorohexoxy)phenyl]-4-naphthalen-2-yl-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 4-[4-(cyclopropylmethyl)phenyl]-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 2-[2-fluoro-4-(5,5,5-trifluoropentoxy)phenyl]-4-(4-methylphenyl)-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| N-[4-(4-methylphenyl)-6-oxo-2-(4-phenylmethoxyphenyl)-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]-2-methylsulfonylacetamide | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 4-[4-(difluoromethoxy)phenyl]-6-oxo-N-pyridin-3-yl-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 4-(2-fluoro-4-methylphenyl)-N-(4-methoxyphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| 2-(methanesulfonamido)-N-[4-(4-methylphenyl)-2-oct-1-ynyl-6-oxo-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]acetamide | IC50 | 2 nM | US-9187424: Aryl dihydropyridinones and piperidinone MGAT2 inhibitors |
| (2R)-N-cyclopropylsulfonyl-2-(5-heptyl-1,3-thiazol-2-yl)-4-(4-methylphenyl)-6-oxo-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | IC50 | 2 nM | US-9822074: Dihydropyridinone MGAT2 inhibitors |
| (2S)-N-cyclopropylsulfonyl-4-(5-cyclopropyl-1,3-thiazol-2-yl)-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-6-oxo-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | IC50 | 2 nM | US-9822074: Dihydropyridinone MGAT2 inhibitors |
| (2S)-4-[1-(cyclopropylmethyl)pyrazol-3-yl]-N-cyclopropylsulfonyl-6-oxo-2-(trifluoromethyl)-2-[4-(5,5,5-trifluoropentyl)phenyl]-1,3-dihydropyridine-5-carboxamide | IC50 | 2 nM | US-9822074: Dihydropyridinone MGAT2 inhibitors |
| (2S)-N-cyclopropylsulfonyl-4-(4-ethylphenyl)-2-methyl-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-1,3-dihydropyridine-5-carboxamide | IC50 | 2 nM | US-9822074: Dihydropyridinone MGAT2 inhibitors |
| (2S)-4-(5-cyclopropyl-1H-imidazol-2-yl)-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-5-(5-oxotetrazolidin-1-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 2 nM | US-10093650: Tetrazolone-substituted dihydropyridinone MGAT2 inhibitors |
| 1-(5-Ethylthiazol-2-yl)ethanone | IC50 | 2.1 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| (2S)-4-(5-ethyl-1,3-thiazol-2-yl)-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 2.1 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| 1-(5-Cyclopropylthiophen-2-yl)ethanone | IC50 | 2.2 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| (2S)-4-(5-ethylthiophen-2-yl)-5-(2H-tetrazol-5-yl)-2-[4-(6,6,6-trifluorohexoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 2.2 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| N-[[(2S)-4-(5-methyl-2-pyridinyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]methyl]-1,2-oxazole-5-carboxamide | IC50 | 2.2 nM | US-10335401: Non-aromatic heterocyclic derivative having MGAT2 inhibitory activity |
| 3,3,3-trifluoro-N-[[(2S)-4-(5-methyl-2-pyridinyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]methyl]propanamide | IC50 | 2.3 nM | US-10335401: Non-aromatic heterocyclic derivative having MGAT2 inhibitory activity |
| (S,E)-2-Methyl-N-(2,2,2-trifluoro-1-(4-(4,4,4-trifluorobutoxy) phenyl)ethylidene)propane-2-sulfinamide | IC50 | 2.5 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
| N-[[(2S)-4-(5-methoxy-2-pyridinyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]methyl]-2-methylsulfonylacetamide | IC50 | 2.5 nM | US-10335401: Non-aromatic heterocyclic derivative having MGAT2 inhibitory activity |
| (2S)-4-[1-(cyclopropylmethyl)pyrazol-3-yl]-5-(2H-tetrazol-5-yl)-2-[4-(6,6,6-trifluorohexoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | IC50 | 2.7 nM | US-9701672: Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders |
ChEMBL bioactivities
1574 potent at pChembl≥5 of 1584 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.70 | IC50 | 0.2 | nM | CHEMBL4457459 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL5824866 |
| 9.65 | IC50 | 0.224 | nM | CHEMBL5748063 |
| 9.54 | IC50 | 0.285 | nM | CHEMBL5768466 |
| 9.52 | IC50 | 0.3 | nM | CHEMBL4564881 |
| 9.42 | IC50 | 0.38 | nM | CHEMBL4572662 |
| 9.39 | IC50 | 0.409 | nM | CHEMBL6035455 |
| 9.36 | IC50 | 0.439 | nM | CHEMBL5816249 |
| 9.30 | IC50 | 0.5 | nM | CHEMBL5813899 |
| 9.21 | IC50 | 0.62 | nM | CHEMBL5991713 |
| 9.20 | IC50 | 0.63 | nM | CHEMBL3893594 |
| 9.19 | IC50 | 0.64 | nM | CHEMBL4463750 |
| 9.15 | IC50 | 0.7 | nM | CHEMBL5820966 |
| 9.15 | IC50 | 0.706 | nM | CHEMBL5871193 |
| 9.14 | IC50 | 0.73 | nM | CHEMBL4560153 |
| 9.12 | IC50 | 0.76 | nM | CHEMBL4457459 |
| 9.05 | IC50 | 0.9 | nM | CHEMBL4457459 |
| 9.00 | IC50 | 1 | nM | CHEMBL3581716 |
| 9.00 | IC50 | 1 | nM | CHEMBL3961967 |
| 9.00 | IC50 | 1 | nM | CHEMBL3965215 |
| 9.00 | IC50 | 1 | nM | CHEMBL3981198 |
| 9.00 | IC50 | 1 | nM | CHEMBL3937187 |
| 9.00 | IC50 | 1 | nM | CHEMBL3943858 |
| 9.00 | IC50 | 1 | nM | CHEMBL3932509 |
| 9.00 | IC50 | 1 | nM | CHEMBL3986069 |
| 9.00 | IC50 | 1 | nM | CHEMBL3960802 |
| 9.00 | IC50 | 1 | nM | CHEMBL6048166 |
| 9.00 | IC50 | 1 | nM | CHEMBL5960634 |
| 9.00 | IC50 | 1 | nM | CHEMBL5986274 |
| 9.00 | IC50 | 1 | nM | CHEMBL5779894 |
| 9.00 | IC50 | 1 | nM | CHEMBL5965136 |
| 9.00 | IC50 | 1 | nM | CHEMBL6046535 |
| 8.98 | IC50 | 1.05 | nM | CHEMBL5883234 |
| 8.98 | IC50 | 1.04 | nM | CHEMBL6036045 |
| 8.97 | IC50 | 1.06 | nM | CHEMBL5840224 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL4465236 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL4457459 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL5934884 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL5803244 |
| 8.95 | IC50 | 1.12 | nM | CHEMBL5998821 |
| 8.94 | IC50 | 1.14 | nM | CHEMBL5757628 |
| 8.94 | IC50 | 1.15 | nM | CHEMBL5890961 |
| 8.93 | IC50 | 1.17 | nM | CHEMBL6004478 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL3581717 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL5817097 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL6016017 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL5753020 |
| 8.92 | IC50 | 1.21 | nM | CHEMBL5755241 |
| 8.91 | IC50 | 1.24 | nM | CHEMBL5985571 |
| 8.90 | IC50 | 1.25 | nM | CHEMBL5838599 |
PubChem BioAssay actives
153 with measured affinity, of 183 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 |
|---|---|---|---|---|
| (2S)-4-(5-cyclopropylthiophen-2-yl)-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 1573551: Inhibition of recombinant human MGAT2 | ic50 | 0.0002 | uM |
| 4-(5-ethylthiophen-2-yl)-3-(2H-tetrazol-5-yl)-6-[4-(6,6,6-trifluorohexoxy)-2-(trifluoromethyl)phenyl]-1H-pyridin-2-one | 1573551: Inhibition of recombinant human MGAT2 | ic50 | 0.0003 | uM |
| 2-cyclobutylsulfanyl-6-[3-(2,3-dihydro-1H-inden-2-ylamino)propanoyl]-3-phenyl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-one | 1573540: Inhibition of recombinant human MGAT2 using 2-monooleoyl glycerol/[1-14C]-oleoyl CoA as substrate after 30 mins by liquid scintillation counting method | ic50 | 0.0004 | uM |
| (2S)-N-(4-methoxyphenyl)-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | 1785300: Inhibition of human MGAT2 in mouse STC-1 cell based assay | ic50 | 0.0006 | uM |
| 2-cyclobutylsulfanyl-3-phenyl-6-[2-[5-[4-(trifluoromethyl)phenoxy]pentylamino]acetyl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-one | 1573551: Inhibition of recombinant human MGAT2 | ic50 | 0.0006 | uM |
| N-[[(2S)-4-[5-(2-hydroxypropan-2-yl)-2-pyridinyl]-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]methyl]-2-methylsulfonylacetamide | 1573551: Inhibition of recombinant human MGAT2 | ic50 | 0.0007 | uM |
| N-[5-[(2,4-difluorophenyl)sulfamoyl]-1-(2-phenylethyl)-2,3-dihydroindol-7-yl]acetamide | 1228343: In vitro inhibition of full length human MGAT2 transfected in FreeStyle293 cells assessed as dioleoylglycerol by RapidFire/MS assay | ic50 | 0.0010 | uM |
| 3-[(3S)-4’-(2-cyclopropyl-1,3-thiazol-5-yl)-6’-oxo-6-(4,4,4-trifluorobutoxy)spiro[1,2-dihydroindene-3,2’-1,3-dihydropyridine]-5’-yl]-4H-1,2,4-oxadiazol-5-one | 1573551: Inhibition of recombinant human MGAT2 | ic50 | 0.0010 | uM |
| (2S)-4-[4-(difluoromethyl)phenyl]-2-[2-fluoro-4-(6,6,6-trifluorohexoxy)phenyl]-N-methylsulfonyl-6-oxo-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | 1573551: Inhibition of recombinant human MGAT2 | ic50 | 0.0010 | uM |
| 2-cyclobutylsulfanyl-6-[3-(2,3-dihydro-1,4-benzodioxin-3-ylmethylamino)propanoyl]-3-phenyl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-one | 1573551: Inhibition of recombinant human MGAT2 | ic50 | 0.0011 | uM |
| N-[5-[(2,4-difluorophenyl)sulfamoyl]-1-[2-(4-fluorophenyl)ethyl]-2,3-dihydroindol-7-yl]acetamide | 1228343: In vitro inhibition of full length human MGAT2 transfected in FreeStyle293 cells assessed as dioleoylglycerol by RapidFire/MS assay | ic50 | 0.0012 | uM |
| 2-[(1R)-1-(3,5-difluorophenyl)ethyl]-N-[3-(pyrrolidine-1-carbonyl)-1,2,4-oxadiazol-5-yl]-3,4-dihydro-1H-isoquinoline-7-sulfonamide | 1573551: Inhibition of recombinant human MGAT2 | ic50 | 0.0016 | uM |
| N-(2,4-difluorophenyl)-3,3-diethyl-5-oxo-2,4-dihydro-1H-1,4-benzodiazepine-7-sulfonamide | 745096: Inhibition of human recombinant MGAT2 expressed in insect cell membrane using 2-oleoyl-sn-glycerol and oleoyl coenzyme A as substrate after 40 mins by Ellmans assay based rapidfire LCMS analysis | ic50 | 0.0016 | uM |
| (2S)-4-[1-(cyclopropylmethyl)pyrazol-3-yl]-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 2015133: Inhibition of human MGAT2 using 2-oleoylglycerol and oleoyl-coenzyme A as substrate by LC-MS analysis | ic50 | 0.0019 | uM |
| (2S)-4-(5-cyclopropyl-1,3-thiazol-2-yl)-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-5-(5-oxo-1H-tetrazol-4-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 2015133: Inhibition of human MGAT2 using 2-oleoylglycerol and oleoyl-coenzyme A as substrate by LC-MS analysis | ic50 | 0.0019 | uM |
| (2S)-N-cyclopentyl-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0019 | uM |
| N-[5-[(2,4-difluorophenyl)sulfamoyl]-1-(2-phenylethyl)indol-7-yl]acetamide | 1228343: In vitro inhibition of full length human MGAT2 transfected in FreeStyle293 cells assessed as dioleoylglycerol by RapidFire/MS assay | ic50 | 0.0021 | uM |
| N-[5-[(4-methoxyphenyl)sulfamoyl]-1-(2-phenylethyl)-2,3-dihydroindol-7-yl]acetamide | 1228343: In vitro inhibition of full length human MGAT2 transfected in FreeStyle293 cells assessed as dioleoylglycerol by RapidFire/MS assay | ic50 | 0.0022 | uM |
| benzyl 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxo-1,3-diazinan-1-yl)-2,3-dihydroindole-1-carboxylate | 1228343: In vitro inhibition of full length human MGAT2 transfected in FreeStyle293 cells assessed as dioleoylglycerol by RapidFire/MS assay | ic50 | 0.0022 | uM |
| (2S)-4-(5-cyclopropyl-1,3-thiazol-2-yl)-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 2015133: Inhibition of human MGAT2 using 2-oleoylglycerol and oleoyl-coenzyme A as substrate by LC-MS analysis | ic50 | 0.0024 | uM |
| 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxoimidazolidin-1-yl)-N-[4-(trifluoromethyl)phenyl]-2,3-dihydroindole-1-carboxamide | 1228343: In vitro inhibition of full length human MGAT2 transfected in FreeStyle293 cells assessed as dioleoylglycerol by RapidFire/MS assay | ic50 | 0.0025 | uM |
| 4-(4-methoxyphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carbonitrile | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0025 | uM |
| (2S)-4-(5-ethylthiophen-2-yl)-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-5-(5-oxo-1H-tetrazol-4-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 2015133: Inhibition of human MGAT2 using 2-oleoylglycerol and oleoyl-coenzyme A as substrate by LC-MS analysis | ic50 | 0.0025 | uM |
| (2S)-4-(4-methylphenyl)-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-2-[4-(5,5,5-trifluoropentyl)phenyl]-1,3-dihydropyridin-6-one | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0026 | uM |
| (2S)-2-[2-fluoro-4-(6,6,6-trifluorohexoxy)phenyl]-4-(4-methylphenyl)-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0026 | uM |
| 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-N-[4-(trifluoromethyl)phenyl]-2,3-dihydroindole-1-carboxamide | 1228343: In vitro inhibition of full length human MGAT2 transfected in FreeStyle293 cells assessed as dioleoylglycerol by RapidFire/MS assay | ic50 | 0.0031 | uM |
| N-(2,4-difluorophenyl)-3,3-diethyl-2,5-dioxo-1,4-dihydro-1,4-benzodiazepine-7-sulfonamide | 745096: Inhibition of human recombinant MGAT2 expressed in insect cell membrane using 2-oleoyl-sn-glycerol and oleoyl coenzyme A as substrate after 40 mins by Ellmans assay based rapidfire LCMS analysis | ic50 | 0.0032 | uM |
| benzyl 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxoimidazolidin-1-yl)-2,3-dihydroindole-1-carboxylate | 1228343: In vitro inhibition of full length human MGAT2 transfected in FreeStyle293 cells assessed as dioleoylglycerol by RapidFire/MS assay | ic50 | 0.0034 | uM |
| N-(4-tert-butylphenyl)-5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydroindole-1-carboxamide | 1228343: In vitro inhibition of full length human MGAT2 transfected in FreeStyle293 cells assessed as dioleoylglycerol by RapidFire/MS assay | ic50 | 0.0036 | uM |
| N-[5-[(2,4-difluorophenyl)sulfamoyl]-1-(3-phenylpropyl)-2,3-dihydroindol-7-yl]acetamide | 1228343: In vitro inhibition of full length human MGAT2 transfected in FreeStyle293 cells assessed as dioleoylglycerol by RapidFire/MS assay | ic50 | 0.0037 | uM |
| N-[(1S)-1-[4-[[[(3S)-2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-3-yl]methylamino]methyl]phenyl]-2,2,2-trifluoroethyl]methanesulfonamide | 1573548: Inhibition of recombinant human MGAT2 expressed in sf9 cells using 2-monooleoyl glycerol/[14C]-oleoyl CoA as substrate by microscintillation counting method | ic50 | 0.0038 | uM |
| 4-(4-methylphenyl)-6-oxo-N-phenyl-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0040 | uM |
| ethyl 3-[4-[[3-(2-cyclohexylsulfanyl-4-oxo-3-phenyl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine-6-carbonyl)azetidin-1-yl]methyl]phenyl]propanoate | 1573551: Inhibition of recombinant human MGAT2 | ic50 | 0.0040 | uM |
| 3-ethyl-N-(4-methoxyphenyl)-3-methyl-2,5-dioxo-1,4-dihydro-1,4-benzodiazepine-7-sulfonamide | 745096: Inhibition of human recombinant MGAT2 expressed in insect cell membrane using 2-oleoyl-sn-glycerol and oleoyl coenzyme A as substrate after 40 mins by Ellmans assay based rapidfire LCMS analysis | ic50 | 0.0040 | uM |
| (2S)-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-N-[4-(trifluoromethoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0042 | uM |
| (2S)-4-(4-methylphenyl)-5-(tetrazol-1-yl)-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 2015133: Inhibition of human MGAT2 using 2-oleoylglycerol and oleoyl-coenzyme A as substrate by LC-MS analysis | ic50 | 0.0045 | uM |
| (2S)-4-[1-(cyclopropylmethyl)pyrazol-3-yl]-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-5-(5-oxo-1H-tetrazol-4-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 2015133: Inhibition of human MGAT2 using 2-oleoylglycerol and oleoyl-coenzyme A as substrate by LC-MS analysis | ic50 | 0.0046 | uM |
| (2S)-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-4-(4-methylphenyl)-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0050 | uM |
| (2S)-N-(6-methoxy-3-pyridinyl)-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0050 | uM |
| (2S)-N-methyl-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0052 | uM |
| 4-(4-ethoxyphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carbonitrile | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0053 | uM |
| (2S)-2-(4-butylsulfanylphenyl)-4-(4-methylphenyl)-5-(2H-tetrazol-5-yl)-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0055 | uM |
| (2S)-4-(4-methylphenyl)-5-(2H-tetrazol-5-yl)-2-[4-(6,6,6-trifluorohexoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0061 | uM |
| (3S)-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-1,4-dihydro-1,4-benzodiazepine-7-sulfonamide | 1573551: Inhibition of recombinant human MGAT2 | ic50 | 0.0063 | uM |
| N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-1-(2-phenylethyl)-2,3-dihydroindole-5-sulfonamide | 1228343: In vitro inhibition of full length human MGAT2 transfected in FreeStyle293 cells assessed as dioleoylglycerol by RapidFire/MS assay | ic50 | 0.0067 | uM |
| N-(4-methoxyphenyl)-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0067 | uM |
| (2S)-2-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-4-(4-methylphenyl)-6-oxo-N-[4-(2H-tetrazol-5-yl)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | 1573551: Inhibition of recombinant human MGAT2 | ic50 | 0.0070 | uM |
| (2S)-N-(6-methoxypyridazin-3-yl)-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0071 | uM |
| (2S)-4-(4-methylphenyl)-5-(2H-tetrazol-5-yl)-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 1785280: Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay | ic50 | 0.0071 | uM |
| 4-(4-methylphenyl)-5-(2H-tetrazol-5-yl)-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one | 2015133: Inhibition of human MGAT2 using 2-oleoylglycerol and oleoyl-coenzyme A as substrate by LC-MS analysis | ic50 | 0.0071 | uM |
CTD chemical–gene interactions
42 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Cadmium | increases expression, decreases expression, increases abundance | 2 |
| Nickel | increases expression | 2 |
| Valproic Acid | decreases methylation, increases expression | 2 |
| Cyclosporine | decreases expression, increases expression | 2 |
| Cadmium Chloride | decreases expression, increases abundance, increases expression | 2 |
| aristolochic acid I | increases expression | 1 |
| GSK-J4 | decreases expression | 1 |
| 7-(4,6-di-tert-butylpyrimidin-2-yl)-3-(4-trifluoromethoxyphenyl)-5,6,7,8-tetrahydro(1,2,4)triazolo(4,3-a)pyrazine | decreases activity | 1 |
| bisphenol F | affects cotreatment, increases expression | 1 |
| alpha phellandrene | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| bisphenol A | decreases expression | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | decreases expression | 1 |
| isobutyl alcohol | affects cotreatment, decreases expression, increases abundance | 1 |
| 2,3-dimethoxy-1,4-naphthoquinone | decreases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| Lycopene | increases expression | 1 |
| Ethanol | affects cotreatment, decreases expression, increases abundance | 1 |
| Antimony | decreases expression | 1 |
| Antimony Potassium Tartrate | decreases expression | 1 |
| Atrazine | increases expression | 1 |
| Chromium | decreases expression | 1 |
| Cisplatin | decreases expression, decreases reaction | 1 |
| Dexamethasone | affects cotreatment, increases expression | 1 |
| Dimethylnitrosamine | decreases expression | 1 |
| Fluorouracil | affects response to substance | 1 |
| Gasoline | affects cotreatment, decreases expression, increases abundance | 1 |
| Indomethacin | affects cotreatment, increases expression | 1 |
| Mercury | decreases expression | 1 |
| Methyl Methanesulfonate | decreases expression | 1 |
ChEMBL screening assays
32 unique, capped per target: 32 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL2329320 | Binding | Inhibition of human GNT2 GalNAc-transferase using GnMan3-octyl as substrate at 0.5 mM after 1 hr in presence of phosphatidylcholine | Selective inhibition of glycosyltransferases by bivalent imidazolium salts. — Bioorg Med Chem |
Cellosaurus cell lines
8 cell lines: 6 spontaneously immortalized cell line, 2 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_C3MD | SfSWT-4 | Spontaneously immortalized cell line | Female |
| CVCL_C3ME | SfSWT-5 | Spontaneously immortalized cell line | Female |
| CVCL_C3MF | SfSWT-6 | Spontaneously immortalized cell line | Female |
| CVCL_C3MG | SfSWT-7 | Spontaneously immortalized cell line | Female |
| CVCL_SY25 | HAP1 MGAT2 (-) 1 | Cancer cell line | Male |
| CVCL_SY26 | HAP1 MGAT2 (-) 2 | Cancer cell line | Male |
| CVCL_Z366 | SfSWT-1 | Spontaneously immortalized cell line | Female |
| CVCL_Z367 | SfSWT-3 | Spontaneously immortalized cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Associated diseases: MGAT2-congenital disorder of glycosylation
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): MGAT2-congenital disorder of glycosylation