SLC47A1
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Also known as FLJ10847MATE1
Summary
SLC47A1 (solute carrier family 47 member 1, HGNC:25588) is a protein-coding gene on chromosome 17p11.2, encoding Multidrug and toxin extrusion protein 1 (Q96FL8). Multidrug efflux pump that functions as a H(+)/organic cation antiporter.
This gene is located within the Smith-Magenis syndrome region on chromosome 17. It encodes a protein of unknown function.
Source: NCBI Gene 55244 — RefSeq curated summary.
At a glance
- GWAS associations: 20
- Clinical variants (ClinVar): 96 total
- Druggable target: yes — 47 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_018242
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:25588 |
| Approved symbol | SLC47A1 |
| Name | solute carrier family 47 member 1 |
| Location | 17p11.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | FLJ10847, MATE1 |
| Ensembl gene | ENSG00000142494 |
| Ensembl biotype | protein_coding |
| OMIM | 609832 |
| Entrez | 55244 |
Gene structure
Transcript identifiers
Ensembl transcripts: 16 — 8 protein_coding, 5 retained_intron, 3 protein_coding_CDS_not_defined
ENST00000270570, ENST00000395585, ENST00000436810, ENST00000495425, ENST00000497548, ENST00000571335, ENST00000573009, ENST00000574596, ENST00000575023, ENST00000575362, ENST00000575377, ENST00000576095, ENST00000581558, ENST00000584348, ENST00000901046, ENST00000943824
RefSeq mRNA: 1 — MANE Select: NM_018242
NM_018242
CCDS: CCDS11209
Canonical transcript exons
ENST00000270570 — 17 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001836672 | 19577327 | 19579034 |
| ENSE00002277438 | 19533854 | 19534074 |
| ENSE00003459042 | 19555593 | 19555690 |
| ENSE00003481665 | 19555995 | 19556062 |
| ENSE00003505639 | 19555212 | 19555309 |
| ENSE00003512581 | 19566790 | 19566859 |
| ENSE00003545175 | 19572780 | 19572861 |
| ENSE00003561496 | 19551424 | 19551468 |
| ENSE00003569548 | 19567096 | 19567228 |
| ENSE00003605240 | 19560418 | 19560493 |
| ENSE00003620413 | 19546435 | 19546503 |
| ENSE00003621711 | 19542393 | 19542494 |
| ENSE00003625114 | 19555796 | 19555909 |
| ENSE00003627735 | 19549635 | 19549677 |
| ENSE00003641639 | 19547985 | 19548133 |
| ENSE00003655212 | 19560188 | 19560296 |
| ENSE00003683381 | 19571478 | 19571572 |
Expression profiles
Bgee: expression breadth ubiquitous, 230 present calls, max score 98.25.
FANTOM5 (CAGE): breadth broad, TPM avg 3.5221 / max 203.7094, expressed in 862 samples.
FANTOM5 promoters (3 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 159848 | 3.2326 | 822 |
| 159849 | 0.2407 | 115 |
| 159847 | 0.0489 | 12 |
Top tissues by expression
276 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| right adrenal gland cortex | UBERON:0035827 | 98.25 | gold quality |
| nephron tubule | UBERON:0001231 | 97.73 | gold quality |
| right adrenal gland | UBERON:0001233 | 97.71 | gold quality |
| adrenal cortex | UBERON:0001235 | 97.67 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 97.50 | gold quality |
| left adrenal gland | UBERON:0001234 | 97.44 | gold quality |
| kidney epithelium | UBERON:0004819 | 96.97 | gold quality |
| adrenal gland | UBERON:0002369 | 96.42 | gold quality |
| renal glomerulus | UBERON:0000074 | 96.23 | gold quality |
| metanephric glomerulus | UBERON:0004736 | 95.93 | gold quality |
| right lobe of liver | UBERON:0001114 | 95.63 | gold quality |
| liver | UBERON:0002107 | 95.06 | gold quality |
| adult organism | UBERON:0007023 | 94.31 | gold quality |
| adult mammalian kidney | UBERON:0000082 | 93.41 | gold quality |
| adrenal tissue | UBERON:0018303 | 92.89 | gold quality |
| endocervix | UBERON:0000458 | 91.58 | gold quality |
| kidney | UBERON:0002113 | 91.49 | gold quality |
| gastrocnemius | UBERON:0001388 | 90.32 | gold quality |
| muscle of leg | UBERON:0001383 | 89.98 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 89.55 | gold quality |
| cortex of kidney | UBERON:0001225 | 89.35 | gold quality |
| upper leg skin | UBERON:0004262 | 88.99 | gold quality |
| muscle organ | UBERON:0001630 | 88.82 | gold quality |
| skeletal muscle organ | UBERON:0014892 | 88.82 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 88.20 | gold quality |
| metanephros | UBERON:0000081 | 88.09 | gold quality |
| vastus lateralis | UBERON:0001379 | 87.55 | gold quality |
| biceps brachii | UBERON:0001507 | 87.33 | gold quality |
| adenohypophysis | UBERON:0002196 | 86.63 | gold quality |
| quadriceps femoris | UBERON:0001377 | 86.21 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-CURD-119 | yes | 47.51 |
| E-ANND-3 | yes | 5.59 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): AP1, KLF12, NKX2-5, USF1
miRNA regulators (miRDB)
50 targeting SLC47A1, 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-4455 | 100.00 | 65.48 | 1587 |
| HSA-MIR-4533 | 100.00 | 69.48 | 2758 |
| HSA-MIR-552-5P | 99.93 | 68.56 | 1583 |
| HSA-MIR-6780A-5P | 99.88 | 66.69 | 2776 |
| HSA-MIR-4728-5P | 99.85 | 69.39 | 4718 |
| HSA-MIR-6785-5P | 99.82 | 68.68 | 4428 |
| HSA-MIR-4307 | 99.82 | 70.45 | 3374 |
| HSA-MIR-323A-3P | 99.79 | 70.30 | 1739 |
| HSA-MIR-1273H-5P | 99.77 | 66.32 | 2471 |
| HSA-MIR-149-3P | 99.72 | 68.22 | 3963 |
| HSA-MIR-12129 | 99.72 | 67.45 | 1311 |
| HSA-MIR-33A-3P | 99.70 | 70.27 | 3362 |
| HSA-MIR-30B-3P | 99.70 | 65.76 | 2325 |
| HSA-MIR-3689A-3P | 99.70 | 65.73 | 2306 |
| HSA-MIR-3689B-3P | 99.70 | 65.71 | 2311 |
| HSA-MIR-3689C | 99.70 | 65.71 | 2311 |
| HSA-MIR-6779-5P | 99.70 | 65.76 | 2363 |
| HSA-MIR-6883-5P | 99.69 | 68.05 | 3785 |
| HSA-MIR-10393-5P | 99.65 | 68.01 | 1368 |
| HSA-MIR-6512-3P | 99.65 | 66.07 | 1468 |
| HSA-MIR-6720-5P | 99.65 | 66.22 | 1459 |
| HSA-MIR-4666B | 99.64 | 68.69 | 1282 |
| HSA-MIR-4261 | 99.59 | 70.30 | 3415 |
| HSA-MIR-3942-3P | 99.57 | 69.03 | 2854 |
| HSA-MIR-6733-3P | 99.54 | 67.80 | 1281 |
| HSA-MIR-7106-5P | 99.53 | 67.47 | 3574 |
| HSA-MIR-4452 | 99.50 | 68.45 | 1493 |
| HSA-MIR-183-3P | 99.41 | 69.41 | 1598 |
| HSA-MIR-5690 | 99.25 | 67.58 | 1012 |
| HSA-MIR-6797-3P | 99.17 | 66.94 | 668 |
Literature-anchored findings (GeneRIF, showing 40)
- MATE1 appears to be the long searched for polyspecific organic cation exporter that directly transports toxic organic cations into urine and bile. (PMID:16330770)
- an oppositely directed H(+) gradient serves as a driving force of tetraethylammonium transport via rMATE1 (PMID:17047166)
- The results suggest that hOCT2 and hMATE1 mediate paraquat transport in the kidney. (PMID:17495125)
- hMATE1 and hMATE2-K function together as a detoxication system, by mediating the tubular secretion of intracellular ionic compounds across the brush-border membranes of the kidney. (PMID:17509534)
- Sp1 functions as basal transcriptional regulator of human and rat MATE1 gene through two GC boxes. May be conserved among species. We have identified rSNP of hMATE1 gene (G-32A) (belonging to Sp1-binding site) that affects promoter activity. (PMID:17855482)
- The molecular basis of substrate recognition by MATE1 was investigated via amino acid substitution in the conserved transmembrane regions. (PMID:18305230)
- These findings suggested that the loss of transport activities of the MATE1 G64D and MATE2-K G211V variants were due to the alteration of protein expression in cell surface membranes. (PMID:19158817)
- Genetic variants in multidrug and toxic compound extrusion-1, hMATE1, alter transport function. (PMID:19172157)
- Guanin/adenine single nucleotide polymorphism is associated with a reduction in A1C level suggesting it role in the pharmacokinetics of metformin in diabetics. (PMID:19228809)
- the rate of transcription of MATE1 is regulated by AP-1 and AP-2rep and that a common promoter variant, g.-66T>C may affect the expression level of MATE1 in human kidney, and ultimately result in variation in drug disposition and response. (PMID:19745787)
- interaction between polymorphisms and OCT1 polymorphisms on the glucose lowering effect of metformin (PMID:19898263)
- The purpose of this study was to evaluate the effects of heterozygous MATE variants on the disposition of metformin in mice and humans. (PMID:20016398)
- 4’,6-diamidino-2-phenylindole (DAPI) can be used as a probe substrate for rapid assays of the functionality of the human MATE1 (PMID:20047987)
- This study showed that coordinate function of MATE1 with OCT2 likely contributes to the vectorial renal elimination of organic cationic drugs and that altered activity of MATE1 should be considered as a determinant of renal cationic drug elimination. (PMID:20053795)
- characterization of MATE1: kinetic analysis of transport of cimetidine and tetraethylammonium; inhibitors; comparison to hMATE2-K and rMATE1 (PMID:20067714)
- The results suggest that agmatine disposition may be influenced by hOCT2 and hMATE1, two transporters critical in the renal elimination of xenobiotic compounds. (PMID:21128598)
- Homozygous MATE1 variant could be one of the risk factors for metformin-induced lactic acidosis. (PMID:22242910)
- The 808G>T single-nucleotide polymorphism in OCT2 ameliorated cisplatin-induced nephrotoxicity without alteration of disposition, whereas the rs2289669 G>A single-nucleotide polymorphism in MATE1 had no effect on cisplatin toxicity. (PMID:22569819)
- Twelve transmembrane helices form the functional core of mammalian MATE1 (multidrug and toxin extruder 1) protein. (PMID:22722930)
- Seven polymorphisms in OCT1, OCT2, and MATE1 genes were compared between 53 type 2 diabetes patients with side effects of metformin and 193 metformin users without symptoms of metformin intolerance. (PMID:22735389)
- Twenty percent of patients with diabetes that are homozygous for A-allele of SLC47A1 had twofold reduction in HbA1c in comparison with the patients carrying G-allele. (PMID:22882994)
- The effect of novel promoter variants in MATE1 … on the pharmacokinetics and pharmacodynamics of metformin (PMID:23267855)
- Decreasing expression of OCT3 and MATE1 in human placenta indicates these transporters may play a role in fetal protection preferentially at earlier stages of gestation. (PMID:23303678)
- The results confirmed that OAT1, OAT3, OCT2, MATE1, and MATE2-K were coexpressed in tubular epithelial cells. (PMID:23630107)
- ADMA and L-arginine are substrates of human CAT2A, CAT2B, OCT2 and MATE1. Transport kinetics of CAT2A, CAT2B, and OCT2 indicate a low affinity, high capacity transport, which may be relevant for renal and hepatic elimination of ADMA or L-arginine (PMID:23864433)
- MATE1 is a membrane transporter for quercetin.MATE1 was highly expressed in peroxisomes and the endoplasmic reticulum as well as in plasma membranes in the liver and intestine. (PMID:25241911)
- Disease progression according to RECIST was also more frequent in carriers of at least one polymorphic MATE1 A-allele (44%) as compared with homozygous carriers of the wild-type G-allele (12.5%) (P=0.07). OCT1 and MATE1 were not associated with PFS. (PMID:25753371)
- MRNA levels of multidrug and toxin extrusion protein 1 (MATE1 or SLC47A1, encoded by 1 of the 11 genes) were significantly lower in patients with FILI. (PMID:25862351)
- SLC47A1 rs2289669 G>A variants improve the glucose-lowering effect of metformin through slowing its excretion in type 2 diabetes populations. (PMID:26004431)
- MATE1 sequesters organic cations within an intracellular compartment that has no influence on secretion in renal proximal tubules. (PMID:26538438)
- MATE1 rs2289669 may be a significant determinant in the renal clearance of metformin in the case of transporter-mediated drug interactions (PMID:26784938)
- MATE1 mRNA levels in peripheral blood cells were significantly higher in patients carrying the minor allele of rs2453579, but not rs2252281, compared to those with other genotypes (PMID:27025966)
- Pazopanib inhibits OCT2, MATE1 and MATE2-K, which are involved in cisplatin secretion into urine, potentiating cisplatin toxicity. (PMID:27178732)
- This study did not identify any of these known SLC47A1 coding SNPs in the Xhosa individuals who participated in this study. (PMID:27226103)
- The impact of assay conditions on IC50 determination is negligible, kinetic characteristics differ among used test substrates, and substrate-dependent inhibition exists for MATE1 and MATE2-K, giving valuable insight into the assessment of clinically relevant MATE-mediated drug interactions in vitro. (PMID:27271370)
- substrate identity exerts comparatively little influence on ligand interaction with MATE1. (PMID:27418674)
- MATE1 polymorphisms were associated with hematological toxicity in non-small cell lung cancer patients. (PMID:27590272)
- MATE1 is the major transporter for the cellular uptake of imatinib and crucial for the therapeutic success in CML patients. We suggest that the detailed analysis of MATE1 expression levels and mutations could be a predictor for the response to imatinib therapy. (PMID:27635733)
- genetic association studies in population in China: Data confirm that an SNP in an intron of SLC47A1 (rs2289669) is associated with hypoglycemic response to metformin in patients with newly diagnosed type 2 diabetes; differential increases in basal GLP1 plasma levels are also related to this SNP. (SLC47A1 = solute carrier family 47 member 1; GLP1 = glucagon-like peptide-1) (PMID:28321905)
- The combination of ENT1, MATE1 and OCT2 SNPs may serve as a predictive and prognostic marker in metastatic colorectal carcinoma patients treated with TAS-102. (PMID:28992563)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | slc47a1 | ENSDARG00000046012 |
| danio_rerio | slc47a4 | ENSDARG00000079340 |
| mus_musculus | Slc47a1 | ENSMUSG00000010122 |
| rattus_norvegicus | Slc47a1 | ENSRNOG00000057404 |
Paralogs (1): SLC47A2 (ENSG00000180638)
Protein
Protein identifiers
Multidrug and toxin extrusion protein 1 — Q96FL8 (reviewed: Q96FL8)
Alternative names: Solute carrier family 47 member 1
All UniProt accessions (5): Q96FL8, E7EX57, I3L345, J3KRZ3, J3KSS8
UniProt curated annotations — full annotation on UniProt →
Function. Multidrug efflux pump that functions as a H(+)/organic cation antiporter. Plays a physiological role in the excretion of cationic compounds including endogenous metabolites, drugs, toxins through the kidney and liver, into urine and bile respectively. Mediates the efflux of endogenous compounds such as creatinine, vitamin B1/thiamine, agmatine and estrone-3-sulfate. May also contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier.
Subcellular location. Cell membrane. Apical cell membrane.
Tissue specificity. Widely expressed. The highest expression is found in adrenal gland, and to a lower extent in liver, skeletal muscle and kidney. In testis, primarily localized throughout the adluminal compartment of the seminiferous tubules with expression at the peritubular myoid cells and Leydig cells.
Miscellaneous. Mediates the efflux of cationic compounds such as the model cations, tetraethylammonium (TEA), the neurotoxin 1-methyl-4-phenylpyridinium (MPP), the platinum-based drugs cisplatin and oxaliplatin, the drugs procainamide, acyclovir and topotecan, or weak bases that are positively charged at physiological pH, such as cimetidine or the antidiabetic drug metformin.
Similarity. Belongs to the multi antimicrobial extrusion (MATE) (TC 2.A.66.1) family.
Isoforms (3)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q96FL8-1 | 1 | yes |
| Q96FL8-2 | 2 | |
| Q96FL8-3 | 3 |
RefSeq proteins (1): NP_060712* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR002528 | MATE_fam | Family |
| IPR045069 | MATE_euk | Family |
Pfam: PF01554
Catalyzed reactions (Rhea), 4 shown:
- thiamine(out) + H(+)(in) = thiamine(in) + H(+)(out) (RHEA:71271)
- agmatine(in) + H(+)(out) = agmatine(out) + H(+)(in) (RHEA:72127)
- estrone 3-sulfate(in) + H(+)(out) = estrone 3-sulfate(out) + H(+)(in) (RHEA:72139)
- creatinine(in) + H(+)(out) = creatinine(out) + H(+)(in) (RHEA:72183)
UniProt features (52 total): topological domain 14, transmembrane region 13, mutagenesis site 8, sequence variant 6, sequence conflict 4, splice variant 3, chain 1, region of interest 1, compositionally biased region 1, modified residue 1
Structure
Experimental structures (PDB)
4 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 9R1F | ELECTRON MICROSCOPY | 2.31 |
| 9R1G | ELECTRON MICROSCOPY | 2.95 |
| 9R1E | ELECTRON MICROSCOPY | 3.2 |
| 9R10 | ELECTRON MICROSCOPY | 3.3 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q96FL8-F1 | 85.87 | 0.77 |
Antibody-complex structures (SAbDab): 4 — 9R10, 9R1E, 9R1F, 9R1G
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Post-translational modifications (1): 1
Mutagenesis-validated functional residues (8):
| Position | Phenotype |
|---|---|
| 273 | abolishes membrane subcellular location. abolishes tea transport. |
| 273 | does not affect membrane subcellular location. decreases tea transport. higher affinity for cimetidine and reduced affin |
| 273 | no change in subcellular location and abolition of mate1-dependent tea transport activity. |
| 278 | does not affect membrane subcellular location. abolishes tea transport. |
| 278 | does not affect membrane subcellular location. decreases tea transport. |
| 299 | decreased tea and metformin uptake. |
| 300 | does not affect membrane subcellular location. decreases tea transport. |
| 389 | does not affect membrane subcellular location. decreases tea transport. |
Function
Pathways and Gene Ontology
Reactome pathways
4 pathways
| ID | Pathway |
|---|---|
| R-HSA-549127 | SLC-mediated transport of organic cations |
| R-HSA-425366 | |
| R-HSA-382551 | Transport of small molecules |
| R-HSA-425407 | SLC-mediated transmembrane transport |
MSigDB gene sets: 161 (showing top):
GSE37336_LY6C_POS_VS_NEG_NAIVE_CD4_TCELL_UP, CLAUS_PGR_POSITIVE_MENINGIOMA_UP, GOBP_XENOBIOTIC_TRANSMEMBRANE_TRANSPORT, GOBP_AMINO_ACID_TRANSMEMBRANE_TRANSPORT, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_ORGANIC_ACID_TRANSPORT, MODULE_205, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM4, GOBP_AMINO_ACID_TRANSPORT, GOBP_BASIC_AMINO_ACID_TRANSPORT, GOBP_DETOXIFICATION, GOBP_ORGANIC_ANION_TRANSPORT, GOBP_SULFUR_COMPOUND_TRANSPORT, GOMF_PROTON_TRANSMEMBRANE_TRANSPORTER_ACTIVITY, GOBP_VITAMIN_TRANSPORT
GO Biological Process (13): xenobiotic transmembrane transport (GO:0006855), obsolete organic cation transport (GO:0015695), putrescine transport (GO:0015847), xenobiotic transport (GO:0042908), transmembrane transport (GO:0055085), amino acid import across plasma membrane (GO:0089718), L-arginine import across plasma membrane (GO:0097638), L-alpha-amino acid transmembrane transport (GO:1902475), xenobiotic detoxification by transmembrane export across the plasma membrane (GO:1990961), thiamine transmembrane transport (GO:0071934), monoatomic cation transmembrane transport (GO:0098655), proton transmembrane transport (GO:1902600), L-arginine transmembrane transport (GO:1903826)
GO Molecular Function (10): obsolete organic cation transmembrane transporter activity (GO:0015101), L-amino acid transmembrane transporter activity (GO:0015179), thiamine transmembrane transporter activity (GO:0015234), antiporter activity (GO:0015297), putrescine transmembrane transporter activity (GO:0015489), transmembrane transporter activity (GO:0022857), xenobiotic transmembrane transporter activity (GO:0042910), L-arginine transmembrane transporter activity (GO:0061459), polyspecific organic cation:proton antiporter activity (GO:0140968), protein binding (GO:0005515)
GO Cellular Component (4): plasma membrane (GO:0005886), membrane (GO:0016020), basolateral plasma membrane (GO:0016323), apical plasma membrane (GO:0016324)
Reactome top-level categories
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| SLC-mediated transmembrane transport | 1 |
| Transport of small molecules | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| xenobiotic transport | 2 |
| transmembrane transport | 2 |
| transport | 2 |
| amino acid transmembrane transport | 2 |
| L-arginine transmembrane transport | 2 |
| L-alpha-amino acid transmembrane transport | 2 |
| plasma membrane region | 2 |
| polyamine transport | 1 |
| cellular process | 1 |
| import across plasma membrane | 1 |
| amino acid import across plasma membrane | 1 |
| L-amino acid transport | 1 |
| carboxylic acid transmembrane transport | 1 |
| xenobiotic export from cell | 1 |
| detoxification | 1 |
| export across plasma membrane | 1 |
| thiamine transport | 1 |
| vitamin transmembrane transport | 1 |
| azole transmembrane transport | 1 |
| pyrimidine-containing compound transmembrane transport | 1 |
| monoatomic cation transport | 1 |
| monoatomic ion transmembrane transport | 1 |
| monoatomic cation transmembrane transport | 1 |
| basic amino acid transmembrane transport | 1 |
| amino acid transmembrane transporter activity | 1 |
| carboxylic acid transmembrane transporter activity | 1 |
| thiamine transmembrane transport | 1 |
| vitamin transmembrane transporter activity | 1 |
| azole transmembrane transporter activity | 1 |
| sulfur compound transmembrane transporter activity | 1 |
| secondary active transmembrane transporter activity | 1 |
| polyamine transmembrane transporter activity | 1 |
| putrescine transport | 1 |
| transporter activity | 1 |
| transmembrane transporter activity | 1 |
| basic amino acid transmembrane transporter activity | 1 |
| L-amino acid transmembrane transporter activity | 1 |
| proton transmembrane transporter activity | 1 |
| antiporter activity | 1 |
| binding | 1 |
Protein interactions and networks
STRING
1598 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| SLC47A1 | SLC22A2 | O15244 | 888 |
| SLC47A1 | SLC22A1 | O15245 | 856 |
| SLC47A1 | SLC22A8 | Q8TCC7 | 802 |
| SLC47A1 | SLCO1B3 | Q9NPD5 | 763 |
| SLC47A1 | SLCO1B1 | Q9Y6L6 | 760 |
| SLC47A1 | SLC22A9 | Q8IVM8 | 760 |
| SLC47A1 | SLC22A11 | Q9NSA0 | 750 |
| SLC47A1 | SLCO2B1 | O94956 | 741 |
| SLC47A1 | SLC22A4 | Q9H015 | 734 |
| SLC47A1 | SLC22A6 | Q4U2R8 | 733 |
| SLC47A1 | SLC29A4 | Q7RTT9 | 729 |
| SLC47A1 | SLC22A7 | Q9Y694 | 729 |
| SLC47A1 | SLC22A3 | O75751 | 716 |
| SLC47A1 | ABCG2 | Q9UNQ0 | 715 |
| SLC47A1 | SLCO4C1 | Q6ZQN7 | 703 |
IntAct
39 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| SLC47A1 | FXYD6 | psi-mi:“MI:0915”(physical association) | 0.560 |
| GPR21 | TMEM120B | psi-mi:“MI:0914”(association) | 0.530 |
| SLC39A4 | TMEM120B | psi-mi:“MI:0914”(association) | 0.530 |
| LYPD6 | PLXNB2 | psi-mi:“MI:0914”(association) | 0.530 |
| TMPRSS12 | FZD6 | psi-mi:“MI:0914”(association) | 0.530 |
| CHRND | TPST2 | psi-mi:“MI:0914”(association) | 0.530 |
| GABRA3 | HLA-C | psi-mi:“MI:0914”(association) | 0.530 |
| SLC47A1 | DES | psi-mi:“MI:0915”(physical association) | 0.400 |
| TTYH1 | TMEM223 | psi-mi:“MI:0914”(association) | 0.350 |
| TSPAN15 | TMEM223 | psi-mi:“MI:0914”(association) | 0.350 |
| TNFSF18 | TMEM120B | psi-mi:“MI:0914”(association) | 0.350 |
| LRRC55 | TMEM120B | psi-mi:“MI:0914”(association) | 0.350 |
| TNFRSF10C | SLC22A23 | psi-mi:“MI:0914”(association) | 0.350 |
| ZACN | FAM234B | psi-mi:“MI:0914”(association) | 0.350 |
| SLC47A1 | FAM234B | psi-mi:“MI:0914”(association) | 0.350 |
| TCTN2 | TMEM131L | psi-mi:“MI:0914”(association) | 0.350 |
| LLCFC1 | POTEF | psi-mi:“MI:0914”(association) | 0.350 |
| KLRC4 | RAP1BL | psi-mi:“MI:0914”(association) | 0.350 |
| KLRC1 | METTL15 | psi-mi:“MI:0914”(association) | 0.350 |
| PTH2R | METTL15 | psi-mi:“MI:0914”(association) | 0.350 |
| SLC39A12 | psi-mi:“MI:0914”(association) | 0.350 | |
| NKAIN1 | GPR89A | psi-mi:“MI:0914”(association) | 0.350 |
| KIR2DL4 | GPR89A | psi-mi:“MI:0914”(association) | 0.350 |
| HTR3C | GET1 | psi-mi:“MI:0914”(association) | 0.350 |
| SLC17A2 | ABCD4 | psi-mi:“MI:0914”(association) | 0.350 |
| KLRC2 | CLGN | psi-mi:“MI:0914”(association) | 0.350 |
| CD3D | CLGN | psi-mi:“MI:0914”(association) | 0.350 |
| KLRC3 | RNF13 | psi-mi:“MI:0914”(association) | 0.350 |
| HTR3A | EXTL3 | psi-mi:“MI:0914”(association) | 0.350 |
| SLC22A2 | FADS1 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (116): SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS), SLC47A1 (Affinity Capture-MS)
ESM2 similar proteins: A1L1P9, A4IIS8, A7KAU2, A7KAU3, A8I499, B3TP03, B5D5N9, F4J158, F4JH46, F4KBM7, H9BZ66, O49660, O64759, P18581, P30823, P30825, P31637, P38142, P38767, P52569, P53793, P53794, Q05360, Q09143, Q10917, Q16928, Q17320, Q22397, Q27256, Q2UVJ5, Q3EAQ5, Q3V050, Q5I0E9, Q5PR34, Q5R7E4, Q5RFD2, Q66KG0, Q84MA5, Q86VL8, Q8K0H1
Diamond homologs: A1L1P9, A4IIS8, A7KAU2, A7KAU3, F4IHU9, O80695, Q10085, Q3V050, Q4PSF4, Q5I0E9, Q5R7E4, Q5RFD2, Q86VL8, Q8K0H1, Q8L731, Q94AL1, Q96FL8, Q9C9M8, Q9FH21, Q9FHB6, Q9LE20, Q9LUH2, Q9LUH3, Q9LVD9, Q9LYT3, Q9SZE2, Q9USK3, Q9UT92, Q9ZVH5, F4HQ05, O49660, O82752, Q9C994, Q9FJ87, Q9SIA5, F4HZH9, F4JH46, F4JKB9, Q05497, Q1PFG9
SIGNOR signaling
0 interactions.
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 59 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.
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| positive regulation of natural killer cell mediated cytotoxicity | 5 | 51.1× | 1e-05 |
| monoatomic ion transmembrane transport | 5 | 18.9× | 6e-04 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
96 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 71 |
| Likely benign | 7 |
| Benign | 3 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
2921 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 17:19534072:GCG:G | donor_gain | 1.0000 |
| 17:19534075:G:GG | donor_gain | 1.0000 |
| 17:19534079:G:GG | donor_gain | 1.0000 |
| 17:19542391:A:AG | acceptor_gain | 1.0000 |
| 17:19542392:G:GA | acceptor_gain | 1.0000 |
| 17:19542392:GTT:G | acceptor_gain | 1.0000 |
| 17:19542392:GTTC:G | acceptor_gain | 1.0000 |
| 17:19542492:GCG:G | donor_gain | 1.0000 |
| 17:19542494:GGTA:G | donor_loss | 1.0000 |
| 17:19542495:G:GA | donor_loss | 1.0000 |
| 17:19542495:G:GG | donor_gain | 1.0000 |
| 17:19542496:T:TC | donor_loss | 1.0000 |
| 17:19547973:T:TA | acceptor_gain | 1.0000 |
| 17:19547975:T:TA | acceptor_gain | 1.0000 |
| 17:19547978:A:AG | acceptor_gain | 1.0000 |
| 17:19547979:C:G | acceptor_gain | 1.0000 |
| 17:19547983:A:AG | acceptor_gain | 1.0000 |
| 17:19547984:G:GG | acceptor_gain | 1.0000 |
| 17:19547984:GAC:G | acceptor_gain | 1.0000 |
| 17:19548130:CCAGG:C | donor_loss | 1.0000 |
| 17:19548134:G:T | donor_loss | 1.0000 |
| 17:19548135:T:G | donor_loss | 1.0000 |
| 17:19534073:CGG:C | donor_loss | 0.9900 |
| 17:19534074:GGT:G | donor_loss | 0.9900 |
| 17:19534075:G:GA | donor_loss | 0.9900 |
| 17:19534078:AGT:A | donor_loss | 0.9900 |
| 17:19542388:CCCA:C | acceptor_loss | 0.9900 |
| 17:19542389:CCA:C | acceptor_loss | 0.9900 |
| 17:19542390:CA:C | acceptor_loss | 0.9900 |
| 17:19542392:GT:G | acceptor_gain | 0.9900 |
AlphaMissense
3662 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 17:19542432:A:C | S59R | 0.994 |
| 17:19542434:C:A | S59R | 0.994 |
| 17:19542434:C:G | S59R | 0.994 |
| 17:19555852:A:C | S266R | 0.990 |
| 17:19555854:C:A | S266R | 0.990 |
| 17:19555854:C:G | S266R | 0.990 |
| 17:19555879:T:A | W275R | 0.989 |
| 17:19555879:T:C | W275R | 0.989 |
| 17:19542486:G:C | A77P | 0.988 |
| 17:19542487:C:A | A77E | 0.985 |
| 17:19546469:G:A | G91D | 0.985 |
| 17:19560480:T:C | F365L | 0.985 |
| 17:19560482:T:A | F365L | 0.985 |
| 17:19560482:T:G | F365L | 0.985 |
| 17:19555906:A:C | S284R | 0.983 |
| 17:19555908:T:A | S284R | 0.983 |
| 17:19555908:T:G | S284R | 0.983 |
| 17:19571483:T:A | W439R | 0.983 |
| 17:19571483:T:C | W439R | 0.983 |
| 17:19571554:G:C | W462C | 0.983 |
| 17:19571554:G:T | W462C | 0.983 |
| 17:19542474:G:C | A73P | 0.982 |
| 17:19546468:G:C | G91R | 0.982 |
| 17:19560233:G:C | A323P | 0.981 |
| 17:19546462:G:A | G89R | 0.980 |
| 17:19546462:G:C | G89R | 0.980 |
| 17:19567120:G:T | G401W | 0.979 |
| 17:19542448:G:A | G64D | 0.978 |
| 17:19546450:G:C | G85R | 0.977 |
| 17:19542484:T:C | L76P | 0.976 |
dbSNP variants (sampled 300 via entrez): RS1000015147 (17:19547264 G>A), RS1000017537 (17:19546063 T>C), RS1000100362 (17:19535018 G>C), RS1000156855 (17:19554417 C>T), RS1000211065 (17:19559227 A>T), RS1000228758 (17:19578325 C>T), RS1000272096 (17:19569043 C>T), RS1000282941 (17:19541323 T>C,G), RS1000290188 (17:19571779 G>A), RS1000317767 (17:19559789 T>C), RS1000329613 (17:19576019 G>T), RS1000370241 (17:19534983 G>A,C), RS1000402339 (17:19541855 A>C), RS1000475375 (17:19565409 C>T), RS1000492018 (17:19570848 G>C)
Disease associations
OMIM: gene MIM:609832 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
20 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST003372_57 | Glomerular filtration rate (creatinine) | 3.000000e-11 |
| GCST003401_24 | Glomerular filtration rate in non diabetics (creatinine) | 3.000000e-13 |
| GCST004292_34 | Glomerular filtration rate (creatinine) | 5.000000e-12 |
| GCST004627_170 | Lymphocyte count | 6.000000e-09 |
| GCST007344_5 | Estimated glomerular filtration rate | 5.000000e-11 |
| GCST007354_19 | Intracranial aneurysm | 1.000000e-08 |
| GCST007876_139 | Estimated glomerular filtration rate | 3.000000e-21 |
| GCST007877_18 | Creatinine levels | 1.000000e-08 |
| GCST008058_161 | Estimated glomerular filtration rate | 1.000000e-45 |
| GCST008059_124 | Estimated glomerular filtration rate | 5.000000e-40 |
| GCST008064_7 | Chronic kidney disease | 3.000000e-07 |
| GCST008745_18 | Estimated glomerular filtration rate in non-diabetics | 5.000000e-14 |
| GCST008747_154 | Estimated glomerular filtration rate | 5.000000e-25 |
| GCST008747_85 | Estimated glomerular filtration rate | 3.000000e-28 |
| GCST008971_58 | Urate levels | 7.000000e-10 |
| GCST008972_31 | Urate levels | 3.000000e-10 |
| GCST90002388_491 | Lymphocyte count | 1.000000e-15 |
| GCST90002389_224 | Lymphocyte percentage of white cells | 4.000000e-12 |
| GCST90002399_284 | Neutrophil percentage of white cells | 6.000000e-11 |
| GCST90002404_350 | Red cell distribution width | 7.000000e-12 |
EFO canonical traits (5, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004587 | lymphocyte count |
| EFO:0004531 | urate measurement |
| EFO:0007993 | lymphocyte percentage of leukocytes |
| EFO:0007990 | neutrophil percentage of leukocytes |
| EFO:0009188 | Red cell distribution width |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL1743126 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
47 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 578,889 (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 |
|---|---|---|---|
| CHEMBL1017 | TELMISARTAN | 4 | 27,457 |
| CHEMBL11 | IMIPRAMINE | 4 | 48,893 |
| CHEMBL1106 | EPINASTINE | 4 | 8,530 |
| CHEMBL1200629 | VECURONIUM BROMIDE | 4 | 5,399 |
| CHEMBL128 | SUMATRIPTAN | 4 | 28,367 |
| CHEMBL1294 | QUINIDINE | 4 | 71,943 |
| CHEMBL134 | CLONIDINE | 4 | 97,993 |
| CHEMBL1393 | SPIRONOLACTONE | 4 | 49,171 |
| CHEMBL1502 | PANTOPRAZOLE | 4 | 14,689 |
| CHEMBL163 | RITONAVIR | 4 | 53,773 |
| CHEMBL1732 | DIHYDROERGOTAMINE | 4 | 12,897 |
| CHEMBL1790041 | RANITIDINE | 4 | 30,599 |
| CHEMBL2 | PRAZOSIN | 4 | 31,107 |
| CHEMBL219916 | DOMPERIDONE | 4 | 18,305 |
| CHEMBL256907 | MARAVIROC | 4 | 5 |
| CHEMBL289469 | GRANISETRON | 4 | 431 |
| CHEMBL290106 | BITHIONOL | 4 | 6,439 |
| CHEMBL296419 | ASTEMIZOLE | 4 | 21,577 |
| CHEMBL30 | CIMETIDINE | 4 | 47,191 |
| CHEMBL339427 | TUBOCURARINE | 4 | 4,123 |
| CHEMBL364713 | NOSCAPINE | 4 | |
| CHEMBL46 | ONDANSETRON | 4 | |
| CHEMBL481 | IRINOTECAN | 4 | |
| CHEMBL49 | BUSPIRONE | 4 | |
| CHEMBL517 | DISOPYRAMIDE | 4 | |
| CHEMBL5315124 | LEVOFLOXACIN | 4 | |
| CHEMBL55 | PENTAMIDINE | 4 | |
| CHEMBL58 | MITOXANTRONE | 4 | |
| CHEMBL603 | ZAFIRLUKAST | 4 | |
| CHEMBL660 | AMANTADINE | 4 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB clinical annotations
2 annotations.
| Variant | Type | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| rs2252281 | Efficacy | 3 | metformin | Diabetes Mellitus;Type 2;Polycystic Ovary Syndrome |
| rs2289669 | Efficacy | 3 | metformin | Diabetes Mellitus;Type 2;Polycystic Ovary Syndrome |
PharmGKB variants
3 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs2252281 | SLC47A1 | 3 | 3.50 | 1 | metformin |
| rs2289669 | SLC47A1, SNORA59B | 3 | 4.00 | 1 | metformin |
| rs8065082 | SLC47A1 | 0.00 | 0 |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: transporter — SLC47 family of multidrug and toxin extrusion transporters
Most potent curated ligand interactions (2 total), top 2:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| pyrimethamine | Inhibition | 7.1 | pKi |
| cimetidine | Inhibition | 6.0 | pKi |
ChEMBL bioactivities
54 potent at pChembl≥5 of 70 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 7.52 | IC50 | 30 | nM | ONDANSETRON |
| 7.40 | IC50 | 40 | nM | IMATINIB |
| 7.30 | IC50 | 50 | nM | IMATINIB |
| 7.10 | IC50 | 80 | nM | RITONAVIR |
| 6.82 | IC50 | 150 | nM | ONDANSETRON |
| 6.80 | IC50 | 160 | nM | ONDANSETRON |
| 6.72 | IC50 | 190 | nM | MITOXANTRONE |
| 6.46 | IC50 | 350 | nM | IMATINIB |
| 6.40 | IC50 | 400 | nM | MITOXANTRONE |
| 6.39 | IC50 | 410 | nM | PENTAMIDINE |
| 6.30 | IC50 | 500 | nM | GABEXATE |
| 6.28 | IC50 | 530 | nM | MITOXANTRONE |
| 6.19 | IC50 | 650 | nM | NIFEKALANT |
| 6.16 | IC50 | 700 | nM | CHLORHEXIDINE |
| 6.12 | IC50 | 760 | nM | FAMOTIDINE |
| 5.96 | IC50 | 1100 | nM | TACRINE |
| 5.96 | IC50 | 1100 | nM | NIFEKALANT |
| 5.96 | IC50 | 1100 | nM | EPINASTINE |
| 5.92 | IC50 | 1200 | nM | CIMETIDINE |
| 5.89 | IC50 | 1300 | nM | TOPOTECAN |
| 5.89 | IC50 | 1300 | nM | ZAFIRLUKAST |
| 5.80 | IC50 | 1600 | nM | RISPERIDONE |
| 5.80 | IC50 | 1600 | nM | PRAZOSIN |
| 5.77 | IC50 | 1700 | nM | INDINAVIR |
| 5.77 | IC50 | 1700 | nM | BUSPIRONE |
| 5.72 | IC50 | 1900 | nM | INDINAVIR |
| 5.72 | IC50 | 1900 | nM | VECURONIUM BROMIDE |
| 5.70 | IC50 | 2000 | nM | PENTAMIDINE |
| 5.70 | IC50 | 2000 | nM | CHEMBL5194558 |
| 5.68 | IC50 | 2100 | nM | RITONAVIR |
| 5.68 | IC50 | 2100 | nM | IRINOTECAN |
| 5.66 | IC50 | 2200 | nM | CIMETIDINE |
| 5.64 | IC50 | 2300 | nM | DOMPERIDONE |
| 5.57 | IC50 | 2700 | nM | PENTAMIDINE |
| 5.57 | IC50 | 2700 | nM | CHEMBL5563848 |
| 5.55 | IC50 | 2800 | nM | PANTOPRAZOLE |
| 5.55 | IC50 | 2800 | nM | DIHYDROERGOTAMINE |
| 5.54 | IC50 | 2900 | nM | CAMOSTAT |
| 5.37 | IC50 | 4300 | nM | IRINOTECAN |
| 5.36 | IC50 | 4400 | nM | RITONAVIR |
| 5.30 | IC50 | 5000 | nM | GRANISETRON |
| 5.28 | IC50 | 5200 | nM | BITHIONOL |
| 5.24 | IC50 | 5700 | nM | CIMETIDINE |
| 5.19 | IC50 | 6500 | nM | NIFEKALANT |
| 5.17 | IC50 | 6700 | nM | SUMATRIPTAN |
| 5.14 | IC50 | 7300 | nM | RIMANTADINE |
| 5.11 | IC50 | 7800 | nM | INDINAVIR |
| 5.10 | IC50 | 7900 | nM | IRINOTECAN |
| 5.09 | IC50 | 8100 | nM | DABIGATRAN |
| 5.08 | IC50 | 8300 | nM | RANITIDINE |
PubChem BioAssay actives
55 with measured affinity, of 149 total; 35 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 |
|---|---|---|---|---|
| Ondansetron | 721746: Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | ic50 | 0.0100 | uM |
| Imatinib | 721746: Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | ic50 | 0.0400 | uM |
| Ritonavir | 721747: Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis | ic50 | 0.0800 | uM |
| Mitoxantrone | 721746: Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | ic50 | 0.1900 | uM |
| Pentamidine | 721746: Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | ic50 | 0.4100 | uM |
| ethyl 4-[6-(diaminomethylideneamino)hexanoyloxy]benzoate | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 0.5000 | uM |
| 6-[2-[2-hydroxyethyl-[3-(4-nitrophenyl)propyl]amino]ethylamino]-1,3-dimethylpyrimidine-2,4-dione | 721746: Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | ic50 | 0.6500 | uM |
| Chlorhexidine | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 0.7000 | uM |
| Famotidine | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 0.7600 | uM |
| 1,2,3,4-tetrahydroacridin-9-amine | 692195: Inhibition of human MATE1 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay | ic50 | 1.1000 | uM |
| Epinastine | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 1.1000 | uM |
| Cimetidine | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 1.2000 | uM |
| Zafirlukast | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 1.3000 | uM |
| Topotecan | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 1.3000 | uM |
| Prazosin | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 1.6000 | uM |
| Risperidone | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 1.6000 | uM |
| Buspirone | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 1.7000 | uM |
| (2S)-1-[(2S,4R)-4-benzyl-2-hydroxy-5-[[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-5-oxopentyl]-N-tert-butyl-4-(pyridin-3-ylmethyl)piperazine-2-carboxamide;hydrate | 721747: Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis | ic50 | 1.7000 | uM |
| Vecuronium Bromide | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 1.9000 | uM |
| N-[2-[(5-methyl-1H-imidazol-4-yl)methylsulfanyl]ethyl]pyrimidin-2-amine | 1848080: Inhibition of human MATE1 | ic50 | 2.0000 | uM |
| Irinotecan | 721747: Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis | ic50 | 2.1000 | uM |
| Domperidone | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 2.3000 | uM |
| 4-methyl-6-[4-[[(3S,5R)-3-methyl-5-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)piperazin-1-yl]methyl]triazol-2-yl]pyridine-3-carbonitrile | 2077521: Inhibition of MATE1 (unknown origin) | ic50 | 2.7000 | uM |
| Dihydroergotamine | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 2.8000 | uM |
| Pantoprazole | 721746: Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | ic50 | 2.8000 | uM |
| [4-[2-[2-(dimethylamino)-2-oxoethoxy]-2-oxoethyl]phenyl] 4-(diaminomethylideneamino)benzoate | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 2.9000 | uM |
| 1-methyl-N-(9-methyl-9-azabicyclo[3.3.1]nonan-3-yl)indazole-3-carboxamide | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 5.0000 | uM |
| 2,4-dichloro-6-(3,5-dichloro-2-hydroxyphenyl)sulfanylphenol | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 5.2000 | uM |
| Sumatriptan | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 6.7000 | uM |
| Rimantadine | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 7.3000 | uM |
| Dabigatran | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 8.1000 | uM |
| 1-N’-[2-[[5-[(dimethylamino)methyl]furan-2-yl]methylsulfanyl]ethyl]-1-N-methyl-2-nitroethene-1,1-diamine | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 8.3000 | uM |
| Tubocurarine | 721754: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | ic50 | 9.4000 | uM |
| (1S,2S)-6-(5-ethylsulfonyl-1,3-benzoxazol-2-yl)-1,2-dihydronaphthalene-1,2-diol | 1580335: Inhibition of MATE1 (unknown origin) | ic50 | 10.0000 | uM |
| Imipramine | 692195: Inhibition of human MATE1 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay | ic50 | 10.0000 | uM |
CTD chemical–gene interactions
113 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Tetraethylammonium | increases import, affects uptake, decreases reaction, increases uptake, affects transport (+1 more) | 7 |
| Estradiol | affects cotreatment, decreases expression, increases expression | 5 |
| Metformin | decreases reaction, increases uptake, decreases uptake | 5 |
| Paraquat | decreases reaction, increases uptake, increases expression, affects uptake, decreases uptake (+1 more) | 4 |
| Valproic Acid | affects expression, affects cotreatment, increases expression | 4 |
| Verapamil | decreases reaction, increases import, increases uptake, decreases activity | 4 |
| Benzo(a)pyrene | affects methylation, decreases expression, increases methylation | 3 |
| Cimetidine | affects transport, decreases reaction, increases uptake, decreases activity | 3 |
| Aflatoxin B1 | affects expression, decreases expression, increases methylation | 3 |
| bisphenol A | affects cotreatment, increases methylation, decreases reaction, increases uptake, decreases activity (+1 more) | 2 |
| tetrabutylammonium | decreases reaction, increases uptake, affects uptake | 2 |
| tetramethylammonium | affects reaction, increases uptake, affects uptake, decreases reaction | 2 |
| tetrapropylammonium | affects uptake, decreases reaction, increases uptake | 2 |
| entinostat | affects cotreatment, increases expression | 2 |
| Oxaliplatin | decreases uptake, increases uptake | 2 |
| Amiloride | decreases activity, decreases reaction, increases uptake | 2 |
| Imipramine | decreases reaction, increases uptake, decreases activity | 2 |
| Progesterone | affects cotreatment, decreases expression, increases expression | 2 |
| Pyrimethamine | decreases reaction, increases uptake, decreases activity | 2 |
| Quinidine | decreases activity, decreases reaction, increases uptake | 2 |
| Tacrine | increases uptake, decreases reaction | 2 |
| Tobacco Smoke Pollution | decreases reaction, increases import, decreases expression | 2 |
| 1-Methyl-4-phenylpyridinium | decreases reaction, increases uptake, decreases activity, affects reaction | 2 |
| Cyclosporine | decreases expression | 2 |
| Ondansetron | decreases reaction, increases uptake | 2 |
| bisphenol F | decreases reaction, increases uptake | 1 |
| ethohexadiol | affects reaction, increases uptake | 1 |
| methyleugenol | decreases expression | 1 |
| nuciferine | decreases reaction, increases uptake | 1 |
| cinchonine | decreases reaction, increases uptake | 1 |
ChEMBL screening assays
21 unique, capped per target: 16 binding, 4 admet, 1 toxicity
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1743155 | ADMET | Substrates of transporters of clinical importance in the absorption and disposition of drugs, MATE1 | Membrane transporters in drug development. — Nat Rev Drug Discov |
| CHEMBL2320298 | Binding | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. — J Med Chem |
| CHEMBL5099091 | Toxicity | Inhibition of human MATE1 | Fluorophenylalkyl-substituted cyanoguanidine derivatives as bacteria-selective MATE transporter inhibitors for the treatment of antibiotic-resistant infections. — Bioorg Med Chem |
Cellosaurus cell lines
7 cell lines: 4 cancer cell line, 2 transformed cell line, 1 induced pluripotent stem cell
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B6AD | HepaRG MATE1 KO | Cancer cell line | Female |
| CVCL_B6AV | SA7K MATE1 KO | Transformed cell line | Female |
| CVCL_B6AW | SA7K MATE1/MATE2K KO | Transformed cell line | Female |
| CVCL_C3LG | STBCi322-A-6 | Induced pluripotent stem cell | Female |
| CVCL_D4TV | HuH7-SLC47A1-KO-c4 | Cancer cell line | Male |
| CVCL_D4TW | HuH7-SLC47A1-KO-c7 | Cancer cell line | Male |
| CVCL_TN85 | HAP1 SLC47A1 (-) | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Targeted by drugs: Cimetidine, Metformin, Pyrimethamine
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): brain aneurysm