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TAS1R3

gene
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Also known as T1R3

Summary

TAS1R3 (taste 1 receptor member 3, HGNC:15661) is a protein-coding gene on chromosome 1p36.33, encoding Taste receptor type 1 member 3 (Q7RTX0). Putative taste receptor.

The protein encoded by this gene is a G-protein coupled receptor involved in taste responses. The encoded protein can form a heterodimeric receptor with TAS1R1 to elicit the umami taste response, or it can bind with TAS1R2 to form a receptor for the sweet taste response.

Source: NCBI Gene 83756 — RefSeq curated summary.

At a glance

  • GWAS associations: 2
  • Clinical variants (ClinVar): 276 total — 1 likely-pathogenic
  • Druggable target: yes — 2 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_152228

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:15661
Approved symbolTAS1R3
Nametaste 1 receptor member 3
Location1p36.33
Locus typegene with protein product
StatusApproved
AliasesT1R3
Ensembl geneENSG00000169962
Ensembl biotypeprotein_coding
OMIM605865
Entrez83756

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000339381

RefSeq mRNA: 1 — MANE Select: NM_152228 NM_152228

CCDS: CCDS30556

Canonical transcript exons

ENST00000339381 — 6 exons

ExonStartEnd
ENSE0000113044613320241332806
ENSE0000137911813335061335314
ENSE0000162795113332591333379
ENSE0000169112613312801331536
ENSE0000169480113329211333124
ENSE0000177998313316381331938

Expression profiles

Bgee: expression breadth ubiquitous, 124 present calls, max score 73.61.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.1437 / max 36.4201, expressed in 55 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter IDTPM avgSamples expressed
890.129953
900.01386

Top tissues by expression

127 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
bone marrow cellCL:000209273.61gold quality
mucosa of transverse colonUBERON:000499168.36gold quality
spleenUBERON:000210667.24gold quality
cortical plateUBERON:000534364.90gold quality
bone marrowUBERON:000237164.38gold quality
tonsilUBERON:000237264.16gold quality
duodenumUBERON:000211464.10gold quality
lymph nodeUBERON:000002963.86gold quality
lower esophagus mucosaUBERON:003583463.75gold quality
ganglionic eminenceUBERON:000402363.25gold quality
hindlimb stylopod muscleUBERON:000425263.04gold quality
sural nerveUBERON:001548862.96silver quality
gastrocnemiusUBERON:000138862.89gold quality
skeletal muscle tissueUBERON:000113462.67gold quality
muscle of legUBERON:000138362.59gold quality
heart left ventricleUBERON:000208461.88gold quality
bloodUBERON:000017861.70gold quality
granulocyteCL:000009461.58gold quality
vermiform appendixUBERON:000115460.87gold quality
small intestineUBERON:000210860.59gold quality
apex of heartUBERON:000209860.58gold quality
small intestine Peyer’s patchUBERON:000345460.41gold quality
saliva-secreting glandUBERON:000104460.11gold quality
ventricular zoneUBERON:000305360.00gold quality
pituitary glandUBERON:000000759.62gold quality
adenohypophysisUBERON:000219658.63gold quality
minor salivary glandUBERON:000183058.44gold quality
esophagus mucosaUBERON:000246958.33gold quality
transverse colonUBERON:000115757.66gold quality
muscle tissueUBERON:000238556.70gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 2.

ExperimentMarker?Max mean expression
E-HCAD-38yes151.81
E-ANND-3yes5.38
E-MTAB-8410no3.43

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CEBPB, GLI3

miRNA regulators (miRDB)

38 targeting TAS1R3, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-10401-5P99.9965.79948
HSA-MIR-477599.9875.006394
HSA-MIR-6888-3P99.9765.951170
HSA-MIR-590-3P99.9674.346478
HSA-MIR-3180-5P99.8269.122422
HSA-MIR-6720-5P99.6566.221459
HSA-MIR-4743-3P99.6268.122095
HSA-MIR-5580-5P99.3866.961139
HSA-MIR-4652-3P99.3370.022742
HSA-MIR-429299.1665.571767
HSA-MIR-6791-5P99.1665.921844
HSA-MIR-5587-5P99.0768.58838
HSA-MIR-6871-5P98.9066.67671
HSA-MIR-76098.8166.651392
HSA-MIR-7851-3P98.7264.88980
HSA-MIR-3187-5P98.3665.741776
HSA-MIR-4436B-3P98.2565.261494
HSA-MIR-6735-5P98.2465.361488
HSA-MIR-7843-5P98.1265.261421
HSA-MIR-5088-5P97.9764.28487
HSA-MIR-130297.9267.27844
HSA-MIR-4632-5P97.8265.381470
HSA-MIR-6879-5P97.7765.521521
HSA-MIR-1285-3P97.7267.021932
HSA-MIR-5189-5P97.7266.961814
HSA-MIR-9851-5P97.5767.491067
HSA-MIR-445697.5064.881678
HSA-MIR-61297.2665.951597
HSA-MIR-429897.2666.59765
HSA-MIR-686097.2166.311656

Literature-anchored findings (GeneRIF, showing 40)

  • sequence differences in T1R receptors within and between species (human and mouse) can significantly influence the selectivity and specificity of taste responses (PMID:11894099)
  • The mechanism of interaction of the sweet protein monellin with T1R2-T1R3 receptor. (PMID:12706725)
  • cysteine-rich region of T1R3 has a role in determining responses to intensely sweet proteins (PMID:15299024)
  • findings demonstrate the different functional roles of T1R3 and T1R2 and the presence of multiple ligand binding sites on the sweet taste receptor (PMID:15353592)
  • An immunohistochemistry study to determine whether and where T1R3 may be localized in the liver and pancreas. (PMID:15585941)
  • transmembrane domains of human T1R3 bind with lactisole to inhibit sweet taste (PMID:15668251)
  • water rinses remove the inhibitor from the heteromeric sweetener receptor TAS1R2-TAS1R3, which activates cells and results in the perception of strong sweetness from pure water (PMID:16633339)
  • Although T1R2-T1R3 is known to have multiple potential ligand-binding sites to receive a wide variety of sweeteners, the present study is apparently the first to identify the ATD of hT1R3 as a new sweetener-binding region. (PMID:17499612)
  • These results show that T1R2 and T1R3 receptors, in addition to their role in taste perception, may also have a role in intrahepatic cholangiocytes. (PMID:17928076)
  • Some of the amino acid positions crucial for activation of hTAS1R2+hTAS1R3 by neohesperidin dihydrochalcone are involved in the binding of allosteric modulators in other class C GPCRs (PMID:17935609)
  • Expressed in the sweet/umami gustatory pathways in taste receptor cells and trigeminal neural pathways in transgenic mice. (PMID:18539481)
  • The heteromeric G-protein-coupled receptor T1R2:T1R3 responds to a vast array of chemically diverse natural and artificial sweeteners. (PMID:19083128)
  • Taken together, these results suggest that Tas1R1-Tas1R3 receptor variants found in human fungiform papillae might contribute to inter-individual differences of sensitivity to L-glutamate. (PMID:19146926)
  • Allelic polymorphism within the TAS1R3 promoter is associated with human taste sensitivity to sucrose. (PMID:19559618)
  • In our sample of subjects, the frequencies of 2 nsSNPs, C329T in tas1r1 and C2269T in tas1r3, were significantly higher in [glutamate] nontasters than expected, whereas G1114A in tas1r1 was more frequent in tasters. (PMID:19571223)
  • Variations in perception of umami taste correlated with variations in the human TAS1R3 gene. (PMID:19587085)
  • Interactions between the human sweet-sensing T1R2-T1R3 receptor and sweeteners detected by saturation transfer difference NMR spectroscopy. (PMID:19664591)
  • Results from mutagenesis and chimeras of the receptor indicated that brazzein interacts with both T1R2 and T1R3 and that the Venus flytrap module of T1R2 is important for brazzein agonism. (PMID:20302879)
  • The sweet taste receptors (alpha-gustducin and T1R3) are involved in glucose-stimulated secretion of GLP-1 and PYY. (PMID:21324568)
  • amino acid substitutions (F749S and R757C), located in the transmembrane domain of T1R3, severely impair receptor functions in vitro (PMID:21422378)
  • T1R2/T1R3 is involved in glucose-dependent secretion of satiation peptides (PMID:21540445)
  • Data show that that Tas1r1 and Tas1r3 are expressed in murine and human spermatozoa. (PMID:22427794)
  • Overexpressed the human N-terminal domain of T1R3 in E. coli and found that the refolded protein behaves as a dimer; showed that hT1R3-NTD is functional and capable of binding sucralose with an affinity in the millimolar range. (PMID:22450161)
  • T1R3 is a receptor responsible for the detection of calcium by taste. (PMID:22773945)
  • Five amino acid residues in cysteine-rich domain of human T1R3 were involved in the response for sweet-tasting protein, thaumatin (PMID:23370115)
  • effects of artificial sweeteners on adipose tissue may be largely independent of the classical sweet taste receptors, T1R2 and T1R3 (PMID:24068707)
  • A complex molecular mechanism involving changes in the properties of both the orthosteric and non-orthosteric sites of T1R1 underlies the determination of ligand specificity in mammalian T1R1/T1R3. (PMID:24214976)
  • human and mouse membrane trafficking systems for sweet taste receptors T1r2 and T1r3 (PMID:25029362)
  • TAS1R3 gene rs307355 polymorphism found independent risk factor for dental caries experience by logistic regression & increased risk of caries. Moderate caries (4-7 caries) found to be associated w/TAS1R3 rs307355 heterozygous genotype (PMID:25924601)
  • The transcripts of TAS1R3 and UCN2 in peripheral blood cells may be considered potential biomarkers of consumption of sugary and fatty food, respectively, to complement data of food-intake questionnaires. (PMID:26168276)
  • T1R3 gene expression in the tongue is suppressed by chemotherapy. (PMID:26422579)
  • The molecular anatomy of sweet taste receptor dimers T1R2-T1R3 has been presented. (PMID:27936499)
  • We observe that binding of agonists to VFD2 of TAS1R2 leads to major conformational changes to form a TM6/TM6 interface between TMDs of TAS1R2 and TAS1R3, which is consistent with the activation process observed biophysically on the metabotropic glutamate receptor 2 homodimer. (PMID:28228527)
  • Regarding “consumption of carbohydrates (% energy) and higher amount of sweet foods, respectively…no associations were found for the TAS1R3 alleles.” (PMID:29110749)
  • These studies are the first to demonstrate a protective effect of an artificial sweetener, through the sweet taste receptor T1R3, on VEGF-induced vasculogenesis in a retinal microvascular endothelial cell line. (PMID:30353220)
  • Studied association of taste 1 receptor member 1 (TAS1R1) and taste 1 receptor member 3 (TAS1R3) single nucleotide polymorphisms (SNPs) with food choices at a buffet meal. and found certain TAS1R1 and TAS1R3 SNPs to be associated with fat and savoury-tasting and protein-rich food choices following a laboratory buffet in humans. (PMID:30518043)
  • The data further reveal that the C terminus of the extracellular cysteine-rich domain needs to be properly folded for T1R3 dimerization and co-trafficking, but not for surface expression of T1R2 alone. These results guided the modeling of the T1R2-T1R3 dimer in living cells. (PMID:30723160)
  • Structural insights into the differences among lactisole derivatives in inhibitory mechanisms against the human sweet taste receptor. (PMID:30883570)
  • Conserved Residues Control the T1R3-Specific Allosteric Signaling Pathway of the Mammalian Sweet-Taste Receptor. (PMID:30893427)
  • Using homology modeling, molecular docking and molecular dynamics (MD) simulations, this study investigates the effects of five natural umami ligands on the structural dynamics of T1R1-T1R3. (PMID:31092329)

Cross-species orthologs

3 orthologs

OrganismSymbolGene ID
danio_reriotas1r3ENSDARG00000006341
mus_musculusTas1r3ENSMUSG00000029072
rattus_norvegicusTas1r3ENSRNOG00000019589

Paralogs (4): CASR (ENSG00000036828), GPRC6A (ENSG00000173612), TAS1R1 (ENSG00000173662), TAS1R2 (ENSG00000179002)

Protein

Protein identifiers

Taste receptor type 1 member 3 — Q7RTX0 (reviewed: Q7RTX0)

Alternative names: Sweet taste receptor T1R3

All UniProt accessions (1): Q7RTX0

UniProt curated annotations — full annotation on UniProt →

Function. Putative taste receptor. TAS1R1/TAS1R3 responds to the umami taste stimulus (the taste of monosodium glutamate). TAS1R2/TAS1R3 recognizes diverse natural and synthetic sweeteners. TAS1R3 is essential for the recognition and response to the disaccharide trehalose. Sequence differences within and between species can significantly influence the selectivity and specificity of taste responses.

Subunit / interactions. Forms homodimers or heterodimers with TAS1R1 and TAS1R2.

Subcellular location. Cell membrane.

Similarity. Belongs to the G-protein coupled receptor 3 family. TAS1R subfamily.

RefSeq proteins (1): NP_689414* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000068GPCR_3_Ca_sens_rcpt-relFamily
IPR000337GPCR_3Family
IPR001828ANF_lig-bd_rcptDomain
IPR011500GPCR_3_9-Cys_domDomain
IPR017978GPCR_3_CDomain
IPR017979GPCR_3_CSConserved_site
IPR028082Peripla_BP_IHomologous_superfamily
IPR038550GPCR_3_9-Cys_sfHomologous_superfamily

Pfam: PF00003, PF01094, PF07562

UniProt features (34 total): topological domain 8, glycosylation site 8, transmembrane region 7, mutagenesis site 6, signal peptide 1, chain 1, region of interest 1, sequence variant 1, sequence conflict 1

Structure

Experimental structures (PDB)

16 structures.

PDBMethodResolution (Å)
9NOUELECTRON MICROSCOPY2.8
9NOXELECTRON MICROSCOPY3
9O38ELECTRON MICROSCOPY3
9NOWELECTRON MICROSCOPY3.1
9UT9ELECTRON MICROSCOPY3.18
9NOVELECTRON MICROSCOPY3.3
9UTCELECTRON MICROSCOPY3.33
9NORELECTRON MICROSCOPY3.4
9UT8ELECTRON MICROSCOPY3.41
9NOSELECTRON MICROSCOPY3.5
9OQ6ELECTRON MICROSCOPY3.57
9OQ4ELECTRON MICROSCOPY3.59
9UTBELECTRON MICROSCOPY3.59
9UTAELECTRON MICROSCOPY3.77
9NOTELECTRON MICROSCOPY3.8
9OQ5ELECTRON MICROSCOPY3.93

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q7RTX0-F187.350.62

Antibody-complex structures (SAbDab): 2 — 9NOX, 9O38

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Glycosylation sites (8): 85, 130, 264, 285, 380, 411, 432, 475

Mutagenesis-validated functional residues (6):

PositionPhenotype
537retains partial activity toward brazzein; however response to other sweeteners tested is suppressed.
537receptor unresponsive to all sweeteners tested.
537abolished the response to brazzein.
540reduces the response to brazzein and monellin.
540reduces the response to monellin.
540reduces the response to brazzein; p-540 also enhances responses to the small molecule sweeteners.

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

IDPathway
R-HSA-418594G alpha (i) signalling events
R-HSA-420499Class C/3 (Metabotropic glutamate/pheromone receptors)
R-HSA-9717207Sensory perception of sweet, bitter, and umami (glutamate) taste

MSigDB gene sets: 53 (showing top): GOBP_SENSORY_PERCEPTION_OF_CHEMICAL_STIMULUS, GOBP_DETECTION_OF_CHEMICAL_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION_OF_TASTE, GOBP_SENSORY_PERCEPTION_OF_TASTE, GOBP_DETECTION_OF_STIMULUS, GOBP_SENSORY_PERCEPTION, GOCC_PLASMA_MEMBRANE_SIGNALING_RECEPTOR_COMPLEX, GOCC_MEMBRANE_PROTEIN_COMPLEX, GOCC_RECEPTOR_COMPLEX, GOCC_PLASMA_MEMBRANE_PROTEIN_COMPLEX, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_TASTE_RECEPTOR_ACTIVITY, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, chr1p36, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_DETECTION_OF_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION

GO Biological Process (6): detection of chemical stimulus involved in sensory perception of sweet taste (GO:0001582), G protein-coupled receptor signaling pathway (GO:0007186), sensory perception of sweet taste (GO:0050916), sensory perception of umami taste (GO:0050917), signal transduction (GO:0007165), sensory perception of taste (GO:0050909)

GO Molecular Function (3): G protein-coupled receptor activity (GO:0004930), taste receptor activity (GO:0008527), sweet taste receptor activity (GO:0033041)

GO Cellular Component (4): Golgi apparatus (GO:0005794), plasma membrane (GO:0005886), membrane (GO:0016020), sweet taste receptor complex (GO:1903767)

Reactome top-level categories

Rollup of top-3 pathways:

CategoryPathways
GPCR downstream signalling1
GPCR ligand binding1
Sensory perception of taste1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
detection of chemical stimulus involved in sensory perception of taste2
sensory perception of taste2
transmembrane signaling receptor activity2
sensory perception of sweet taste1
G protein-coupled receptor activity1
signal transduction1
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
sensory perception of chemical stimulus1
G protein-coupled receptor signaling pathway1
detection of chemical stimulus involved in sensory perception of sweet taste1
taste receptor activity1
cytoplasm1
endomembrane system1
intracellular membrane-bounded organelle1
membrane1
cell periphery1
cellular anatomical structure1
taste receptor complex1

Protein interactions and networks

STRING

1518 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
TAS1R3GNAT3A8MTJ3987
TAS1R3TAS1R2Q8TE23986
TAS1R3TAS1R1Q7RTX1985
TAS1R3SLC5A1P13866949
TAS1R3PLCB2Q00722877
TAS1R3GCGP01275863
TAS1R3TRPM5Q9NZQ8860
TAS1R3TAS2R4Q9NYW5816
TAS1R3FFAR4Q5NUL3802
TAS1R3GLP2RO95838763
TAS1R3TAS2R38P59533727
TAS1R3GLP1RP43220690
TAS1R3GNA14O95837685
TAS1R3PKD2L1Q9P0L9673
TAS1R3INSP01308670

IntAct

7 interactions, top by confidence:

ABTypeScore
TAS1R3TAS1R2psi-mi:“MI:0407”(direct interaction)0.520
TAS1R3psi-mi:“MI:0407”(direct interaction)0.520
TAS1R2TAS1R3psi-mi:“MI:0407”(direct interaction)0.520
TAS1R3SUN1psi-mi:“MI:0914”(association)0.350
HOXD13TAS1R3psi-mi:“MI:0914”(association)0.350

BioGRID (13): TAS1R3 (Affinity Capture-MS), TAS1R3 (Affinity Capture-RNA), TAS1R3 (Protein-RNA), TAS1R3 (Affinity Capture-Western), TAS1R3 (Affinity Capture-Western), LRRC3 (Affinity Capture-MS), TAS1R3 (Affinity Capture-MS), SUN1 (Affinity Capture-MS), STIM1 (Affinity Capture-MS), ACP2 (Affinity Capture-MS), HYAL2 (Affinity Capture-MS), GJA1 (Affinity Capture-MS), TMEM11 (Affinity Capture-MS)

ESM2 similar proteins: A0JND9, E1BPW0, O14773, O18956, O35795, O55026, O75173, O75355, O75356, O75578, O89023, O93295, P08514, P08648, P11688, P17405, P49961, P55772, P56201, P79784, P97687, Q04519, Q0VD19, Q12794, Q32M88, Q49HH9, Q49KI5, Q5DRK1, Q5IS74, Q5MY95, Q5RFL1, Q5RFQ8, Q60HH1, Q6P3E7, Q6P6S9, Q717C1, Q717C2, Q7RTX0, Q8BFW6, Q8BNJ2

Diamond homologs: A3QNZ9, Q49HH9, Q49HI0, Q49KI5, Q54ET0, Q70VB1, Q717C1, Q717C2, Q7RTX0, Q7RTX1, Q8K4Z6, Q923K1, Q925D8, Q925I4, Q99PG6, Q9Z0R7, Q9Z0R8, A3QNZ8, A3QP00, A3QP01, A3QP07, A3QP08, A3QP09, O62714, P35384, Q5U9X3, Q8TE23, Q9PW88, Q54SW3, E1BPQ3, O70410, P41180, P48442, Q5T6X5, Q8GXJ4, Q9QY96, O75899, O88871, Q80T41, E9Q6I0

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

276 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic1
Uncertain significance232
Likely benign30
Benign7

Top pathogenic / likely-pathogenic (1)

Variant IDHGVSClassification
980934GRCh37/hg19 1p36.33(chr1:849466-1806659)x1Likely pathogenic

SpliceAI

745 predictions. Top by Δscore:

VariantEffectΔscore
1:1331533:CCAG:Cdonor_loss0.9900
1:1331534:CAG:Cdonor_loss0.9900
1:1331535:AGGT:Adonor_loss0.9900
1:1331536:GG:Gdonor_loss0.9900
1:1331537:G:Adonor_loss0.9900
1:1331934:CCCAG:Cdonor_loss0.9900
1:1331935:CCAG:Cdonor_loss0.9900
1:1331936:CAG:Cdonor_loss0.9900
1:1331937:AGG:Adonor_loss0.9900
1:1331938:GGTG:Gdonor_loss0.9900
1:1331939:G:GAdonor_loss0.9900
1:1331940:T:Adonor_loss0.9900
1:1332018:TTGCA:Tacceptor_loss0.9900
1:1332019:TGCA:Tacceptor_loss0.9900
1:1332020:GCA:Gacceptor_loss0.9900
1:1332021:CA:Cacceptor_loss0.9900
1:1332022:A:ACacceptor_loss0.9900
1:1332919:A:AGacceptor_gain0.9900
1:1332920:G:GGacceptor_gain0.9900
1:1333121:CCAG:Cdonor_loss0.9900
1:1333122:CAG:Cdonor_loss0.9900
1:1333126:T:Gdonor_loss0.9900
1:1333376:CCAGG:Cdonor_loss0.9900
1:1333378:AGGTG:Adonor_loss0.9900
1:1333379:GGTGA:Gdonor_loss0.9900
1:1333380:G:Adonor_loss0.9900
1:1333381:T:Adonor_loss0.9900
1:1333502:ACAG:Aacceptor_loss0.9900
1:1333503:CAGAC:Cacceptor_loss0.9900
1:1333504:A:AGacceptor_gain0.9900

AlphaMissense

5505 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
1:1332027:A:CS166R0.994
1:1332029:C:AS166R0.994
1:1332029:C:GS166R0.994
1:1331783:A:CS113R0.989
1:1331785:C:AS113R0.989
1:1331785:C:GS113R0.989
1:1333543:G:CW546C0.988
1:1333543:G:TW546C0.988
1:1332147:T:AW206R0.987
1:1332147:T:CW206R0.987
1:1332759:T:AC410S0.987
1:1332760:G:CC410S0.987
1:1332717:G:CA396P0.985
1:1332742:T:CL404P0.985
1:1331873:G:TG143W0.984
1:1331868:T:AV141D0.983
1:1333106:G:CW487C0.983
1:1333106:G:TW487C0.983
1:1331865:C:AA140D0.982
1:1331934:C:AP163H0.981
1:1331873:G:AG143R0.980
1:1331873:G:CG143R0.980
1:1332149:G:CW206C0.980
1:1332149:G:TW206C0.980
1:1332420:T:AW297R0.980
1:1332420:T:CW297R0.980
1:1332718:C:AA396D0.979
1:1332733:C:AA401D0.979
1:1331466:T:CF41L0.978
1:1331467:T:GF41C0.978

dbSNP variants (sampled 300 via entrez): RS1000029917 (1:1332787 ACCC>A), RS1000583389 (1:1331077 G>A,C), RS1000975084 (1:1329954 C>T), RS1001002384 (1:1330897 C>A,T), RS1001328592 (1:1330006 TTGTG>T,TTG), RS1001707902 (1:1335278 T>G), RS1002228340 (1:1330131 C>T), RS1002259396 (1:1330221 C>T), RS1002443009 (1:1334387 T>C,G), RS1002561922 (1:1329670 C>T), RS1002593198 (1:1329755 T>C), RS1002870420 (1:1333247 G>A), RS1002967253 (1:1335628 T>C), RS1003170701 (1:1331080 C>G,T), RS1003250649 (1:1335024 G>A,C)

Disease associations

OMIM: gene MIM:605865 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

2 associations (top):

StudyTraitp-value
GCST004131_103Inflammatory bowel disease2.000000e-07
GCST004133_40Ulcerative colitis3.000000e-06

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL1613742 (SINGLE PROTEIN), CHEMBL3832641 (PROTEIN COMPLEX), CHEMBL3832642 (PROTEIN COMPLEX)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 166,345 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL752ADENOSINE PHOSPHATE4165,316
CHEMBL3715108LACTISOLE SODIUM11,029

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Taste 1 receptors

Most potent curated ligand interactions (1 total), top 1:

LigandActionAffinityParameter
lactisoleNegative4.19pIC50

Binding affinities (BindingDB)

268 measured of 271 human assays (271 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
N-hexan-3-yl-3-methyl-4-methylsulfanylbenzamideEC50120 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl 2-[(3-chloro-4-methoxybenzoyl)amino]hexanoateEC50120 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-hexan-3-yl-3,4-dimethylbenzamideEC50140 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
2,3,5,6-tetrafluoro-4-methyl-N-(3-methylbutan-2-yl)benzamideEC50140 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[(4-ethenylbenzoyl)amino]-4-methylpentanoateEC50180 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N’-[(2,4-dimethoxyphenyl)methyl]-N-[2-(furan-2-yl)ethyl]oxamideEC50180 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N’-[(4-ethoxy-2-methoxyphenyl)methyl]-N-[2-(5-methyl-2-pyridinyl)ethyl]oxamideEC50190 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3-chloro-2-hydroxy-N-(2-methyl-1,2,3,4-tetrahydronaphthalen-1-yl)benzamideEC50190 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-methoxy-3-methyl-N-(2-methylpentan-3-yl)benzamideEC50200 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-methoxy-3-methyl-N-(2-methylhexan-3-yl)benzamideEC50200 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[(4-ethylsulfanylbenzoyl)amino]-4-methylpentanoateEC50200 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-(3,3-dimethylbutan-2-yl)-2,3,5,6-tetrafluoro-4-methylbenzamideEC50210 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3,6-dichloro-N-(4-ethoxyphenyl)-2-methoxybenzamideEC50220 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-heptan-4-yl-4-methoxy-3-methylbenzamideEC50220 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[(3,4-dimethylbenzoyl)amino]-3-methylbutanoateEC50250 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[(4-methoxy-3-methylbenzoyl)amino]-4-methylpentanoateEC50250 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-ethoxy-3-methyl-N-pentan-3-ylbenzamideEC50260 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-[(2R)-1-methoxy-4-methylpentan-2-yl]-3-methyl-4-methylsulfanylbenzamideEC50290 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-[(2,4-dimethoxyphenyl)methyl]-3-pyrrol-1-ylpyridine-4-carboxamideEC50290 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl 2-[(3-chloro-4-methoxybenzoyl)amino]pentanoateEC50290 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
(E)-N-(2,4-dimethylpentan-3-yl)-3-(4-methoxyphenyl)prop-2-enamideEC50290 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2S)-2-(1-benzofuran-2-carbonylamino)-4-methylpentanoateEC50310 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2S)-2-[(5-methoxy-1-benzofuran-2-carbonyl)amino]-4-methylpentanoateEC50320 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-ethoxy-N-heptan-4-ylbenzamideEC50320 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-4-methyl-2-[(4-methylbenzoyl)amino]pentanoateEC50320 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[[(E)-3-(4-methoxyphenyl)prop-2-enoyl]amino]-4-methylpentanoateEC50320 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3-(1,1-difluoroethyl)-N-heptan-4-ylbenzamideEC50330 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-heptan-4-yl-3-(trifluoromethyl)benzamideEC50330 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-ethyl-N-heptan-4-ylbenzamideEC50340 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-ethoxy-3-methyl-N-(5-methylhexan-3-yl)benzamideEC50340 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[(3-methoxy-4-methylbenzoyl)amino]-4-methylpentanoateEC50340 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R,3R)-2-(1,3-benzodioxole-5-carbonylamino)-2,3-dimethylpentanoateEC50350 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3-fluoro-N-heptan-4-yl-4-methoxybenzamideEC50350 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-4-methyl-2-(naphthalene-2-carbonylamino)pentanoateEC50370 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
1-(2-chlorophenyl)-3-heptan-4-ylureaEC50370 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
2-methyl-N-(2-methylheptan-4-yl)-1,3-benzoxazole-5-carboxamideEC50380 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-heptan-4-yl-4-methylsulfanylbenzamideEC50390 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2S)-2-(1-benzothiophene-2-carbonylamino)-4-methylpentanoateEC50400 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-methoxy-3-methyl-N-(4-phenylbutan-2-yl)benzamideEC50400 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-(2-methylcyclohexyl)-3-(trifluoromethoxy)benzamideEC50420 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3-chloro-4-methoxy-N-(2-methylcyclohexyl)benzamideEC50440 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3-chloro-5-fluoro-N-(2-methylcyclohexyl)benzamideEC50450 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
5-methoxy-N-[(2R)-1-methoxy-4-methylpentan-2-yl]-1-benzofuran-2-carboxamideEC50460 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-ethenyl-N-heptan-4-ylbenzamideEC50460 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-heptan-4-yl-4-methoxybenzamideEC50460 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3-chloro-4-methoxy-N-pentan-2-ylbenzamideEC50470 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
5-bromo-N-heptan-4-ylfuran-2-carboxamideEC50490 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl 2-(1,3-benzodioxole-5-carbonylamino)hexanoateEC50490 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
1-(2,4-dichlorophenyl)-3-(1-phenylpropyl)ureaEC50490 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-[(2R)-3,3-dimethylbutan-2-yl]-2,3,5,6-tetrafluoro-4-methylbenzamideEC50490 nMUS-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators

ChEMBL bioactivities

523 potent at pChembl≥5 of 556 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
6.92EC50120nMCHEMBL3719142
6.92EC50120nMCHEMBL3717666
6.85EC50140nMCHEMBL3716217
6.85EC50140nMCHEMBL3717758
6.75EC50180nMCHEMBL3717202
6.75EC50180nMCHEMBL3715156
6.72EC50190nMCHEMBL3718834
6.72IC50190nMLACTISOLE SODIUM
6.72EC50190nMCHEMBL3719110
6.70EC50200nMCHEMBL3718431
6.70EC50200nMCHEMBL3719352
6.70EC50200nMCHEMBL3719220
6.68IC50210nMLACTISOLE SODIUM
6.68EC50210nMCHEMBL3716208
6.66EC50220nMCHEMBL3718284
6.66EC50220nMCHEMBL3714931
6.60EC50250nMCHEMBL3718656
6.60EC50250nMCHEMBL3715023
6.58EC50260nMCHEMBL3715281
6.54EC50290nMCHEMBL3717168
6.54EC50290nMCHEMBL3717504
6.54EC50290nMCHEMBL3717894
6.54EC50290nMCHEMBL3716393
6.51EC50310nMCHEMBL3715808
6.51EC50310nMCHEMBL4111248
6.50EC50320nMCHEMBL3718018
6.50EC50320nMCHEMBL3717726
6.50EC50320nMCHEMBL3715084
6.50EC50320nMCHEMBL3716141
6.50EC50320nMCHEMBL4114892
6.48EC50330nMCHEMBL3716606
6.48EC50330nMCHEMBL3909427
6.47EC50340nMCHEMBL3717635
6.47EC50340nMCHEMBL3719291
6.47EC50340nMCHEMBL3718505
6.46EC50350nMCHEMBL3717722
6.46EC50350nMCHEMBL3718486
6.46IC50350nMLACTISOLE SODIUM
6.46EC50350nMCHEMBL4107128
6.43EC50370nMCHEMBL3715936
6.43EC50370nMCHEMBL3715875
6.42EC50380nMCHEMBL3717692
6.41EC50390nMCHEMBL3715364
6.40EC50400nMCHEMBL3715954
6.40EC50400nMCHEMBL3717599
6.40EC50400nMCHEMBL4114511
6.38EC50420nMCHEMBL3715898
6.36EC50440nMCHEMBL3716867
6.35EC50450nMCHEMBL3717965
6.34EC50460nMCHEMBL3716609

CTD chemical–gene interactions

26 total (human), top 26 by PubMed support.

ChemicalActions (top 5)PubMed papers
lactisoledecreases reaction, increases activity, decreases activity, affects binding3
Aspartameaffects binding, increases reaction, decreases expression, decreases reaction, increases activity3
Cyclamatesaffects binding, increases activity, decreases reaction3
neohesperidin dihydrochalconedecreases reaction, increases activity, affects binding2
trichlorosucroseaffects binding, increases activity2
neotameaffects binding, increases activity2
aristolochic acid Iincreases expression1
triphenyl phosphateaffects expression1
1-chlorosucroseaffects binding, increases activity1
1,6-dichlorosucroseincreases activity, affects binding1
jinfukangdecreases expression, affects cotreatment1
Resveratrolaffects cotreatment, decreases expression1
Sunitinibincreases expression1
Air Pollutantsincreases abundance, affects expression1
Benzo(a)pyreneaffects methylation1
Cisplatinaffects cotreatment, decreases expression1
Glucoseincreases reaction, affects binding1
Oxygenincreases expression1
Ozoneaffects expression, increases abundance1
Plant Extractsaffects cotreatment, decreases expression1
Silicon Dioxidedecreases expression1
Sodium Glutamateincreases expression1
Sucroseaffects binding, increases activity1
Sweetening Agentsaffects binding, increases activity1
Tobacco Smoke Pollutionincreases expression1
Okadaic Acidincreases expression1

ChEMBL screening assays

68 unique, capped per target: 43 binding, 25 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL3720951FunctionalActivity at human T1R3 containing rat T1R3 extracellular loop-2 assessed as calcium response by fluo-4-AM dye based FLIPR assayT1R hetero-oligomeric taste receptors, cell lines that express said receptors, and taste compounds
CHEMBL3720853BindingActivity at human T1R1/T1R3 expressed in HEK293T cells co-expressing Galpha15 assessed as induction of left-ward shift of glutamate dose response curve at 1 mM relative to untreated controlT1R hetero-oligomeric taste receptors, cell lines that express said receptors, and taste compounds

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 81

This page pulls from 81 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatentpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot