SLC2A4
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Summary
SLC2A4 (solute carrier family 2 member 4, HGNC:11009) is a protein-coding gene on chromosome 17p13.1, encoding Solute carrier family 2, facilitated glucose transporter member 4 (P14672). Insulin-regulated facilitative glucose transporter, which plays a key role in removal of glucose from circulation.
This gene is a member of the solute carrier family 2 (facilitated glucose transporter) family and encodes a protein that functions as an insulin-regulated facilitative glucose transporter. In the absence of insulin, this integral membrane protein is sequestered within the cells of muscle and adipose tissue. Within minutes of insulin stimulation, the protein moves to the cell surface and begins to transport glucose across the cell membrane. Mutations in this gene have been associated with noninsulin-dependent diabetes mellitus (NIDDM).
Source: NCBI Gene 6517 — RefSeq curated summary.
At a glance
- GWAS associations: 23
- Clinical variants (ClinVar): 68 total — 1 pathogenic
- Druggable target: yes
- MANE Select transcript:
NM_001042
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:11009 |
| Approved symbol | SLC2A4 |
| Name | solute carrier family 2 member 4 |
| Location | 17p13.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000181856 |
| Ensembl biotype | protein_coding |
| OMIM | 138190 |
| Entrez | 6517 |
Gene structure
Transcript identifiers
Ensembl transcripts: 8 — 6 protein_coding, 2 nonsense_mediated_decay
ENST00000317370, ENST00000424875, ENST00000570783, ENST00000571308, ENST00000572485, ENST00000859022, ENST00000859023, ENST00000954706
RefSeq mRNA: 1 — MANE Select: NM_001042
NM_001042
CCDS: CCDS11097
Canonical transcript exons
ENST00000317370 — 11 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001276523 | 7283974 | 7284089 |
| ENSE00001276531 | 7283738 | 7283862 |
| ENSE00001276536 | 7283473 | 7283645 |
| ENSE00001276548 | 7283245 | 7283361 |
| ENSE00001771157 | 7286426 | 7288257 |
| ENSE00002664276 | 7281718 | 7281967 |
| ENSE00003580687 | 7284485 | 7284672 |
| ENSE00003593177 | 7285088 | 7285189 |
| ENSE00003626827 | 7285705 | 7285908 |
| ENSE00003645804 | 7284835 | 7284939 |
| ENSE00003667029 | 7284217 | 7284379 |
Expression profiles
Bgee: expression breadth ubiquitous, 127 present calls, max score 97.95.
FANTOM5 (CAGE): breadth broad, TPM avg 3.0118 / max 296.1942, expressed in 496 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 159128 | 2.9741 | 494 |
| 159129 | 0.0377 | 19 |
Top tissues by expression
131 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| gastrocnemius | UBERON:0001388 | 97.95 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 97.95 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 97.90 | gold quality |
| apex of heart | UBERON:0002098 | 97.63 | gold quality |
| muscle of leg | UBERON:0001383 | 96.57 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 96.38 | gold quality |
| lower esophagus | UBERON:0013473 | 96.32 | gold quality |
| heart left ventricle | UBERON:0002084 | 96.08 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 95.55 | gold quality |
| right atrium auricular region | UBERON:0006631 | 94.25 | gold quality |
| muscle tissue | UBERON:0002385 | 93.66 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 93.57 | gold quality |
| heart | UBERON:0000948 | 92.67 | gold quality |
| mucosa of stomach | UBERON:0001199 | 92.42 | gold quality |
| urinary bladder | UBERON:0001255 | 86.60 | gold quality |
| fundus of stomach | UBERON:0001160 | 85.82 | gold quality |
| esophagus | UBERON:0001043 | 85.21 | gold quality |
| colon | UBERON:0001155 | 84.94 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 84.91 | gold quality |
| left uterine tube | UBERON:0001303 | 83.96 | gold quality |
| omental fat pad | UBERON:0010414 | 82.85 | gold quality |
| adipose tissue | UBERON:0001013 | 82.54 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 82.12 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 82.11 | gold quality |
| intestine | UBERON:0000160 | 80.90 | gold quality |
| transverse colon | UBERON:0001157 | 80.43 | gold quality |
| prostate gland | UBERON:0002367 | 80.23 | gold quality |
| tibial artery | UBERON:0007610 | 80.07 | gold quality |
| popliteal artery | UBERON:0002250 | 80.06 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 79.37 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-6819 | yes | 4508.92 |
| E-ANND-3 | yes | 13.47 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): ATF6, CEBPA, CEBPB, CEBPG, CNBP, DNMT1, EBF1, EPAS1, ESR1, ESR2, FOXO1, GATA6, HDAC4, HDAC5, HIF1A, KLF15, MEF2A, MEF2C, MEF2D, MLXIPL, MYC, MYOD1, NFIA, NFIC, NFKB, NR0B2, NR1H3, NR1H4, NR2F2, NR4A3, NRF1, OCLN, PAX3, PLAGL1, POU4F2, PPARA, PPARD, PPARG, PPARGC1A, PRKAA1
miRNA regulators (miRDB)
105 targeting SLC2A4, 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-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-5011-5P | 100.00 | 83.46 | 5820 |
| HSA-MIR-4510 | 100.00 | 66.60 | 2050 |
| HSA-MIR-6127 | 100.00 | 66.76 | 2188 |
| HSA-MIR-6129 | 100.00 | 66.46 | 2080 |
| HSA-MIR-6130 | 100.00 | 66.69 | 2012 |
| HSA-MIR-6133 | 100.00 | 66.48 | 2064 |
| HSA-MIR-4476 | 100.00 | 68.18 | 2030 |
| HSA-MIR-6876-5P | 100.00 | 67.68 | 2126 |
| HSA-MIR-5196-5P | 100.00 | 67.98 | 2761 |
| HSA-MIR-6758-5P | 100.00 | 66.21 | 1470 |
| HSA-MIR-190A-3P | 100.00 | 80.35 | 5520 |
| HSA-MIR-6856-5P | 100.00 | 65.47 | 1298 |
| HSA-MIR-371B-5P | 99.99 | 75.34 | 4759 |
| HSA-MIR-6077 | 99.99 | 68.04 | 2299 |
| HSA-MIR-4789-3P | 99.99 | 70.75 | 2484 |
| HSA-MIR-373-5P | 99.98 | 75.36 | 4753 |
| HSA-MIR-616-5P | 99.98 | 75.58 | 4775 |
| HSA-MIR-607 | 99.97 | 73.62 | 5593 |
| HSA-MIR-512-3P | 99.97 | 67.35 | 1049 |
| HSA-MIR-6825-5P | 99.96 | 69.81 | 3431 |
| HSA-MIR-4725-3P | 99.96 | 69.53 | 2520 |
| HSA-MIR-6780B-5P | 99.96 | 69.60 | 2562 |
| HSA-MIR-5680 | 99.91 | 69.83 | 3421 |
| HSA-MIR-106A-5P | 99.90 | 73.94 | 2683 |
| HSA-MIR-17-5P | 99.89 | 73.83 | 2665 |
| HSA-MIR-6780A-5P | 99.88 | 66.69 | 2776 |
| HSA-MIR-106B-5P | 99.88 | 74.72 | 2795 |
| HSA-MIR-20A-5P | 99.88 | 74.76 | 2769 |
Literature-anchored findings (GeneRIF, showing 40)
- The insulin-sensitive glucose transporter, GLUT4, interacts physically with Daxx (PMID:11842083)
- Regulated transport of the glucose transporter GLUT4. A review. (PMID:11994746)
- observed differential response of individual isoforms GLUT1, GLUT3, & GLUT4 in neutrophils and granulocytes to hypoglycemia may represent a mechanism to protect the cells from the stress of glucose deprivation (PMID:12064911)
- The expression of the glucose transporter 4 was downregulated by up to 80% in the failing heart. (PMID:12145475)
- an effect of acid maltase deficiency extending to various vesicle systems linked to lysosomes. The enzyme defect may also affect the homoeostasis of receptors cycling through these organelles such as glucose transporter 4. (PMID:12467732)
- Data describe the expression of peroxisome proliferator-activated receptor gamma (PPAR gamma) co-activator 1, PPAR gamma, insulin receptor substrate-1, glucose transporter isoform-4, and mitochondrial uncoupling protein-1 in adipose tissue. (PMID:12565902)
- Embedded in microvillous (maternal-facing) and basal (fetal-facing) membranes of syncytiotrophoblast, main placental barrier layer. (review) (PMID:12583599)
- upregulation of the p38 mitogen-activated protein kinase pathway might contribute to the loss of GLUT4 protein expression observed in adipose tissue from type 2 diabetic patients (PMID:12606502)
- Data suggest that GLUT4 is transported from the cell surface to a subdomain of the trans-Golgi network that is enriched in syntaxins 6 and 16 and that an acidic targeting motif in the C-terminal tail of GLUT4 plays an important role in this process. (PMID:12631717)
- The regulation of the GLUT4 gene is of special clinical interest because insulin-mediated glucose homeostasis is highly sensitive to the levels of GLUT4 protein in muscle and adipose tissue, as evidenced in this review. (PMID:12700047)
- Expression in human slow-twitch muscle fibres is not correlated with intracellular triglyceride content. (PMID:12716391)
- AICAR increases glucose transport and cell-surface GLUT4 content in skeletal muscle from subjects with type 2 diabetes. (PMID:12716734)
- TUG traps endocytosed GLUT4 and tethers it intracellularly, and insulin mobilizes this pool of retained GLUT4 by releasing this tether (PMID:14562105)
- GLUT4 transcription activation depends on the protein-protein interaction of GEF and MEF2A (PMID:14630949)
- Strength training increases the muscle content of GLUT4. (PMID:14747278)
- ATPase inhibitors block translocation of GLUT4 in adipose cells by inhibiting formation of small insulin-responsive vesicles on donor intracellular membranes. (PMID:15166000)
- Muscle samples were obtained before the start of cycle exercise training and 24 h after the first and seventh exercise sessions. GLUT-4 protein expression was increased after 7 days of exercise training compared to baseline. (PMID:15184360)
- EHD1 and EHBP1, but not EHD2, are required for perinuclear localization of GLUT4 and reveal that loss of EHBP1 disrupts insulin-regulated GLUT4 recycling in cultured adipocytes. (PMID:15247266)
- GLUT4 is present in endometrium of normal and polycystic ovary syndrome (PCOS)subjects. hyperinsulinism and obesity seem to have negative effect on endometrial GLUT4 expression in PCOS. (PMID:15292352)
- 8 weeks of exercise training increases insulin-stimulated glucose disposal primarily by increasing GLUT4 protein expression without enhancing insulin-stimulated phosphatidylinositol 3-Kinase signaling. (PMID:15334390)
- Expression in response to exercise training in glucose intolerant elderly men. (PMID:15480742)
- The insulin-regulatable GLUT4 is expressed in the cytosol of first trimester syncytiotrophoblasts compatible with a role for GLUT4 in placental glucose transport in early pregnancy. (PMID:15528266)
- endometrial GLUT4 expression is not affected by polycystic ovary syndrome itself, whereas it is reduced by obesity in those patients. (PMID:15731326)
- Enhanced insulin-stimulated glycogen synthesis in human skeletal muscle cell culture coincides with increased GLUT4 mRNA expression following treatment with various antidiabetic agents. (PMID:15864539)
- Hyperlipidemia, exhibited as a high free fatty acid level, modulates GLUT4 gene expression in cardiac muscle via a complex mechanism including GLUT4 and the PPARgamma genes (PMID:16096283)
- Our findings that AS160 knockdown only partially releases basal GLUT4 retention provides evidence that insulin signals to GLUT4 exocytosis by both AS160-dependent and -independent mechanisms. (PMID:16213228)
- GLUT4 expression is not required for adipogenic differentiation but is necessary for full lipogenic capacity of differentiated adipocytes (PMID:16497797)
- Glut4 plasma membrane translocation and glucose uptake are induced by insulin and leptin in a human neuronal cell line by a phosphatidylinositol 3-kinase- dependent mechanism (PMID:16497805)
- In conclusion, exercise at approximately 40 and approximately 80% V(O2 peak), with total work equal, increased GLUT4 mRNA and GLUT4 protein in human skeletal muscle to a similar extent, despite differences in exercise intensity and duration. (PMID:16763099)
- results suggest that upregulation of GLUT4 gene transcription might be directly mediated by SREBP-1c in adipose tissue (PMID:16787385)
- GLUT4 and GLUT12 were predominantly expressed in type I oxidative fibers; however, GLUT5 was expressed predominantly in type II (white) fibers (PMID:16803853)
- Results suggest involvement of AMP-activated protein kinase in the control of expression of both metabolic genes, UCP3 and GLUT4, in the skeletal muscle of mice and of human newborns. (PMID:16966355)
- Adipose LPIN1 gene expression associates with basal and insulin-mediated subcutaneous adipocyte glucose transport as well as mRNA levels of glucose transporter 4. (PMID:17035674)
- Differences in GLUT4 transcription when whole adipose tissue and cell culture model systems are compared can be correlated to a posttranslational phosphorylation of the transcription factor MEF2A. (PMID:17164432)
- the luminal Vps10p domain of sortilin plays the predominant role in targeting to insulin-responsive Glut4-containing vesicles (PMID:17220298)
- enhanced GLUT4 activity was paralleled by increased transporter abundance in the plasma membrane. Disruption of the SGK1 phosphorylation site on GLUT4 ((S274A)GLUT4) abrogated the stimulating effect of SGK1. (PMID:17382906)
- Our findings implicate the muscular GLUT4 system in the glucose intolerance of liver cirrhosis by a mechanism different from that in diabetes. (PMID:17448565)
- signaling connections spanning the insulin receptor and GLUT4 [REVIEW] (PMID:17496362)
- Findings suggest that characteristic differences in the patterns of glucose uptake can exist according to the histological type and that GLUT1, GLUT3 and GLUT4 could be related to tumor angiogenesis in epithelial ovarian carcinoma. (PMID:17611657)
- Study indicated that further progress in teasing apart the GLUT4 code will require the development and application of novel and advanced technologies that can discriminate one molecule from another in the living cell. (PMID:17717074)
Cross-species orthologs
44 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Slc2a4 | ENSMUSG00000018566 |
| rattus_norvegicus | Slc2a4 | ENSRNOG00000017226 |
| drosophila_melanogaster | Glut3 | FBGN0015230 |
| drosophila_melanogaster | sut4 | FBGN0028560 |
| drosophila_melanogaster | sut3 | FBGN0028561 |
| drosophila_melanogaster | sut2 | FBGN0028562 |
| drosophila_melanogaster | sut1 | FBGN0028563 |
| drosophila_melanogaster | CG4607 | FBGN0029932 |
| drosophila_melanogaster | CG15406 | FBGN0031517 |
| drosophila_melanogaster | CG8837 | FBGN0031520 |
| drosophila_melanogaster | CG3285 | FBGN0031522 |
| drosophila_melanogaster | CG15408 | FBGN0031523 |
| drosophila_melanogaster | CG7882 | FBGN0033047 |
| drosophila_melanogaster | Tret1-2 | FBGN0033644 |
| drosophila_melanogaster | CG8249 | FBGN0034045 |
| drosophila_melanogaster | CG6484 | FBGN0034247 |
| drosophila_melanogaster | CG14160 | FBGN0036066 |
| drosophila_melanogaster | nebu | FBGN0036316 |
| drosophila_melanogaster | CG1208 | FBGN0037386 |
| drosophila_melanogaster | CG14606 | FBGN0037485 |
| drosophila_melanogaster | CG14605 | FBGN0037486 |
| drosophila_melanogaster | CG6901 | FBGN0038414 |
| drosophila_melanogaster | CG17929 | FBGN0038415 |
| drosophila_melanogaster | CG17930 | FBGN0038416 |
| drosophila_melanogaster | Tret1-1 | FBGN0050035 |
| drosophila_melanogaster | CG32053 | FBGN0052053 |
| drosophila_melanogaster | CG32054 | FBGN0052054 |
| drosophila_melanogaster | CG33281 | FBGN0053281 |
| drosophila_melanogaster | CG33282 | FBGN0053282 |
| drosophila_melanogaster | Srg2 | FBGN0262007 |
| drosophila_melanogaster | CG42826 | FBGN0262008 |
| caenorhabditis_elegans | WBGENE00008730 | |
| caenorhabditis_elegans | WBGENE00010684 | |
| caenorhabditis_elegans | WBGENE00010811 | |
| caenorhabditis_elegans | WBGENE00012536 | |
| caenorhabditis_elegans | WBGENE00013074 | |
| caenorhabditis_elegans | WBGENE00016431 | |
| caenorhabditis_elegans | WBGENE00017382 | |
| caenorhabditis_elegans | WBGENE00019207 | |
| caenorhabditis_elegans | WBGENE00019547 | |
| caenorhabditis_elegans | WBGENE00019548 | |
| caenorhabditis_elegans | WBGENE00019549 | |
| caenorhabditis_elegans | WBGENE00019550 | |
| caenorhabditis_elegans | WBGENE00043980 |
Paralogs (13): SLC2A3 (ENSG00000059804), SLC2A9 (ENSG00000109667), SLC2A1 (ENSG00000117394), SLC2A11 (ENSG00000133460), SLC2A8 (ENSG00000136856), SLC2A5 (ENSG00000142583), SLC2A12 (ENSG00000146411), SLC2A13 (ENSG00000151229), SLC2A6 (ENSG00000160326), SLC2A2 (ENSG00000163581), SLC2A14 (ENSG00000173262), SLC2A7 (ENSG00000197241), SLC2A10 (ENSG00000197496)
Protein
Protein identifiers
Solute carrier family 2, facilitated glucose transporter member 4 — P14672 (reviewed: P14672)
Alternative names: Glucose transporter type 4, insulin-responsive
All UniProt accessions (4): P14672, F5H081, I3L1S2, I3L2R4
UniProt curated annotations — full annotation on UniProt →
Function. Insulin-regulated facilitative glucose transporter, which plays a key role in removal of glucose from circulation. Response to insulin is regulated by its intracellular localization: in the absence of insulin, it is efficiently retained intracellularly within storage compartments in muscle and fat cells. Upon insulin stimulation, translocates from these compartments to the cell surface where it transports glucose from the extracellular milieu into the cell.
Subunit / interactions. Interacts with NDUFA9. Binds to DAXX. Interacts via its N-terminus with SRFBP1. Interacts with TRARG1; the interaction is required for proper SLC2A4 recycling after insulin stimulation.
Subcellular location. Cell membrane. Endomembrane system. Cytoplasm. Perinuclear region.
Tissue specificity. Skeletal and cardiac muscles; brown and white fat.
Post-translational modifications. Sumoylated. Palmitoylated. Palmitoylation by ZDHHC7 controls the insulin-dependent translocation of GLUT4 to the plasma membrane.
Disease relevance. Type 2 diabetes mellitus (T2D) [MIM:125853] A multifactorial disorder of glucose homeostasis caused by a lack of sensitivity to insulin. Affected individuals usually have an obese body habitus and manifestations of a metabolic syndrome characterized by diabetes, insulin resistance, hypertension and hypertriglyceridemia. The disease results in long-term complications that affect the eyes, kidneys, nerves, and blood vessels. The disease may be caused by variants affecting the gene represented in this entry.
Domain organisation. The dileucine internalization motif is critical for intracellular sequestration.
Miscellaneous. Insulin-stimulated phosphorylation of TBC1D4 is required for GLUT4 translocation.
Similarity. Belongs to the major facilitator superfamily. Sugar transporter (TC 2.A.1.1) family. Glucose transporter subfamily.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P14672-1 | 1 | yes |
| P14672-2 | 2 |
RefSeq proteins (1): NP_001033* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR002441 | Glc_transpt_4 | Family |
| IPR003663 | Sugar/inositol_transpt | Family |
| IPR005828 | MFS_sugar_transport-like | Family |
| IPR005829 | Sugar_transporter_CS | Conserved_site |
| IPR020846 | MFS_dom | Domain |
| IPR036259 | MFS_trans_sf | Homologous_superfamily |
| IPR045263 | GLUT | Family |
Pfam: PF00083
Catalyzed reactions (Rhea), 1 shown:
- D-glucose(out) = D-glucose(in) (RHEA:60376)
UniProt features (84 total): helix 28, topological domain 13, transmembrane region 12, binding site 6, sequence variant 5, turn 5, modified residue 4, splice variant 2, mutagenesis site 2, chain 1, region of interest 1, short sequence motif 1, lipid moiety-binding region 1, glycosylation site 1, sequence conflict 1, strand 1
Structure
Experimental structures (PDB)
2 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 7WSM | ELECTRON MICROSCOPY | 3.25 |
| 7WSN | ELECTRON MICROSCOPY | 3.31 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P14672-F1 | 88.12 | 0.68 |
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): 177; 298–299; 304; 333; 396; 404
Post-translational modifications (5): 10, 274, 486, 488, 223
Glycosylation sites (1): 57
Mutagenesis-validated functional residues (2):
| Position | Phenotype |
|---|---|
| 223 | loss of palmitoylation. |
| 489–490 | changes subcellular location mainly to the plasma membrane. |
Function
Pathways and Gene Ontology
Reactome pathways
3 pathways
| ID | Pathway |
|---|---|
| R-HSA-1445148 | Translocation of SLC2A4 (GLUT4) to the plasma membrane |
| R-HSA-189200 | Cellular hexose transport |
| R-HSA-381340 | Transcriptional regulation of white adipocyte differentiation |
MSigDB gene sets: 299 (showing top):
REACTOME_TRANSCRIPTIONAL_REGULATION_OF_WHITE_ADIPOCYTE_DIFFERENTIATION, GOBP_MEMORY, GOBP_SYNAPTIC_VESICLE_LOCALIZATION, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_RESPONSE_TO_ETHANOL, GOBP_CARBOHYDRATE_TRANSPORT, FREAC2_01, GOBP_COGNITION, WWTAAGGC_UNKNOWN, GOBP_BEHAVIOR, KEGG_ADIPOCYTOKINE_SIGNALING_PATHWAY, TGCGCANK_UNKNOWN, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_VESICLE_LOCALIZATION, GOBP_RESPONSE_TO_PEPTIDE
GO Biological Process (21): carbohydrate metabolic process (GO:0005975), learning or memory (GO:0007611), short-term memory (GO:0007614), long-term memory (GO:0007616), amylopectin biosynthetic process (GO:0010021), positive regulation of brain-derived neurotrophic factor receptor signaling pathway (GO:0031550), cellular response to insulin stimulus (GO:0032869), glucose homeostasis (GO:0042593), glucose import in response to insulin stimulus (GO:0044381), response to ethanol (GO:0045471), obsolete D-glucose import (GO:0046323), brown fat cell differentiation (GO:0050873), white fat cell proliferation (GO:0070343), dehydroascorbic acid transport (GO:0070837), cellular response to tumor necrosis factor (GO:0071356), cellular response to hypoxia (GO:0071456), cellular response to osmotic stress (GO:0071470), regulation of synaptic vesicle budding from presynaptic endocytic zone membrane (GO:0098694), transport across blood-brain barrier (GO:0150104), D-glucose transmembrane transport (GO:1904659), transmembrane transport (GO:0055085)
GO Molecular Function (4): D-glucose uniporter activity (GO:0015304), D-glucose transmembrane transporter activity (GO:0055056), protein binding (GO:0005515), transmembrane transporter activity (GO:0022857)
GO Cellular Component (24): multivesicular body (GO:0005771), trans-Golgi network (GO:0005802), cytosol (GO:0005829), plasma membrane (GO:0005886), clathrin-coated pit (GO:0005905), external side of plasma membrane (GO:0009897), endomembrane system (GO:0012505), vesicle membrane (GO:0012506), membrane (GO:0016020), sarcoplasmic reticulum (GO:0016529), clathrin-coated vesicle (GO:0030136), trans-Golgi network transport vesicle (GO:0030140), T-tubule (GO:0030315), cytoplasmic vesicle membrane (GO:0030659), insulin-responsive compartment (GO:0032593), sarcolemma (GO:0042383), membrane raft (GO:0045121), perinuclear region of cytoplasm (GO:0048471), extracellular exosome (GO:0070062), presynapse (GO:0098793), cytoplasm (GO:0005737), endosome (GO:0005768), cell surface (GO:0009986), vesicle (GO:0031982)
Reactome top-level categories
Rollup of top-3 pathways:
| Category | Pathways |
|---|---|
| Membrane Trafficking | 1 |
| SLC-mediated transmembrane transport | 1 |
| Adipogenesis | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 6 |
| plasma membrane | 3 |
| memory | 2 |
| cytoplasm | 2 |
| membrane | 2 |
| primary metabolic process | 1 |
| behavior | 1 |
| cognition | 1 |
| macromolecule biosynthetic process | 1 |
| carbohydrate derivative biosynthetic process | 1 |
| amylopectin metabolic process | 1 |
| positive regulation of signal transduction | 1 |
| brain-derived neurotrophic factor receptor signaling pathway | 1 |
| regulation of brain-derived neurotrophic factor receptor signaling pathway | 1 |
| response to insulin | 1 |
| cellular response to peptide hormone stimulus | 1 |
| carbohydrate homeostasis | 1 |
| cellular response to insulin stimulus | 1 |
| D-glucose import across plasma membrane | 1 |
| response to alcohol | 1 |
| fat cell differentiation | 1 |
| fat cell proliferation | 1 |
| vitamin transport | 1 |
| response to tumor necrosis factor | 1 |
| cellular response to cytokine stimulus | 1 |
| response to hypoxia | 1 |
| cellular response to stress | 1 |
| cellular response to decreased oxygen levels | 1 |
| response to osmotic stress | 1 |
| cellular response to chemical stress | 1 |
| cellular response to abiotic stimulus | 1 |
| synaptic vesicle budding from presynaptic endocytic zone membrane | 1 |
| regulation of organelle organization | 1 |
| vascular transport | 1 |
| hexose transmembrane transport | 1 |
| hexose uniporter activity | 1 |
| D-glucose transmembrane transporter activity | 1 |
| hexose transmembrane transporter activity | 1 |
| binding | 1 |
| transporter activity | 1 |
Protein interactions and networks
STRING
3882 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| SLC2A4 | INS | P01308 | 978 |
| SLC2A4 | TBC1D4 | O60343 | 969 |
| SLC2A4 | IRS1 | P35568 | 939 |
| SLC2A4 | VAMP2 | P19065 | 911 |
| SLC2A4 | LNPEP | Q9UIQ6 | 891 |
| SLC2A4 | AKT1 | P31749 | 886 |
| SLC2A4 | ADIPOQ | Q15848 | 877 |
| SLC2A4 | PPARG | P37231 | 872 |
| SLC2A4 | RAB10 | P61026 | 844 |
| SLC2A4 | DAXX | Q9UER7 | 841 |
| SLC2A4 | LEP | P41159 | 838 |
| SLC2A4 | STX4 | Q12846 | 822 |
| SLC2A4 | RHOQ | P17081 | 806 |
| SLC2A4 | IRS2 | Q9Y4H2 | 805 |
| SLC2A4 | STXBP3 | O00186 | 804 |
IntAct
20 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| DAXX | SLC2A4 | psi-mi:“MI:0915”(physical association) | 0.630 |
| SLC2A4 | DAXX | psi-mi:“MI:0915”(physical association) | 0.630 |
| SLC2A4 | CREB3 | psi-mi:“MI:0915”(physical association) | 0.560 |
| SLC2A4 | tax | psi-mi:“MI:0915”(physical association) | 0.490 |
| tax | SLC2A4 | psi-mi:“MI:0915”(physical association) | 0.490 |
| ALG13 | SLC2A4 | psi-mi:“MI:0915”(physical association) | 0.400 |
| SLC2A4 | SMAP2 | psi-mi:“MI:0914”(association) | 0.350 |
| SLC2A4 | TUBB2A | psi-mi:“MI:0914”(association) | 0.350 |
| SLC2A4 | RAB29 | psi-mi:“MI:0914”(association) | 0.350 |
| UPK2 | IFT56 | psi-mi:“MI:0914”(association) | 0.350 |
| SLC2A4 | PTPRA | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (85): SLC2A4 (Reconstituted Complex), DNAJC12 (Affinity Capture-MS), WDR73 (Affinity Capture-MS), SMAP2 (Affinity Capture-MS), AP1M1 (Reconstituted Complex), CREB3 (Two-hybrid), SMAP2 (Affinity Capture-MS), DNAJC12 (Affinity Capture-MS), SLC2A4 (Affinity Capture-Western), DAXX (Reconstituted Complex), DAXX (Affinity Capture-Western), SLC2A4 (Affinity Capture-Western), SLC2A4 (Reconstituted Complex), GOPC (Affinity Capture-Western), GOPC (Co-fractionation)
ESM2 similar proteins: A4ZYQ5, O35956, O57379, O62786, O62787, P0C6A1, P11166, P11167, P11168, P11169, P12336, P13355, P14142, P14246, P14672, P17809, P19357, P20303, P22732, P27674, P28568, P32037, P43427, P46896, P47842, P47843, P58351, P58352, P58353, P79365, Q07647, Q27994, Q28ES4, Q5R608, Q5RET7, Q66J52, Q6A4L0, Q6DFR1, Q6NUB3, Q6NYN7
Diamond homologs: A0A0H2VG78, A1Z8N1, A4ZYQ5, A5LGM7, A9ZSY2, A9ZSY3, B0WC46, B3MG58, B3NSE1, B4GAP7, B4HNS0, B4HNS1, B4J913, B4KR05, B4LPX5, B4MYA4, B4P624, B4QBN2, B4QBN3, C0SPB2, O04036, O04249, O34718, O44827, O52733, O62787, P0AE24, P0AE25, P0AEP1, P0AEP2, P0C6A1, P11166, P11167, P11169, P13355, P14142, P14246, P14672, P15686, P17809
SIGNOR signaling
15 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| EXOC7 | up-regulates | SLC2A4 | |
| PPARGC1A | “up-regulates quantity by expression” | SLC2A4 | “transcriptional regulation” |
| PRKAA1 | “up-regulates quantity by expression” | SLC2A4 | “transcriptional regulation” |
| MAPK1 | up-regulates | SLC2A4 | |
| INS | “up-regulates activity” | SLC2A4 | |
| AKT1 | up-regulates | SLC2A4 | |
| SLC2A4 | “up-regulates quantity” | glucose | relocalization |
| SLC2A4 | “up-regulates quantity” | α-D-glucose | relocalization |
| TP53 | “down-regulates quantity by repression” | SLC2A4 | “transcriptional regulation” |
| AKT | up-regulates | SLC2A4 | |
| RHOQ | up-regulates | SLC2A4 | |
| TBC1D4 | down-regulates | SLC2A4 | |
| SGK1 | “up-regulates activity” | SLC2A4 | phosphorylation |
| MEF2A | “up-regulates quantity by expression” | SLC2A4 | “transcriptional regulation” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
68 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 1 |
| Likely pathogenic | 0 |
| Uncertain significance | 50 |
| Likely benign | 5 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 980124 | GRCh37/hg19 17p13.1(chr17:7014481-7283233)x1 | Pathogenic |
SpliceAI
1605 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 17:7281965:GAA:G | donor_gain | 1.0000 |
| 17:7281968:G:GG | donor_gain | 1.0000 |
| 17:7283230:T:TA | acceptor_gain | 1.0000 |
| 17:7283234:T:TA | acceptor_gain | 1.0000 |
| 17:7283238:T:TA | acceptor_gain | 1.0000 |
| 17:7283242:CAG:C | acceptor_loss | 1.0000 |
| 17:7283243:A:AG | acceptor_gain | 1.0000 |
| 17:7283243:AG:A | acceptor_gain | 1.0000 |
| 17:7283243:AGGAT:A | acceptor_gain | 1.0000 |
| 17:7283244:G:GG | acceptor_gain | 1.0000 |
| 17:7283244:GG:G | acceptor_gain | 1.0000 |
| 17:7283244:GGA:G | acceptor_gain | 1.0000 |
| 17:7283244:GGAT:G | acceptor_gain | 1.0000 |
| 17:7283244:GGATG:G | acceptor_gain | 1.0000 |
| 17:7283358:GAAG:G | donor_gain | 1.0000 |
| 17:7283359:AAGGT:A | donor_loss | 1.0000 |
| 17:7283361:GGT:G | donor_loss | 1.0000 |
| 17:7283362:G:GG | donor_gain | 1.0000 |
| 17:7283363:T:A | donor_loss | 1.0000 |
| 17:7283642:G:GT | donor_gain | 1.0000 |
| 17:7283643:A:T | donor_gain | 1.0000 |
| 17:7283732:T:A | acceptor_gain | 1.0000 |
| 17:7283735:CAG:C | acceptor_loss | 1.0000 |
| 17:7283736:A:AG | acceptor_gain | 1.0000 |
| 17:7283736:AG:A | acceptor_gain | 1.0000 |
| 17:7283737:G:A | acceptor_loss | 1.0000 |
| 17:7283737:G:GG | acceptor_gain | 1.0000 |
| 17:7283737:GG:G | acceptor_gain | 1.0000 |
| 17:7283737:GGA:G | acceptor_gain | 1.0000 |
| 17:7283737:GGAAA:G | acceptor_gain | 1.0000 |
AlphaMissense
3234 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 17:7283327:G:A | G39E | 0.999 |
| 17:7284662:G:A | G302D | 0.999 |
| 17:7284907:G:C | G330R | 0.999 |
| 17:7285765:T:C | F395L | 0.999 |
| 17:7285767:T:A | F395L | 0.999 |
| 17:7285767:T:G | F395L | 0.999 |
| 17:7285894:T:C | F438L | 0.999 |
| 17:7285896:C:A | F438L | 0.999 |
| 17:7285896:C:G | F438L | 0.999 |
| 17:7283326:G:T | G39W | 0.998 |
| 17:7283349:T:A | N46K | 0.998 |
| 17:7283349:T:G | N46K | 0.998 |
| 17:7284072:G:C | G183R | 0.998 |
| 17:7284646:A:C | S297R | 0.998 |
| 17:7284648:C:A | S297R | 0.998 |
| 17:7284648:C:G | S297R | 0.998 |
| 17:7284661:G:C | G302R | 0.998 |
| 17:7284662:G:T | G302V | 0.998 |
| 17:7285133:G:C | G356R | 0.998 |
| 17:7285774:G:C | G398R | 0.998 |
| 17:7285775:G:A | G398D | 0.998 |
| 17:7283326:G:A | G39R | 0.997 |
| 17:7283326:G:C | G39R | 0.997 |
| 17:7283327:G:T | G39V | 0.997 |
| 17:7283338:G:T | G43W | 0.997 |
| 17:7283339:G:A | G43E | 0.997 |
| 17:7283851:G:A | G146D | 0.997 |
| 17:7284073:G:A | G183D | 0.997 |
| 17:7284258:G:C | W202C | 0.997 |
| 17:7284258:G:T | W202C | 0.997 |
dbSNP variants (sampled 300 via entrez): RS1000383151 (17:7281724 T>G), RS1000435440 (17:7281414 T>C), RS1000718694 (17:7280386 T>C), RS1001013141 (17:7288156 G>A), RS1001247756 (17:7282078 G>A), RS1001330377 (17:7286118 C>T), RS1001446536 (17:7282663 G>A), RS1001655463 (17:7288684 G>A,T), RS1002981482 (17:7285495 A>C,G), RS1003034743 (17:7285243 G>A), RS1003735999 (17:7284241 G>A), RS1004446261 (17:7286899 T>C), RS1004795067 (17:7285432 T>C), RS1004986805 (17:7282670 G>C), RS1005337928 (17:7282331 C>T)
Disease associations
OMIM: gene MIM:138190 | disease phenotypes: MIM:125853
GenCC curated gene-disease
Mondo (1): type 2 diabetes mellitus (MONDO:0005148)
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
23 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001391_6 | Metabolite levels | 3.000000e-14 |
| GCST001758_8 | Birth weight | 5.000000e-06 |
| GCST004278_28 | Pulse pressure | 2.000000e-10 |
| GCST004278_46 | Pulse pressure | 2.000000e-07 |
| GCST004280_69 | Diastolic blood pressure | 1.000000e-13 |
| GCST006190_4 | Diastolic blood pressure x smoking status (ever vs never) interaction (2df test) | 3.000000e-10 |
| GCST006190_54 | Diastolic blood pressure x smoking status (ever vs never) interaction (2df test) | 3.000000e-08 |
| GCST006192_52 | Systolic blood pressure x smoking status (ever vs never) interaction (2df test) | 8.000000e-11 |
| GCST006192_75 | Systolic blood pressure x smoking status (ever vs never) interaction (2df test) | 2.000000e-12 |
| GCST006193_37 | Diastolic blood pressure x smoking status (current vs non-current) interaction (2df test) | 9.000000e-11 |
| GCST006193_75 | Diastolic blood pressure x smoking status (current vs non-current) interaction (2df test) | 9.000000e-09 |
| GCST006195_19 | Systolic blood pressure x smoking status (current vs non-current) interaction (2df test) | 3.000000e-11 |
| GCST006195_69 | Systolic blood pressure x smoking status (current vs non-current) interaction (2df test) | 1.000000e-12 |
| GCST007267_235 | Systolic blood pressure | 7.000000e-12 |
| GCST007928_7 | Medication use (diuretics) | 8.000000e-11 |
| GCST008362_88 | Birth weight | 1.000000e-24 |
| GCST008363_6 | Offspring birth weight | 5.000000e-11 |
| GCST010243_87 | Apolipoprotein B levels | 1.000000e-10 |
| GCST90011898_55 | Alanine aminotransferase levels | 2.000000e-12 |
| GCST90011899_141 | Aspartate aminotransferase levels | 2.000000e-11 |
| GCST90013405_8 | Liver enzyme levels (alanine transaminase) | 4.000000e-18 |
| GCST90013663_18 | Alanine aminotransferase levels | 1.000000e-21 |
| GCST90013664_44 | Aspartate aminotransferase levels | 9.000000e-16 |
EFO canonical traits (10, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004725 | metabolite measurement |
| EFO:0004344 | birth weight |
| EFO:0005763 | pulse pressure measurement |
| EFO:0006336 | diastolic blood pressure |
| EFO:0006527 | smoking status measurement |
| EFO:0006335 | systolic blood pressure |
| EFO:0009928 | Diuretic use measurement |
| EFO:0005939 | parental genotype effect measurement |
| EFO:0004615 | apolipoprotein B measurement |
| EFO:0004736 | aspartate aminotransferase measurement |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D003924 | Diabetes Mellitus, Type 2 | C18.452.394.750.149; C19.246.300 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL5874 (SINGLE PROTEIN)
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: transporter — Class I transporters
ChEMBL bioactivities
69 potent at pChembl≥5 of 72 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 7.89 | IC50 | 13 | nM | CHEMBL5661873 |
| 7.80 | IC50 | 16 | nM | CHEMBL5661842 |
| 7.80 | IC50 | 16 | nM | CHEMBL5661852 |
| 7.77 | IC50 | 17 | nM | CHEMBL5661939 |
| 7.54 | IC50 | 29 | nM | CHEMBL5661888 |
| 7.36 | IC50 | 44 | nM | CHEMBL5661849 |
| 7.21 | IC50 | 61 | nM | CHEMBL5661933 |
| 7.06 | IC50 | 88 | nM | CHEMBL5661878 |
| 7.05 | IC50 | 90 | nM | CHEMBL4089982 |
| 7.05 | IC50 | 90 | nM | CHEMBL5661828 |
| 7.03 | IC50 | 94 | nM | CHEMBL5661843 |
| 7.02 | IC50 | 95 | nM | CHEMBL5661915 |
| 6.92 | IC50 | 120 | nM | CHEMBL5661884 |
| 6.80 | IC50 | 160 | nM | CHEMBL5661913 |
| 6.77 | IC50 | 170 | nM | CHEMBL5661901 |
| 6.75 | IC50 | 180 | nM | CHEMBL5661910 |
| 6.72 | IC50 | 190 | nM | CHEMBL5661921 |
| 6.71 | IC50 | 195 | nM | CHEMBL4061928 |
| 6.70 | IC50 | 200 | nM | BAY-876 |
| 6.66 | IC50 | 220 | nM | CHEMBL5661932 |
| 6.57 | IC50 | 270 | nM | BAY-876 |
| 6.55 | IC50 | 280 | nM | CHEMBL5661859 |
| 6.55 | IC50 | 280 | nM | CYTOCHALASIN B |
| 6.54 | IC50 | 290 | nM | BAY-876 |
| 6.47 | IC50 | 340 | nM | CHEMBL5661924 |
| 6.44 | IC50 | 360 | nM | CHEMBL5661938 |
| 6.43 | IC50 | 370 | nM | CHEMBL5661908 |
| 6.43 | IC50 | 370 | nM | CHEMBL5661847 |
| 6.42 | IC50 | 380 | nM | CHEMBL5661874 |
| 6.40 | IC50 | 400 | nM | CHEMBL5661838 |
| 6.39 | IC50 | 410 | nM | CHEMBL5661911 |
| 6.38 | IC50 | 420 | nM | CHEMBL5661918 |
| 6.30 | IC50 | 500 | nM | BAY-588 |
| 6.27 | IC50 | 540 | nM | CHEMBL5661930 |
| 6.21 | IC50 | 610 | nM | CHEMBL5661907 |
| 6.21 | IC50 | 620 | nM | CHEMBL5661934 |
| 6.17 | IC50 | 680 | nM | CHEMBL5661848 |
| 6.06 | IC50 | 870 | nM | CHEMBL5661919 |
| 6.05 | IC50 | 890 | nM | CHEMBL5661895 |
| 6.04 | IC50 | 910 | nM | CHEMBL5661844 |
| 6.04 | IC50 | 910 | nM | CHEMBL5661850 |
| 6.02 | IC50 | 950 | nM | CHEMBL5661929 |
| 6.00 | IC50 | 1000 | nM | CHEMBL5661845 |
| 5.97 | IC50 | 1070 | nM | CHEMBL5661836 |
| 5.95 | IC50 | 1130 | nM | CHEMBL5661902 |
| 5.94 | IC50 | 1140 | nM | CHEMBL5661892 |
| 5.88 | IC50 | 1330 | nM | CHEMBL5661834 |
| 5.87 | IC50 | 1350 | nM | CHEMBL5661867 |
| 5.78 | IC50 | 1670 | nM | CHEMBL5661833 |
| 5.77 | IC50 | 1700 | nM | CHEMBL4171968 |
PubChem BioAssay actives
61 with measured affinity, of 95 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-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-6-methoxyquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.0130 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-5,7-difluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.0160 | uM |
| 4-N-[1-[(5-cyanopyrazin-2-yl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.0160 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-5-methylquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.0170 | uM |
| 8-chloro-4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]quinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.0290 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-6-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.0440 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-1,7-naphthyridine-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.0610 | uM |
| 4-N-[1-[(2-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.0880 | uM |
| (2S)-3-(2-bromophenyl)-2-[[2-(4-methoxyphenyl)acetyl]amino]-N-[(1S)-1-phenylethyl]propanamide | 1425911: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake | ic50 | 0.0900 | uM |
| N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-2-(1,3-thiazol-2-yl)quinoline-4-carboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.0900 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-5-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.0940 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-methylquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.0950 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-6-methylquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.1200 | uM |
| 4-N-[1-[(5-cyanothiophen-2-yl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.1600 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]quinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.1700 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-6,7-difluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.1800 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-8-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.1900 | uM |
| (2S)-3-(4-fluorophenyl)-2-[[2-(3-hydroxyphenyl)acetyl]amino]-N-[(1S)-1-phenylethyl]propanamide | 1425911: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake | ic50 | 0.1950 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2165766: Inhibition of human GLUT4 expressed in CHO cells measured after 15 mins by cell-titer-Glo luminescent cell viability assay | ic50 | 0.2000 | uM |
| 6-bromo-N-[1-[(4-fluorophenyl)methyl]-3,5-dimethylpyrazol-4-yl]-2-(trifluoromethyl)quinoline-4-carboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.2200 | uM |
| 7-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-[1,3]thiazolo[5,4-b]pyridine-5,7-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.2800 | uM |
| (1S,4E,6R,10R,12E,14S,15S,17S,18S,19S)-19-benzyl-6,15-dihydroxy-10,17-dimethyl-16-methylidene-2-oxa-20-azatricyclo[12.7.0.01,18]henicosa-4,12-diene-3,21-dione | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.2800 | uM |
| 6-bromo-N-[1-[2-(4-fluorophenyl)ethyl]-3,5-dimethylpyrazol-4-yl]-2-(trifluoromethyl)quinoline-4-carboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.3400 | uM |
| N-[1-[(4-fluorophenyl)methyl]-3,5-dimethylpyrazol-4-yl]-2,6-dimethylquinoline-4-carboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.3600 | uM |
| 7-fluoro-4-N-[5-methyl-1-[[4-(trifluoromethoxy)phenyl]methyl]-3-(trifluoromethyl)pyrazol-4-yl]quinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.3700 | uM |
| 4-N-[1-[(4-ethylphenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.3700 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-1,6-naphthyridine-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.3800 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-3-methylpyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.4000 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.4100 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methylpyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.4200 | uM |
| 4-N-[1-[(4-tert-butylphenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.5000 | uM |
| N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-2-(2-methyl-1,2,4-triazol-3-yl)quinoline-4-carboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.5400 | uM |
| 7-fluoro-4-N-[5-methyl-1-[(3-methylphenyl)methyl]-3-(trifluoromethyl)pyrazol-4-yl]quinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.6100 | uM |
| 4-N-[1-[(5-cyano-2-pyridinyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.6200 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-3,5-dimethylpyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.6800 | uM |
| 6-bromo-N-[1-[(4-cyano-2-fluorophenyl)methyl]-3,5-dimethylpyrazol-4-yl]-2-(trifluoromethyl)quinoline-4-carboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.8700 | uM |
| 4-N-[1-[(4-cyano-1,3-thiazol-2-yl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.8900 | uM |
| 7-fluoro-4-N-[5-methyl-3-(trifluoromethyl)-1-[[4-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]quinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.9100 | uM |
| N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-2-(2,4-dimethyl-1,3-thiazol-5-yl)quinoline-4-carboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.9100 | uM |
| 4-N-[1-[(3-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 0.9500 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-1,8-naphthyridine-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 1.0000 | uM |
| 7-fluoro-4-N-[5-methyl-1-[[3-(trifluoromethoxy)phenyl]methyl]-3-(trifluoromethyl)pyrazol-4-yl]quinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 1.0700 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoro-2-N-(2-morpholin-4-ylethyl)quinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 1.1300 | uM |
| 7-fluoro-4-N-[5-methyl-1-[(2-methylphenyl)methyl]-3-(trifluoromethyl)pyrazol-4-yl]quinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 1.1400 | uM |
| 4-N-[1-[(5-cyanopyrimidin-2-yl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 1.3300 | uM |
| 4-N-[1-[(3-cyano-1,2-oxazol-5-yl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoroquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 1.3500 | uM |
| 4-N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-methoxyquinoline-2,4-dicarboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 1.6700 | uM |
| N-[[3-[2-(4-fluorophenyl)ethoxy]phenyl]methyl]-4-methoxy-N-(pyridin-4-ylmethyl)benzamide | 1501205: Antagonist activity at human GLUT4 expressed in HEK293 cells transfected with GLUT1 shRNA assessed as inhibition of [3H]2-deoxy-D-glucose uptake preincubated for 5 mins followed by [3H]2-deoxy-D-glucose addition and measured after 6 mins | ic50 | 1.7000 | uM |
| N-[1-[(4-cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)pyrazol-4-yl]-7-fluoro-2-(3-hydroxyazetidine-1-carbonyl)quinoline-4-carboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 1.7800 | uM |
| 6-bromo-N-[1-[(5-cyano-2-pyridinyl)methyl]-3,5-dimethylpyrazol-4-yl]-2-(trifluoromethyl)quinoline-4-carboxamide | 2155045: Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay | ic50 | 2.0200 | uM |
CTD chemical–gene interactions
95 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Rosiglitazone | affects cotreatment, increases expression, affects binding, decreases reaction, increases reaction | 7 |
| sodium arsenite | affects cotreatment, affects localization, decreases reaction, affects reaction, increases expression (+3 more) | 6 |
| Dexamethasone | increases reaction, affects cotreatment, increases expression, affects expression | 5 |
| bisphenol A | decreases expression, increases expression, affects cotreatment, affects binding, increases reaction | 4 |
| Benzo(a)pyrene | decreases expression, increases methylation | 4 |
| Metformin | affects reaction, decreases expression, decreases reaction, increases expression | 4 |
| 1-Methyl-3-isobutylxanthine | affects cotreatment, increases expression, increases reaction | 4 |
| Tetrachlorodibenzodioxin | decreases expression, affects expression | 3 |
| Palmitic Acid | decreases reaction, affects cotreatment, affects expression, decreases expression | 3 |
| Arsenic | affects cotreatment, increases abundance, affects expression, decreases expression | 2 |
| Dichlorodiphenyl Dichloroethylene | decreases reaction, affects cotreatment, increases expression, increases reaction, decreases expression | 2 |
| Diethylhexyl Phthalate | decreases expression, decreases reaction | 2 |
| Estradiol | increases expression | 2 |
| Testosterone | affects reaction, decreases expression, affects cotreatment, increases expression | 2 |
| Aflatoxin B1 | decreases expression | 2 |
| aristolochic acid I | decreases expression | 1 |
| STF-31 | affects cotreatment, decreases expression, decreases reaction | 1 |
| AKT activator SC79 | affects cotreatment, affects localization, decreases reaction | 1 |
| propionaldehyde | increases expression | 1 |
| 2,4,5,2’,4’,5’-hexachlorobiphenyl | decreases reaction, affects cotreatment, decreases expression | 1 |
| mono-(2-ethylhexyl)phthalate | decreases expression | 1 |
| cobaltous chloride | decreases expression | 1 |
| butyraldehyde | increases expression | 1 |
| perfluorooctanoic acid | affects cotreatment, decreases expression, decreases reaction | 1 |
| 3-methyladenine | increases reaction, decreases expression | 1 |
| ursodoxicoltaurine | decreases reaction, decreases expression | 1 |
| benazol P | affects expression | 1 |
| S-(1,2-dichlorovinyl)cysteine | decreases reaction, increases expression | 1 |
| prochloraz | decreases expression | 1 |
| arsenic disulfide | decreases expression | 1 |
ChEMBL screening assays
24 unique, capped per target: 23 binding, 1 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1103148 | Binding | Inhibition of GLUT4 | Iridoids from Fraxinus excelsior with adipocyte differentiation-inhibitory and PPARalpha activation activity. — J Nat Prod |
| CHEMBL5209607 | Functional | Inhibition of the Glucose Transporter (GLUT4, SLC2A4) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A4 WT-OE cells (PubChe | Flow cytometry transport assay for SLC2A4 using HEK293 JumpIN TRex SLC2A4 WT-OE cells |
Cellosaurus cell lines
6 cell lines: 6 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B2FT | Abcam HeLa SLC2A4 KO | Cancer cell line | Female |
| CVCL_D4T2 | HuH7-SLC2A4-KO-c1 | Cancer cell line | Male |
| CVCL_D4T3 | HuH7-SLC2A4-KO-c2 | Cancer cell line | Male |
| CVCL_D4VR | LS180-SLC2A4-KO-c5 | Cancer cell line | Female |
| CVCL_D4VS | LS180-SLC2A4-KO-c7 | Cancer cell line | Female |
| CVCL_D8VB | Ubigene HCT 116 SLC2A4 KO | Cancer cell line | Male |
Clinical trials (associated diseases)
300 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00006163 | PHASE4 | COMPLETED | Computer-assisted Diabetes Self-management Interventions |
| NCT00036504 | PHASE4 | COMPLETED | Efficacy and Safety of Twice-Daily Insulin Lispro Low Mixture Compared to a Once-Daily Long Acting Insulin Comparator in Patients Who Have Been Using One or More Oral Antihyperglycemic Agents Without Insulin |
| NCT00044460 | PHASE4 | COMPLETED | Efficacy and Safety In Poorly Controlled Type 2 Diabetics |
| NCT00095446 | PHASE4 | COMPLETED | NovoLog Observation Trial in Subjects With Type 1 and Type 2 Diabetes |
| NCT00101751 | PHASE4 | COMPLETED | INITIATE Plus (INITiation of Insulin to Reach A1c TargEt) Study |
| NCT00110370 | PHASE4 | COMPLETED | Comparing Pre-Mixed Insulin With Insulin Glargine Combined With Rapid-Acting Insulin in Patients With Type 2 Diabetes |
| NCT00110448 | PHASE4 | COMPLETED | Japanese Primary Prevention of Atherosclerosis With Aspirin for Diabetes (JPAD) Trial |
| NCT00118950 | PHASE4 | COMPLETED | Effect of Metformin Versus Repaglinide Treatment in Non-Obese Type 2 Diabetic Patients Uncontrolled by Diet |
| NCT00118963 | PHASE4 | COMPLETED | Effect of Repaglinide Versus Metformin Treatment in Non-Obese Patients With Type-2-Diabetes |
| NCT00121966 | PHASE4 | COMPLETED | South Danish Diabetes Study: Evaluation of the Antidiabetic Treatment of Type 2 Diabetes Mellitus |
| NCT00123604 | PHASE4 | COMPLETED | Vascular Effects of Carvedilol Versus Metoprolol in Hypertensive Patients With Type 2 Diabetes |
| NCT00123643 | PHASE4 | COMPLETED | Vascular Effects of Rosiglitazone Versus Glyburide in Type 2 Diabetic Patients |
| NCT00124397 | PHASE4 | COMPLETED | Atorvastatin and Endothelial Function in Type 2 Diabetes Mellitus (ATTEND-Study) |
| NCT00129233 | PHASE4 | COMPLETED | Comparison of Valsartan With Amlodipine in Hypertensive Patients With Glucose Intolerance |
| NCT00133718 | PHASE4 | COMPLETED | A 2 Year Trial of Patients With Type 2 Diabetes Focusing on Cardiovascular Diagnostics and Metabolic Control |
| NCT00135070 | PHASE4 | TERMINATED | Hospital In-Patient Insulin Study |
| NCT00141232 | PHASE4 | COMPLETED | Evaluating Atorvastatin With Omega-3 Fatty Acids in Cardiovascular Risk Reduction in Patients With Type 2 Diabetes |
| NCT00144144 | PHASE4 | UNKNOWN | A Study on Ca Blocker Versus AII Antagonists in Hypertension With Type 2 Diabetes |
| NCT00149331 | PHASE4 | COMPLETED | The Effects of Two Education Strategies About Insulin on Patient Preferences and Perceptions About Insulin Therapy |
| NCT00162357 | PHASE4 | COMPLETED | Post-PCI:Cardiac Imaging in Patients With Diabetes to Detect Coronary Artery Blockages Previously Opened by Angioplasty |
| NCT00174681 | PHASE4 | COMPLETED | Tulip Study: Testing the Usefulness of Lantus When Initiated Prematurely In Patients With Type 2 Diabetes |
| NCT00174824 | PHASE4 | COMPLETED | Comparison of Insulin Glargine and NPH Human Insulin in Progression of Diabetic Retinopathy in Type 2 Diabetic Patients |
| NCT00177398 | PHASE4 | COMPLETED | Effect of Glargine Insulin on Glucose Control in Hospitalized Patients Who Receive Tube Feedings |
| NCT00179400 | PHASE4 | COMPLETED | The Role of Acute Combined PPAR Alpha and Gamma Stimulation on Insulin Action in Humans |
| NCT00184561 | PHASE4 | COMPLETED | Effectiveness and Safety of Biphasic Insulin Aspart 70/30 in Subjects With Type 2 Diabetes |
| NCT00184626 | PHASE4 | COMPLETED | Comparison of Insulin Glargine Versus Biphasic Insulin Aspart 30/70 or Biphasic Insulin Aspart 30/70 in Combination With Metformin in Subjects With Type 2 Diabetes. |
| NCT00191178 | PHASE4 | COMPLETED | Effects of Insulin in Perceived Mood Symptoms in Patients With Type 2 Diabetes |
| NCT00191282 | PHASE4 | COMPLETED | Hyperglycemia and Cardiovascular Outcomes With Type 2 Diabetes |
| NCT00191464 | PHASE4 | COMPLETED | Long-Term Effects of Insulin Plus Metformin Regimens on the Overall and Postprandial Glycemic Control of Patients With Type 2 Diabetes |
| NCT00192803 | PHASE4 | UNKNOWN | Non-Insulin Dependent Diabetes Mellitus (NIDDM) and Angiotensin Converting Enzyme 2 (ACE2): Diabetic Patients Treated With Antihypertensive Drugs |
| NCT00202033 | PHASE4 | COMPLETED | Impact of Self-Monitoring Blood Glucose Frequency on Glycemic Control in Patients With Type 2 Diabetes |
| NCT00205660 | PHASE4 | COMPLETED | Changes in Adiposity, Metabolic Measures From Atypicals to Aripiprazole |
| NCT00212290 | PHASE4 | COMPLETED | Insulin Resistance and Central Nervous System (CNS) Function in Type 2 Diabetes |
| NCT00212303 | PHASE4 | COMPLETED | Exercise Training in Type 2 Diabetes and Hypertension |
| NCT00225342 | PHASE4 | WITHDRAWN | Study Protocol for Rosiglitazone Versus Gliclazide in Diabetics With Angina |
| NCT00238472 | PHASE4 | COMPLETED | A Pilot Study to Evaluate the Effects of Nateglinide vs. Glibenclamide on Renal Hemodynamics and Albumin Excretion |
| NCT00239538 | PHASE4 | COMPLETED | SMOOTH - Blood Pressure Control in Diabetic/Obese Patients |
| NCT00240253 | PHASE4 | COMPLETED | A Study Evaluating the Efficacy and Safety of Adding Symlin® to Lantus® (Insulin Glargine) in Subjects With Type 2 Diabetes |
| NCT00240422 | PHASE4 | COMPLETED | Trial to Compare the Effects of Either Telmisartan (40-80 mg PO Once Daily) or Ramipril (5-10 mg PO Once Daily) on Renal Endothelial Dysfunction in Hypertensive Patients With Type 2 Diabetes |
| NCT00241085 | PHASE4 | COMPLETED | Effect of Valsartan on Proteinuria in Patients With Hypertension and Diabetes Mellitus |
Related Atlas pages
- Targeted by drugs: 2-DEOXY-D-GLUCOSE
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): type 2 diabetes mellitus