Send feedback

TAS2R5

gene
On this page

Also known as T2R5

Summary

TAS2R5 (taste 2 receptor member 5, HGNC:14912) is a protein-coding gene on chromosome 7q34, encoding Taste receptor type 2 member 5 (Q9NYW4). Receptor that may play a role in the perception of bitterness and is gustducin-linked.

This gene encodes a bitter taste receptor; bitter taste receptors are members of the G protein-coupled receptor superfamily and are specifically expressed by taste receptor cells of the tongue and palate epithelia. Each of these apparently intronless taste receptor genes encodes a 7-transmembrane receptor protein, functioning as a bitter taste receptor. This gene is clustered with another 3 candidate taste receptor genes on chromosome 7 and is genetically linked to loci that influence bitter perception.

Source: NCBI Gene 54429 — RefSeq curated summary.

At a glance

  • GWAS associations: 2
  • Clinical variants (ClinVar): 46 total
  • GTEx eGene: eQTL in 32 tissues, sQTL in 0 (q < 0.05)
  • ChEMBL bioactivity: 1 clinical-phase molecule tested; no curated mechanism-of-action drug
  • Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 1.12 (unconstrained)
  • MANE Select transcript: NM_018980

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:14912
Approved symbolTAS2R5
Nametaste 2 receptor member 5
Location7q34
Locus typegene with protein product
StatusApproved
AliasesT2R5
Ensembl geneENSG00000127366
Ensembl biotypeprotein_coding
OMIM605062
Entrez54429

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

MANE Select: ENST00000247883

ENST00000247883

RefSeq mRNA: 1 — MANE Select: NM_018980 NM_018980

CCDS: CCDS5869

Canonical transcript exons

ENST00000247883 — 1 exons

ExonStartEnd
ENSE00000872187141790217141791367

Expression profiles

Bgee: expression breadth ubiquitous, 156 present calls, max score 90.43.

Highest expression (Bgee): male germ line stem cell (sensu Vertebrata) in testis, uterine tube, ovary, hemisphere of cerebellum, cerebellar hemisphere.

Genetic regulation across tissues (GTEx eQTL / sQTL)

TAS2R5 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 32 tissues and its splicing (sQTL) in 0 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 32 significant tissue × QTL associations:

TissueQTLq-valueSlopeLead variant
Thyroideqtl3.4e-25-0.347:141737464:G:C
Skin Not Sun Exposed Suprapubiceqtl5.1e-24-0.337:141747018:C:T
Cells EBV-transformed lymphocyteseqtl3.4e-22-0.507:141775254:T:C
Esophagus Mucosaeqtl2.8e-21-0.397:141743011:C:T
Skin Sun Exposed Lower legeqtl1.5e-17-0.297:141768038:A:G
Cells Cultured fibroblastseqtl5.3e-13-0.197:141765563:T:C
Brain Cerebellumeqtl1.5e-12-0.477:141769762:A:AAAAT
Stomacheqtl2.3e-12-0.327:141737464:G:C
Colon Transverseeqtl2.8e-12-0.327:141765563:T:C
Esophagus Musculariseqtl7.1e-12-0.277:141768038:A:G
Testiseqtl7.4e-11-0.267:141765563:T:C
Pituitaryeqtl5.3e-10-0.357:141778774:G:C
Esophagus Gastroesophageal Junctioneqtl1.7e-09-0.287:141742413:G:A
Adipose Visceral Omentumeqtl3.5e-09+0.197:141903540:AG:A
Spleeneqtl7.8e-09-0.367:141747018:C:T
Whole Bloodeqtl9.5e-09-0.277:141751282:AGTGCTGT:A
Muscle Skeletaleqtl1.7e-08-0.237:141747751:G:C
Lungeqtl5.5e-08-0.217:141742852:A:G
Colon Sigmoideqtl6.3e-08-0.277:141778774:G:C
Pancreaseqtl1.5e-07-0.377:141778774:G:C

Top tissues by expression

showing 100 of 245 tissues by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047390.43gold quality
right uterine tubeUBERON:000130275.60gold quality
left ovaryUBERON:000211972.31gold quality
right ovaryUBERON:000211871.99gold quality
right hemisphere of cerebellumUBERON:001489071.24gold quality
cerebellar hemisphereUBERON:000224570.54gold quality
cerebellar cortexUBERON:000212970.44gold quality
endocervixUBERON:000045869.62gold quality
ectocervixUBERON:001224969.39gold quality
body of uterusUBERON:000985369.29gold quality
tibial nerveUBERON:000132369.20gold quality
cerebellumUBERON:000203768.93gold quality
skin of abdomenUBERON:000141668.81gold quality
mucosa of stomachUBERON:000119968.26gold quality
skin of legUBERON:000151168.07gold quality
stromal cell of endometriumCL:000225567.98gold quality
uterine cervixUBERON:000000266.59gold quality
left uterine tubeUBERON:000130366.39gold quality
ovaryUBERON:000099266.35gold quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099165.31gold quality
right coronary arteryUBERON:000162565.19gold quality
zone of skinUBERON:000001465.11gold quality
pituitary glandUBERON:000000765.08gold quality
minor salivary glandUBERON:000183065.08gold quality
body of pancreasUBERON:000115065.02gold quality
adenohypophysisUBERON:000219664.82gold quality
small intestine Peyer’s patchUBERON:000345464.77gold quality
myocardiumUBERON:000234964.44gold quality
vaginaUBERON:000099664.32gold quality
muscle layer of sigmoid colonUBERON:003580564.26gold quality
esophagogastric junction muscularis propriaUBERON:003584164.22gold quality
left lobe of thyroid glandUBERON:000112063.69gold quality
metanephros cortexUBERON:001053363.36gold quality
transverse colonUBERON:000115763.34gold quality
esophagus mucosaUBERON:000246963.31gold quality
right lobe of thyroid glandUBERON:000111963.30gold quality
lower esophagusUBERON:001347363.29gold quality
lower esophagus muscularis layerUBERON:003583363.29gold quality
peritoneumUBERON:000235863.15gold quality
omental fat padUBERON:001041463.15gold quality
upper lobe of left lungUBERON:000895263.14gold quality
thyroid glandUBERON:000204663.00gold quality
esophagusUBERON:000104362.95gold quality
popliteal arteryUBERON:000225062.85gold quality
spleenUBERON:000210662.83gold quality
tibial arteryUBERON:000761062.82gold quality
left coronary arteryUBERON:000162662.77gold quality
apex of heartUBERON:000209862.77gold quality
gastrocnemiusUBERON:000138862.59gold quality
body of stomachUBERON:000116162.56gold quality
aortaUBERON:000094762.47gold quality
ascending aortaUBERON:000149662.31gold quality
thoracic aortaUBERON:000151562.26gold quality
muscle of legUBERON:000138362.21gold quality
descending thoracic aortaUBERON:000234562.20gold quality
C1 segment of cervical spinal cordUBERON:000646962.19gold quality
adipose tissue of abdominal regionUBERON:000780861.92gold quality
mouth mucosaUBERON:000372961.87gold quality
coronary arteryUBERON:000162161.74gold quality
small intestineUBERON:000210861.45gold quality
upper lobe of lungUBERON:000894861.38gold quality
right atrium auricular regionUBERON:000663161.15gold quality
lower esophagus mucosaUBERON:003583461.13gold quality
subcutaneous adipose tissueUBERON:000219061.07gold quality
saliva-secreting glandUBERON:000104460.88gold quality
cardiac atriumUBERON:000208160.62gold quality
female reproductive systemUBERON:000047460.44gold quality
granulocyteCL:000009460.43gold quality
right lungUBERON:000216760.40gold quality
spinal cordUBERON:000224060.19gold quality
right frontal lobeUBERON:000281060.06gold quality
colonUBERON:000115559.94gold quality
intestineUBERON:000016059.88gold quality
stomachUBERON:000094559.84gold quality
uterusUBERON:000099559.80gold quality
tendon of biceps brachiiUBERON:000818859.65gold quality
myometriumUBERON:000129659.53gold quality
pancreasUBERON:000126459.52gold quality
large intestineUBERON:000005959.30gold quality
tendonUBERON:000004359.23gold quality
vermiform appendixUBERON:000115459.20gold quality
calcaneal tendonUBERON:000370159.18gold quality
right adrenal glandUBERON:000123359.02gold quality
cortex of kidneyUBERON:000122558.71gold quality
fundus of stomachUBERON:000116058.66gold quality
Brodmann (1909) area 9UBERON:001354058.56gold quality
left adrenal glandUBERON:000123458.40gold quality
nucleus accumbensUBERON:000188258.36gold quality
right adrenal gland cortexUBERON:003582758.35gold quality
heartUBERON:000094858.31gold quality
prostate glandUBERON:000236758.25gold quality
anatomical systemUBERON:000046758.09gold quality
heart left ventricleUBERON:000208458.08gold quality
left adrenal gland cortexUBERON:003582558.08gold quality
right lobe of liverUBERON:000111458.03gold quality
multicellular organismUBERON:000046857.72gold quality
material anatomical entityUBERON:000046557.70gold quality
cardiac ventricleUBERON:000208257.48gold quality
adrenal glandUBERON:000236957.29gold quality
ventricular zoneUBERON:000305357.19gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

ExperimentMarker?Max mean expression
E-ANND-3no1.61

HPA expression

RNA tissue specificity: Low tissue specificity

showing 60 of 61 HPA tissues / cells by nTPM:

Tissue / cellAxisnTPM
Cerebellumtissue8.2
Hypothalamustissue6.6
Midbraintissue6.5
Cerebral cortextissue6.2
Basal gangliatissue6.2
Nucleus accumbenstissue6.2
Medulla oblongatatissue5.9
Ponstissue5.8
Thalamustissue5.6
Spinal cordtissue5.3
Hippocampal formationtissue5.3
Amygdalatissue5.2
Putamentissue4.9
Postcentral gyrustissue4.8
Occipital cortextissue4.8
Hippocampustissue4.5
Locus coeruleustissue4.4
Substantia nigratissue4.2
Skin 1tissue4.0
Retrosplenial cortextissue4.0
Choroid plexustissue3.4
Epididymistissue2.6
Pituitary glandtissue2.5
Vaginatissue2.3
Breasttissue1.5
Retinatissue1.5
Skeletal muscletissue1.3
Endometrium 1tissue1.3
Fallopian tubetissue1.1
Ovarytissue1.0
Spleentissue0.9
Cervixtissue0.7
Thymustissue0.7
Appendixtissue0.7
Lymph nodetissue0.6
Testistissue0.6
Rectumtissue0.6
Pancreastissue0.6
Small intestinetissue0.6
Tonsiltissue0.6
Seminal vesicletissue0.5
Salivary glandtissue0.5
Smooth muscletissue0.5
Placentatissue0.5
Lungtissue0.5
Prostatetissue0.5
Adrenal glandtissue0.5
Colontissue0.4
Thyroid glandtissue0.4
Gallbladdertissue0.4
Kidneytissue0.4
Duodenumtissue0.4
Stomach 1tissue0.3
Adipose tissuetissue0.3
Esophagustissue0.3
Parathyroid glandtissue0.3
Urinary bladdertissue0.3
Tonguetissue0.3
Heart muscletissue0.2
Livertissue0.2

Brain sub-regions (HPA Brain Atlas): detected in 185; highest nTPM — Vermis (8.2), Cerebellar cortex (7.3), Flocculonodular lobe (7.0), Parieto-temporal junction (white matter) (7.0), White matter (7.0).

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

Targeting TAS2R5 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

7 miRNAs:

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-1252-5P100.0069.802774
HSA-MIR-651-3P99.9473.485177
HSA-MIR-466097.7967.441328
HSA-MIR-428797.5567.241247
HSA-MIR-4685-3P97.5567.351255
HSA-MIR-7106-3P97.3365.33644
HSA-MIR-397696.6767.791187

Functional genomics

gnomAD constraint: pLI 3.22e-05, LOEUF 1.12, missense Z 0.657 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000247883 — one region, missense o/e 0.96.

Literature-anchored findings (GeneRIF, showing 1)

  • Polymorphism of TAS2R3, TAS2R5, TAS2R19, and TAS2R50 genes and bitter food intake frequency inelderly woman. (PMID:32227702)

Cross-species orthologs

0 orthologs

Paralogs (23): TAS2R8 (ENSG00000121314), TAS2R10 (ENSG00000121318), TAS2R7 (ENSG00000121377), TAS2R9 (ENSG00000121381), TAS2R3 (ENSG00000127362), TAS2R4 (ENSG00000127364), TAS2R16 (ENSG00000128519), TAS2R1 (ENSG00000169777), TAS2R60 (ENSG00000185899), TAS2R42 (ENSG00000186136), TAS2R19 (ENSG00000212124), TAS2R50 (ENSG00000212126), TAS2R14 (ENSG00000212127), TAS2R13 (ENSG00000212128), TAS2R41 (ENSG00000221855), TAS2R40 (ENSG00000221937), TAS2R46 (ENSG00000226761), TAS2R39 (ENSG00000236398), TAS2R43 (ENSG00000255374), TAS2R20 (ENSG00000255837), TAS2R30 (ENSG00000256188), TAS2R31 (ENSG00000256436), TAS2R38 (ENSG00000257138)

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

OrganismUniProtIdentityMethod
Pan troglodytesQ646A499.7%Diamond
Pan paniscusQ646D599.7%Diamond
Gorilla gorilla gorillaQ645Z198.0%Diamond
Pongo pygmaeusQ645U095.7%Diamond
Papio hamadryasQ646E694.0%Diamond
Rattus norvegicusQ4VHE787.6%Diamond
Mus musculusQ7TQB983.3%Diamond
Gallus gallusQ2AB8339.9%Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

SymbolTypeEntrez
TAS2R3protein-coding50831
TAS2R4protein-coding50832
SSBP1protein-coding6742

Protein

Protein identifiers

Taste receptor type 2 member 5 — Q9NYW4 (reviewed: Q9NYW4)

All UniProt accessions (2): A4D1U0, Q9NYW4

UniProt curated annotations — full annotation on UniProt →

Function. Receptor that may play a role in the perception of bitterness and is gustducin-linked. May play a role in sensing the chemical composition of the gastrointestinal content. The activity of this receptor may stimulate alpha gustducin, mediate PLC-beta-2 activation and lead to the gating of TRPM5.

Subcellular location. Membrane.

Tissue specificity. Expressed in subsets of taste receptor cells of the tongue and palate epithelium and exclusively in gustducin-positive cells.

Miscellaneous. Most taste cells may be activated by a limited number of bitter compounds; individual taste cells can discriminate among bitter stimuli.

Similarity. Belongs to the G protein-coupled receptor T2R family.

RefSeq proteins (1): NP_061853* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR007960TAS2RFamily

Pfam: PF05296

UniProt features (23 total): topological domain 8, transmembrane region 7, sequence variant 6, chain 1, glycosylation site 1

Structure

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q9NYW4-F179.930.22

Human Protein Atlas

Protein class: G-protein coupled receptors, GPCRs excl olfactory receptors, Family T2R receptors (taste receptor GPCRs), Predicted membrane proteins, GPCRHMM predicted membrane proteins

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): nucleoli; nucleoplasm; cytoplasmic bodies

Antibody reliability (HPA): IF approved

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 (1)

TypePositions
N-linked (glcnac…) asparagine155

Function

Pathways and Gene Ontology

Reactome pathways

2 curated (TAS) of 9; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

9 pathways:

IDPathwayEvidence
R-HSA-420499Class C/3 (Metabotropic glutamate/pheromone receptors)curated
R-HSA-418594G alpha (i) signalling eventscurated
R-HSA-388396GPCR downstream signalling—
R-HSA-500792GPCR ligand binding—
R-HSA-9709957Sensory Perception—
R-HSA-9717207Sensory perception of sweet, bitter, and umami (glutamate) tasteelectronic
R-HSA-9717189Sensory perception of taste—
R-HSA-162582Signal Transduction—
R-HSA-372790Signaling by GPCR—

MSigDB gene sets: 36 (showing top): GOBP_BEHAVIOR, GOBP_SENSORY_PERCEPTION_OF_CHEMICAL_STIMULUS, GOBP_DETECTION_OF_CHEMICAL_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION_OF_TASTE, GOBP_SENSORY_PERCEPTION_OF_TASTE, GOBP_CHEMOSENSORY_BEHAVIOR, GOBP_DETECTION_OF_STIMULUS, GOBP_SENSORY_PERCEPTION, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_BITTER_TASTE_RECEPTOR_ACTIVITY, GOMF_TASTE_RECEPTOR_ACTIVITY, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_DETECTION_OF_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION, GOBP_SENSORY_PERCEPTION_OF_BITTER_TASTE, MIR651_3P

GO Biological Process (5): detection of chemical stimulus involved in sensory perception of bitter taste (GO:0001580), chemosensory behavior (GO:0007635), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), sensory perception of taste (GO:0050909)

GO Molecular Function (4): G protein-coupled receptor activity (GO:0004930), taste receptor activity (GO:0008527), bitter taste receptor activity (GO:0033038), protein binding (GO:0005515)

GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

6 top-level categories:

CategoryPathways
Signaling by GPCR2
GPCR downstream signalling1
GPCR ligand binding1
Sensory perception of taste1
Signal Transduction1
Sensory Perception1

GO top-level categories

20 GO namespaces:

CategoryTerms
detection of chemical stimulus involved in sensory perception of taste2
transmembrane signaling receptor activity2
sensory perception of bitter taste1
behavior1
response to chemical1
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
G protein-coupled receptor activity1
signal transduction1
sensory perception of chemical stimulus1
G protein-coupled receptor signaling pathway1
detection of chemical stimulus involved in sensory perception of bitter taste1
taste receptor activity1
binding1
membrane1
cell periphery1
cellular anatomical structure1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 2 of 11 annotations. The rest are phylogenetic / computational / electronic (IEA).

2 experimentally-supported GO terms:

GO termNSEvidence
detection of chemical stimulus involved in sensory perception of bitter tasteBPdirect assay
bitter taste receptor activityMFdirect assay

Protein interactions and networks

STRING

showing 15 of 300 interactions by confidence (×1000):

Protein AProtein BPartner UniProtScore
TAS2R5GNAT3A8MTJ3856
TAS2R5TAS1R2Q8TE23593
TAS2R5TAS1R3Q7RTX0592
TAS2R5OR52L1Q8NGH7569
TAS2R5OR2J3O76001555
TAS2R5TAS1R1Q7RTX1498
TAS2R5OR4F4Q96R69494
TAS2R5OR11H1Q8NG94491
TAS2R5OR1E1P30953468
TAS2R5OR2T33Q8NG76466
TAS2R5OR2T1O43869441
TAS2R5PLCB2Q00722441
TAS2R5OR2L13Q8N349441
TAS2R5OR10G8Q8NGN5441
TAS2R5TRPM5Q9NZQ8437

IntAct

Human interaction partners of TAS2R5 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

6 partners by confidence:

PartnerInteraction typeMIscoreRecords
CCL4physical association0.5603
RTP2physical association0.5603
SFT2D2physical association0.5603
SLC30A2physical association0.5603
TMEM187physical association0.5603
VAMP5physical association0.5603

BioGRID (7 interactions; top human partners by supporting records): CCL4 (Two-hybrid), KRAS (Synthetic Lethality), RTP2 (Two-hybrid), SFT2D2 (Two-hybrid), SLC30A2 (Two-hybrid), TMEM187 (Two-hybrid), VAMP5 (Two-hybrid)

Disease & clinical

Genetic variants

Variant evidence for TAS2R5: 46 ClinVar records (0 pathogenic / likely pathogenic); 2 GWAS associations.

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance43
Likely benign3
Benign0

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 10 predictions of 180):

Position(s)EffectΔscoreSites
7:141791365acceptor_gain0.6600
7:141790992donor_gain0.6500
7:141790960acceptor_gain0.6300
7:141790734donor_gain0.6100
7:141790953acceptor_gain0.6100
7:141791183acceptor_gain0.6000
7:141790925acceptor_gain0.5800
7:141791176acceptor_gain0.5700
7:141790888donor_gain0.5300
7:141791062donor_gain0.5200

AlphaMissense

359 missense substitutions predicted likely pathogenic (of 1,945 scored), across 139 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

ResidueLikely-pathogenic substitutionsMean am_pathogenicityMax am_pathogenicity
D6580.7030.783
F22770.7700.946
F18470.7620.913
M26160.7450.826
H26860.7370.818
P26560.7170.839
K11950.7770.912
N2450.7450.897
C10450.7080.838
F6950.7000.748
P18050.6860.854
S9240.9070.968
S8940.8880.953
S10040.8560.945
F1740.8450.928
F10240.8080.880
F5640.8040.826
W8540.7950.797
F9540.7940.861
W9440.7820.934

HPA cancer prognostics

RNA cancer specificity: Low cancer specificity

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

1 prognostic cancer types:

CancerPrognosticp-value
Rectum Adenocarcinoma (validation)favorable0.000762

Disease associations

OMIM: gene MIM:605062 | disease phenotypes:

GWAS associations

2 associations:

StudyTraitp-value
GCST001961_8Anorexia nervosa2e-7
GCST003815_22Late-onset Alzheimer’s disease7e-6

EFO canonical traits (from GWAS)

1 canonical traits:

EFO IDTrait name
EFO:1001870late-onset Alzheimers disease

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4523473 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 40,435 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

1 molecules by phase:

MoleculeNamePhasePatents
CHEMBL434ISOPROTERENOL440,435

PharmGKB: 1 entry (CPIC guideline: no)

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Taste 2 receptors

Most potent curated ligand interactions (2 total), top 2:

LigandActionAffinityParameter
epigallocatechin-3-gallateAgonist4.91pEC50
Procyanidin C2Agonist4.45pEC50

ChEMBL bioactivities

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

pChemblTypeValueUnitMolecule
8.31EC504.9nMISOPROTERENOL

CTD chemical–gene interactions

10 total (human), top 10 by PubMed support.

ChemicalActions (top 5)PubMed papers
aristolochic acid Iincreases expression1
propionaldehydedecreases expression1
2,2’,4,4’-tetrabromodiphenyl etherincreases expression1
Acetaminophenincreases expression1
Air Pollutantsincreases expression1
Benzo(a)pyreneincreases expression1
Hydralazineaffects cotreatment, increases expression1
Tobacco Smoke Pollutionincreases expression1
Valproic Acidaffects cotreatment, increases expression1
Asbestos, Crocidoliteaffects expression1

ChEMBL screening assays

8 unique, capped per target: 8 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL4346425FunctionalAntagonist activity at recombinant human TAS2R5 transiently expressed in HEK293T co-expressing Galpha16gust44 assessed as inhibition of picoline-induced intracellular calcium level by measuring remaining activity at 25 uM by fluo-4AM dye baDiscovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists. — *J Med Chem*

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for TAS2R5 across ~30M SureChEMBL compounds — explore on Sugi Predict.

  • Targeted by drugs: Epigalocatechin Gallate
  • Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): anorexia nervosa