TAS2R16
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Also known as T2R16
Summary
TAS2R16 (taste 2 receptor member 16, HGNC:14921) is a protein-coding gene on chromosome 7q31.32, encoding Taste receptor type 2 member 16 (Q9NYV7). Gustducin-coupled receptor implicated in the perception of bitter compounds in the oral cavity and the gastrointestinal tract.
This gene encodes a member of a family of candidate taste receptors that are members of the G protein-coupled receptor superfamily. These family members are specifically expressed by taste receptor cells of the tongue and palate epithelia. Each of these apparently intronless genes encodes a 7-transmembrane receptor protein, functioning as a bitter taste receptor. This gene is clustered with another 3 candidate taste receptor genes in chromosome 7 and is genetically linked to loci that influence bitter perception.
Source: NCBI Gene 50833 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 39 total
- Phenotypes (HPO): 2
- Druggable target: yes — 1 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_016945
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:14921 |
| Approved symbol | TAS2R16 |
| Name | taste 2 receptor member 16 |
| Location | 7q31.32 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | T2R16 |
| Ensembl gene | ENSG00000128519 |
| Ensembl biotype | protein_coding |
| OMIM | 604867 |
| Entrez | 50833 |
Gene structure
Transcript identifiers
Ensembl transcripts: 1 — 1 protein_coding
ENST00000249284
RefSeq mRNA: 1 — MANE Select: NM_016945
NM_016945
CCDS: CCDS5785
Canonical transcript exons
ENST00000249284 — 1 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000882036 | 122994704 | 122995700 |
Expression profiles
Bgee: expression breadth tissue_specific, 4 present calls, max score 60.66.
Top tissues by expression
264 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| tibialis anterior | UBERON:0001385 | 60.66 | silver quality |
| pancreatic ductal cell | CL:0002079 | 58.71 | silver quality |
| ileal mucosa | UBERON:0000331 | 57.13 | silver quality |
| decidua | UBERON:0002450 | 56.55 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 54.38 | gold quality |
| deltoid | UBERON:0001476 | 53.11 | silver quality |
| hair follicle | UBERON:0002073 | 52.43 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 50.97 | gold quality |
| quadriceps femoris | UBERON:0001377 | 49.41 | gold quality |
| Brodmann (1909) area 46 | UBERON:0006483 | 49.30 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 49.20 | gold quality |
| olfactory bulb | UBERON:0002264 | 48.92 | gold quality |
| myocardium | UBERON:0002349 | 48.87 | gold quality |
| type B pancreatic cell | CL:0000169 | 48.83 | gold quality |
| cardiac muscle of right atrium | UBERON:0003379 | 48.55 | gold quality |
| CA1 field of hippocampus | UBERON:0003881 | 48.50 | gold quality |
| vastus lateralis | UBERON:0001379 | 48.25 | gold quality |
| left ventricle myocardium | UBERON:0006566 | 48.24 | gold quality |
| orbitofrontal cortex | UBERON:0004167 | 48.20 | gold quality |
| upper arm skin | UBERON:0004263 | 48.06 | gold quality |
| cervix epithelium | UBERON:0004801 | 48.04 | gold quality |
| oviduct epithelium | UBERON:0004804 | 48.00 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 47.92 | gold quality |
| mucosa of urinary bladder | UBERON:0001259 | 47.80 | gold quality |
| metanephric glomerulus | UBERON:0004736 | 47.45 | gold quality |
| thymus | UBERON:0002370 | 47.42 | gold quality |
| kidney epithelium | UBERON:0004819 | 47.39 | gold quality |
| nephron tubule | UBERON:0001231 | 47.30 | gold quality |
| diaphragm | UBERON:0001103 | 47.05 | gold quality |
| gluteal muscle | UBERON:0002000 | 47.03 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 2.14 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): CEBPB
Literature-anchored findings (GeneRIF, showing 16)
- TAS2R16 is present in taste receptor cells on the tongue and is activated by bitter beta-glucopyranosides, and mediates bitter taste (PMID:12379855)
- Functional variant in a bitter-taste receptor (hTAS2R16) influences risk of alcohol dependence, especially in African-Americans. (PMID:16385453)
- Functional variants in both TAS2R16 and TAS2R38 correlate with alcohol consumption in African-American families. (PMID:17250611)
- molecular interaction between hTAS2R16 and beta-D-glucopyranoside (PMID:20605788)
- TAS2R16 is responsible for the bitterness of gentiobiose. (PMID:20965151)
- The authors discuss the association between the TAS2R16 gene and the evolution of bitter taste receptors in different populations. (PMID:21740153)
- Bitter taste receptor polymorphisms in TAS2R16 may be associated with human aging (PMID:23133589)
- Results showed that individuals with at least one derived T-allele at polymorphic site 516 have a higher sensitivity to salicin bitterness compared with individuals homozygous for the ancestral G-allele. (PMID:24177185)
- No significant association between rs702424 alleles and salicin bitter taste recognition, implying that this site does not contribute to salicin phenotypic variance. (PMID:24785689)
- Principal component analysis of binding energies for single-point mutants of hT2R16 bound to an agonist correlate with experimental mutant cell response. (PMID:25393978)
- genetic association studies in populations in Northern Europe, Maghreb, and Sri Lanka: Data suggest that SNPs in TAS2R50 (rs1376251), TRPM5 (rs800345), and TAS2R16 (rs860170) are associated with cultural food preferences; TAS2R16 (rs860170) strongly differentiates populations and is associated to salicin bitterness perception. (TRPM5 = transient receptor potential cation channel subfamily M member 5) (PMID:28366770)
- We did not find any statistically significant association between risk of developing sporadic colorectal cancer and selected single nucleotide polymorphisms. However, after stratification by histology (colon vs. rectum) we found that rs1525489 was associated with increased risk of rectal cancer with a (Ptrend of = 0.0071). (PMID:28915899)
- Dual binding mode of ““bitter sugars”” to their human bitter taste receptor target. (PMID:31186454)
- Suppression of hTAS2R16 Signaling by Umami Substances. (PMID:32987926)
- TAS2R16 Activation Suppresses LPS-Induced Cytokine Expression in Human Gingival Fibroblasts. (PMID:34975834)
- Association of TAS2R16 gene (rs860170, rs978739, rs1357949) polymorphisms and TAS2R16 serum levels in patients with age-related macular degeneration. (PMID:38111140)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | tas2r200.2 | ENSDARG00000074066 |
| danio_rerio | tas2r200.1 | ENSDARG00000079880 |
| mus_musculus | Tas2r118 | ENSMUSG00000043865 |
| rattus_norvegicus | Tas2r118 | ENSRNOG00000021799 |
Paralogs (23): TAS2R8 (ENSG00000121314), TAS2R10 (ENSG00000121318), TAS2R7 (ENSG00000121377), TAS2R9 (ENSG00000121381), TAS2R3 (ENSG00000127362), TAS2R4 (ENSG00000127364), TAS2R5 (ENSG00000127366), 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)
Protein
Protein identifiers
Taste receptor type 2 member 16 — Q9NYV7 (reviewed: Q9NYV7)
All UniProt accessions (2): Q9NYV7, A0A8E5KFD5
UniProt curated annotations — full annotation on UniProt →
Function. Gustducin-coupled receptor implicated in the perception of bitter compounds in the oral cavity and the gastrointestinal tract. Signals through PLCB2 and the calcium-regulated cation channel TRPM5.
Subunit / interactions. Interacts with RTP3 and RTP4.
Subcellular location. Cell membrane.
Tissue specificity. Expressed in a subset of gustducin-positive taste receptor cells of the tongue. Expressed in circumvallate papillae and testis.
Polymorphism. Genetic variation in TAS2R16 influences sensitivity to beta-glucopyranoside tasting (BGLPT) [MIM:617956]. Variant Asn-172 results in greater receptor activation in response to bitter beta-glucopyranoside compounds including salicin, arbutin and amygdalin compared to Lys-172. Variant Lys-172 may influence risk of alcohol dependence.
Miscellaneous. Several bitter taste receptors are expressed in a single taste receptor cell. Confers bitter perception of salicin to non-taster mice.
Similarity. Belongs to the G-protein coupled receptor T2R family.
RefSeq proteins (1): NP_058641* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR007960 | TAS2R | Family |
Pfam: PF05296
UniProt features (29 total): sequence variant 11, topological domain 8, transmembrane region 7, glycosylation site 2, chain 1
Structure
Experimental structures (PDB)
4 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 9K6L | ELECTRON MICROSCOPY | 2.77 |
| 9KPD | ELECTRON MICROSCOPY | 2.84 |
| 9KPF | ELECTRON MICROSCOPY | 3.15 |
| 9KPE | ELECTRON MICROSCOPY | 3.35 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9NYV7-F1 | 82.55 | 0.30 |
Antibody-complex structures (SAbDab): 4 — 9K6L, 9KPD, 9KPE, 9KPF
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 (2): 80, 163
Function
Pathways and Gene Ontology
Reactome pathways
9 pathways
| ID | Pathway |
|---|---|
| R-HSA-418594 | G alpha (i) signalling events |
| R-HSA-420499 | Class C/3 (Metabotropic glutamate/pheromone receptors) |
| R-HSA-9717207 | Sensory perception of sweet, bitter, and umami (glutamate) taste |
| R-HSA-162582 | Signal Transduction |
| R-HSA-372790 | Signaling by GPCR |
| R-HSA-388396 | GPCR downstream signalling |
| R-HSA-500792 | GPCR ligand binding |
| R-HSA-9709957 | Sensory Perception |
| R-HSA-9717189 | Sensory perception of taste |
MSigDB gene sets: 43 (showing top):
GOCC_CELL_SURFACE, GOBP_SENSORY_PERCEPTION_OF_CHEMICAL_STIMULUS, GOCC_TRANS_GOLGI_NETWORK, GOBP_DETECTION_OF_CHEMICAL_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION_OF_TASTE, GOBP_SENSORY_PERCEPTION_OF_TASTE, BLALOCK_ALZHEIMERS_DISEASE_UP, GOBP_DETECTION_OF_STIMULUS, GOBP_SENSORY_PERCEPTION, SHEN_SMARCA2_TARGETS_DN, GOCC_SIDE_OF_MEMBRANE, GOCC_ORGANELLE_SUBCOMPARTMENT, chr7q31, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_BITTER_TASTE_RECEPTOR_ACTIVITY, GOMF_TASTE_RECEPTOR_ACTIVITY
GO Biological Process (4): detection of chemical stimulus involved in sensory perception of bitter taste (GO:0001580), G protein-coupled receptor signaling pathway (GO:0007186), signal transduction (GO:0007165), sensory perception of taste (GO:0050909)
GO Molecular Function (3): G protein-coupled receptor activity (GO:0004930), bitter taste receptor activity (GO:0033038), protein binding (GO:0005515)
GO Cellular Component (5): endoplasmic reticulum (GO:0005783), trans-Golgi network (GO:0005802), plasma membrane (GO:0005886), external side of plasma membrane (GO:0009897), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-6 pathways:
| Category | Pathways |
|---|---|
| Signaling by GPCR | 2 |
| GPCR downstream signalling | 1 |
| GPCR ligand binding | 1 |
| Sensory perception of taste | 1 |
| Signal Transduction | 1 |
| Sensory Perception | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| detection of chemical stimulus involved in sensory perception of taste | 1 |
| sensory perception of bitter taste | 1 |
| G protein-coupled receptor activity | 1 |
| signal transduction | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| sensory perception of chemical stimulus | 1 |
| transmembrane signaling receptor activity | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| detection of chemical stimulus involved in sensory perception of bitter taste | 1 |
| taste receptor activity | 1 |
| binding | 1 |
| cytoplasm | 1 |
| endomembrane system | 1 |
| intracellular membrane-bounded organelle | 1 |
| Golgi apparatus subcompartment | 1 |
| membrane | 1 |
| cell periphery | 1 |
| plasma membrane | 1 |
| cell surface | 1 |
| side of membrane | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
550 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| TAS2R16 | TAS2R38 | P59533 | 939 |
| TAS2R16 | GNAT3 | A8MTJ3 | 758 |
| TAS2R16 | ADH7 | P40394 | 726 |
| TAS2R16 | CHRM2 | P08172 | 719 |
| TAS2R16 | ANKK1 | Q8NFD2 | 677 |
| TAS2R16 | TAS1R1 | Q7RTX1 | 667 |
| TAS2R16 | TAS1R3 | Q7RTX0 | 615 |
| TAS2R16 | ADH1A | P07327 | 590 |
| TAS2R16 | SSTR3 | P32745 | 575 |
| TAS2R16 | ADH6 | P28332 | 569 |
| TAS2R16 | GABRA6 | Q16445 | 549 |
| TAS2R16 | NRXN3 | Q9Y4C0 | 549 |
| TAS2R16 | ADH1B | P00325 | 548 |
| TAS2R16 | TAS1R2 | Q8TE23 | 535 |
| TAS2R16 | ADH5 | P11766 | 511 |
IntAct
0 interactions, top by confidence:
ESM2 similar proteins: P59529, P59533, P59534, P59535, P59551, Q645S2, Q645S5, Q645U1, Q645U4, Q645U5, Q645U6, Q645Y4, Q645Y7, Q645Y8, Q645Y9, Q645Z0, Q646A4, Q646A5, Q646A9, Q646B0, Q646B1, Q646B3, Q646C8, Q646D0, Q646D1, Q646D3, Q646D4, Q646E7, Q646F0, Q646F1, Q646F2, Q67ER9, Q67ES2, Q67ES3, Q67ES7, Q67ET0, Q67ET2, Q697L2, Q697L3, Q697L4
Diamond homologs: P59529, P59536, P59551, Q5Y4Z0, Q645S2, Q645U1, Q645U2, Q645U6, Q645U7, Q645Y3, Q645Y4, Q645Z0, Q646A5, Q646B2, Q646B3, Q646C7, Q646D0, Q646D1, Q646E7, Q646E8, Q646F1, Q646F3, Q646G6, Q67ES2, Q67ES3, Q67ES7, Q7M720, Q7TQA7, Q7TQA9, Q7TQB0, Q7TQB9, Q9JKE7, Q9JKF0, Q9JKT7, Q9JKU0, Q9NYV7, P59530, P59532, P59534, P59537
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
39 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 37 |
| Likely benign | 0 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
397 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 7:122995107:ATACT:A | acceptor_gain | 0.7700 |
| 7:122995655:T:A | donor_gain | 0.6900 |
| 7:122994977:T:A | donor_gain | 0.6700 |
| 7:122995354:C:CT | acceptor_gain | 0.6600 |
| 7:122994956:T:TA | donor_gain | 0.6300 |
| 7:122994808:A:T | acceptor_gain | 0.6200 |
| 7:122994958:A:AC | donor_gain | 0.6200 |
| 7:122994958:AGGG:A | donor_gain | 0.6200 |
| 7:122995280:TCA:T | acceptor_gain | 0.6200 |
| 7:122995109:ACT:A | acceptor_gain | 0.6100 |
| 7:122995587:AAG:A | donor_gain | 0.6100 |
| 7:122994807:C:CT | acceptor_gain | 0.5900 |
| 7:122995106:GATAC:G | acceptor_gain | 0.5900 |
| 7:122995454:A:AC | donor_gain | 0.5900 |
| 7:122995455:C:CC | donor_gain | 0.5900 |
| 7:122995587:A:AC | donor_gain | 0.5900 |
| 7:122995056:C:CT | acceptor_gain | 0.5800 |
| 7:122995108:TACTG:T | acceptor_gain | 0.5800 |
| 7:122995066:A:C | acceptor_gain | 0.5700 |
| 7:122995135:G:C | donor_gain | 0.5700 |
| 7:122995631:T:C | donor_gain | 0.5700 |
| 7:122995635:T:A | donor_gain | 0.5700 |
| 7:122994981:G:A | donor_gain | 0.5600 |
| 7:122995274:TC:T | donor_gain | 0.5600 |
| 7:122995275:CC:C | donor_gain | 0.5600 |
| 7:122995355:A:T | acceptor_gain | 0.5600 |
| 7:122995092:ATGAG:A | donor_gain | 0.5500 |
| 7:122995585:TCAAG:T | donor_gain | 0.5500 |
| 7:122995586:CAAGC:C | donor_gain | 0.5500 |
| 7:122995587:AAGCA:A | donor_gain | 0.5500 |
AlphaMissense
1927 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 7:122995344:G:C | S97R | 0.892 |
| 7:122995344:G:T | S97R | 0.892 |
| 7:122995346:T:G | S97R | 0.892 |
| 7:122994927:A:C | F236L | 0.838 |
| 7:122994927:A:T | F236L | 0.838 |
| 7:122994929:A:G | F236L | 0.838 |
| 7:122995482:G:C | S51R | 0.823 |
| 7:122995482:G:T | S51R | 0.823 |
| 7:122995484:T:G | S51R | 0.823 |
| 7:122995059:G:C | F192L | 0.804 |
| 7:122995059:G:T | F192L | 0.804 |
| 7:122995061:A:G | F192L | 0.804 |
| 7:122995560:G:C | S25R | 0.796 |
| 7:122995560:G:T | S25R | 0.796 |
| 7:122995562:T:G | S25R | 0.796 |
| 7:122995374:A:C | F87L | 0.771 |
| 7:122995374:A:T | F87L | 0.771 |
| 7:122995376:A:G | F87L | 0.771 |
| 7:122995356:G:C | F93L | 0.764 |
| 7:122995356:G:T | F93L | 0.764 |
| 7:122995358:A:G | F93L | 0.764 |
| 7:122995557:G:C | S26R | 0.742 |
| 7:122995557:G:T | S26R | 0.742 |
| 7:122995559:T:G | S26R | 0.742 |
| 7:122995290:A:C | F115L | 0.729 |
| 7:122995290:A:T | F115L | 0.729 |
| 7:122995292:A:G | F115L | 0.729 |
| 7:122995068:G:C | F189L | 0.723 |
| 7:122995068:G:T | F189L | 0.723 |
| 7:122995070:A:G | F189L | 0.723 |
dbSNP variants (sampled 300 via entrez): RS1000312684 (7:122996053 G>A), RS1000428852 (7:122996358 C>T), RS1000644068 (7:122997675 T>A), RS1002117094 (7:122995318 T>C), RS1003987559 (7:122996783 C>A), RS1004275947 (7:122996424 G>T), RS1006692683 (7:122997561 T>C), RS1008020443 (7:122996363 C>T), RS1008360858 (7:122996073 T>C), RS1008537221 (7:122997602 C>G), RS1010779455 (7:122996642 C>T), RS1011877165 (7:122994578 G>A), RS1014542922 (7:122997373 A>G), RS1014632527 (7:122997105 A>G), RS1014844821 (7:122996718 C>T)
Disease associations
OMIM: gene MIM:604867 | disease phenotypes: MIM:103780
GenCC curated gene-disease
Mondo (1): alcohol dependence (MONDO:0007079)
Orphanet (0):
HPO phenotypes
2 total (2 of 2 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0001426 | Non-Mendelian inheritance |
| HP:0030955 | Addictive alcohol use |
GWAS associations
0 associations (top):
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL3309106 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 40,234 (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 |
|---|---|---|---|
| CHEMBL434 | ISOPROTERENOL | 4 | 40,234 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB clinical annotations
1 annotations.
| Variant | Type | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| rs846664 | Toxicity | 3 | ethanol | Alcohol abuse |
PharmGKB variants
4 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs846664 | TAS2R16 | 3 | 1.50 | 1 | ethanol |
| rs860170 | TAS2R16 | 0.00 | 0 | ||
| rs978739 | TAS2R16 | 0.00 | 0 | ||
| rs1204014 | TAS2R16 | 0.00 | 0 |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: gpcr — Taste 2 receptors
Most potent curated ligand interactions (6 total), top 6:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| probenecid | Antagonist | 3.53 | pIC50 |
| 4-Nitrophenyl-β-D-mannopyranoside | Agonist | 3.19 | pEC50 |
| Phenyl-β-D-glucopyranoside | Agonist | 2.96 | pEC50 |
| salicin | Agonist | 2.85 | pEC50 |
| beta-gentiobiose | Agonist | 2.42 | pEC50 |
| D-(-)-Amygdalin | Agonist | 1.7 | pEC50 |
ChEMBL bioactivities
3 potent at pChembl≥5 of 3 total, top 3 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.31 | EC50 | 4.9 | nM | ISOPROTERENOL |
| 6.68 | EC50 | 210 | nM | CHEMBL4105357 |
| 6.60 | EC50 | 250 | nM | CHEMBL4105357 |
CTD chemical–gene interactions
9 total (human), top 9 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| salicin | decreases reaction, increases activity | 1 |
| sodium arsenite | affects methylation | 1 |
| 4-((diethylamino)sulfonyl)benzoic acid | decreases reaction, increases activity | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| Benzo(a)pyrene | affects methylation, decreases methylation | 1 |
| Probenecid | affects binding, decreases activity, decreases reaction, increases activity | 1 |
| Valproic Acid | decreases methylation | 1 |
| Aflatoxin B1 | decreases methylation | 1 |
| Asbestos, Crocidolite | affects expression | 1 |
ChEMBL screening assays
56 unique, capped per target: 54 functional, 2 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL3361954 | Binding | Agonist activity at human TAS2R16 expressed in U2OS cells by summary (Abse5) assay | Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). — Bioorg Med Chem Lett |
| CHEMBL4346431 | Functional | Antagonist activity at recombinant human TAS2R16 transiently expressed in HEK293T co-expressing Galpha16gust44 assessed as inhibition of salicin-induced intracellular calcium level by measuring remaining activity at 25 uM by fluo-4AM dye ba | Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists. — J Med Chem |
Clinical trials (associated diseases)
300 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00000437 | PHASE4 | COMPLETED | Tobacco Dependence in Alcoholism Treatment (Nicotine Patch/Naltrexone) |
| NCT00000438 | PHASE4 | COMPLETED | Naltrexone Treatment for Alcoholism |
| NCT00000441 | PHASE4 | COMPLETED | Drug Therapy for Alcohol Detoxification |
| NCT00000442 | PHASE4 | COMPLETED | Naltrexone for Relapse Prevention |
| NCT00000444 | PHASE4 | COMPLETED | Timing of Smoking Intervention in Alcohol Treatment (Nicotine Patch) |
| NCT00000445 | PHASE4 | COMPLETED | Use of Naltrexone in a Clinical Setting |
| NCT00000447 | PHASE4 | COMPLETED | Behavioral/Drug Therapy for Alcohol-Nicotine Dependence (Naltrexone/Nicotine Patch) |
| NCT00000448 | PHASE4 | COMPLETED | Naltrexone Treatment for Alcoholic Women |
| NCT00000449 | PHASE4 | COMPLETED | Behavior and Naltrexone Treatment for Alcoholics |
| NCT00000450 | PHASE4 | COMPLETED | Naltrexone Maintenance Treatment of Alcoholism |
| NCT00000452 | PHASE4 | COMPLETED | Naltrexone Treatment of Alcohol Dependence |
| NCT00000454 | PHASE4 | COMPLETED | Smoking Cessation in Alcoholism Treatment |
| NCT00000455 | PHASE4 | COMPLETED | Naltrexone for Early Problem Drinkers |
| NCT00000456 | PHASE4 | COMPLETED | Behavioral Therapy Plus Naltrexone for Alcoholism |
| NCT00004551 | PHASE4 | COMPLETED | Behavioral Counseling for Alcohol Dependent Smokers (Nicotine Patch) |
| NCT00004554 | PHASE4 | COMPLETED | Sertraline for Alcohol Dependence and Depression |
| NCT00006203 | PHASE4 | COMPLETED | Naltrexone, Craving, and Drinking |
| NCT00006204 | PHASE4 | COMPLETED | Drug Treatment for Depressed Alcoholics (Naltrexone/Fluoxetine) |
| NCT00006449 | PHASE4 | COMPLETED | Post-Treatment Effects of Naltrexone |
| NCT00006489 | PHASE4 | COMPLETED | Treatment for Alcoholism and Post-Traumatic Stress Disorder (Naltrexone) |
| NCT00018824 | PHASE4 | COMPLETED | Treating Alcohol Use In Older Adults With Depression |
| NCT00044434 | PHASE4 | COMPLETED | Bupropion as a Smoking Cessation Aid in Alcoholics |
| NCT00064844 | PHASE4 | COMPLETED | Combination Nicotine Replacement for Alcoholic Smokers |
| NCT00082199 | PHASE4 | COMPLETED | Study of Aripiprazole in Subjects With Alcoholism |
| NCT00115037 | PHASE4 | COMPLETED | Managing Alcoholism in People Who Do Not Respond to Naltrexone |
| NCT00120601 | PHASE4 | UNKNOWN | Trial for the Treatment of Alcohol Dependence |
| NCT00145847 | PHASE4 | COMPLETED | Naltrexone Treatment of Alcohol Abuse in Schizophrenia |
| NCT00148031 | PHASE4 | COMPLETED | Improving Hepatitis C Treatment in Injection Drug Users |
| NCT00159107 | PHASE4 | COMPLETED | Integrative Therapy in Alcoholism |
| NCT00167687 | PHASE4 | COMPLETED | Prazosin Alcohol Dependence IVR Study |
| NCT00223275 | PHASE4 | COMPLETED | Naltrexone for Bipolar Disorder and Alcohol Dependence |
| NCT00226109 | PHASE4 | SUSPENDED | Clinical Trial Studying the Effects of Spironolactone on Heart and Skeletal Muscle Function in Chronic Alcoholics |
| NCT00246441 | PHASE4 | COMPLETED | Paroxetine for Comorbid Social Anxiety Disorder and Alcoholism |
| NCT00249379 | PHASE4 | TERMINATED | Study of Acamprosate to Prevent Alcohol Relapse in Criminal Justice Supervisees |
| NCT00261872 | PHASE4 | COMPLETED | Treatment of Patients With Alcoholism and Attention Deficit Disorder |
| NCT00317031 | PHASE4 | COMPLETED | Individually Adapted Therapy of Alcoholism |
| NCT00325182 | PHASE4 | COMPLETED | The Effects of Levetiracetam on Alcohol Dependent Subjects |
| NCT00329407 | PHASE4 | COMPLETED | The Effects of Topiramate on Alcohol Use in Alcohol Dependent Subjects |
| NCT00330174 | PHASE4 | COMPLETED | Acamprosate in Alcoholics With Comorbid Anxiety or Depression |
| NCT00352469 | PHASE4 | COMPLETED | Trial of Seroquel SR for Alcohol Dependence and Comorbid Anxiety |
Related Atlas pages
- Targeted by drugs: Probenecid
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): alcohol dependence