TAS2R14

Summary

TAS2R14 (taste 2 receptor member 14, HGNC:14920) is a protein-coding gene on chromosome 12p13.2, encoding Taste receptor type 2 member 14 (Q9NYV8). Gustducin-linked G-protein coupled receptor that plays a role in the perception of bitterness.

This gene product belongs to the family of candidate taste receptors that are members of the G-protein-coupled receptor superfamily. These proteins are specifically expressed in the taste receptor cells of the tongue and palate epithelia. They are organized in the genome in clusters and are genetically linked to loci that influence bitter perception in mice and humans. In functional expression studies, they respond to bitter tastants. This gene maps to the taste receptor gene cluster on chromosome 12p13.

Source: NCBI Gene 50840 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 2 total
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_023922

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:14920
Approved symbol	TAS2R14
Name	taste 2 receptor member 14
Location	12p13.2
Locus type	gene with protein product
Status	Approved
Aliases	T2R14, TRB1
Ensembl gene	ENSG00000212127
Ensembl biotype	protein_coding
OMIM	604790
Entrez	50840

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 1 protein_coding_CDS_not_defined, 1 protein_coding

ENST00000381852, ENST00000537503

RefSeq mRNA: 2 — MANE Select: NM_023922 NM_001316893, NM_023922

CCDS: CCDS8637

Canonical transcript exons

ENST00000537503 — 1 exons

Exon	Start	End
ENSE00002238942	10937410	10939263

Expression profiles

Bgee: expression breadth ubiquitous, 132 present calls, max score 88.33.

FANTOM5 (CAGE): breadth broad, TPM avg 0.9242 / max 54.2742, expressed in 522 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
129604	0.9242	522

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	88.33	gold quality
corpus callosum	UBERON:0002336	77.97	gold quality
adrenal tissue	UBERON:0018303	77.03	gold quality
cerebellar hemisphere	UBERON:0002245	76.61	gold quality
cerebellar cortex	UBERON:0002129	76.51	gold quality
cerebellum	UBERON:0002037	76.24	gold quality
right hemisphere of cerebellum	UBERON:0014890	76.14	gold quality
right ovary	UBERON:0002118	73.01	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	72.88	gold quality
left ovary	UBERON:0002119	72.56	gold quality
endometrium	UBERON:0001295	72.39	gold quality
ovary	UBERON:0000992	72.17	gold quality
mucosa of stomach	UBERON:0001199	71.85	gold quality
body of uterus	UBERON:0009853	71.84	gold quality
monocyte	CL:0000576	71.52	gold quality
leukocyte	CL:0000738	71.18	gold quality
adenohypophysis	UBERON:0002196	71.06	gold quality
popliteal artery	UBERON:0002250	70.50	gold quality
tibial artery	UBERON:0007610	70.50	gold quality
myometrium	UBERON:0001296	70.36	gold quality
pituitary gland	UBERON:0000007	70.24	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	70.24	gold quality
granulocyte	CL:0000094	70.07	gold quality
left adrenal gland	UBERON:0001234	70.04	gold quality
bone marrow cell	CL:0002092	70.01	silver quality
muscle layer of sigmoid colon	UBERON:0035805	69.97	gold quality
left adrenal gland cortex	UBERON:0035825	69.92	gold quality
right adrenal gland cortex	UBERON:0035827	69.89	gold quality
adrenal gland	UBERON:0002369	69.88	gold quality
left lobe of thyroid gland	UBERON:0001120	69.82	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ENAD-17	no	98.15
E-ANND-3	no	0.92

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 21)

• no evidence of statistically significant associations between polymorphisms in the TAS2R14 gene and colon cancer risk (PMID:20534144)
• These results point to a potential route of action by which components of Hoodia might influence appetite control; the natural taste receptor antagonist was identified for further studies as an appetite suppressant. (PMID:20930049)
• TAS2R14 and TAS2R39 were activated by isoflavones and other isoflavonoids. (PMID:21942422)
• Probing the Binding Pocket of the Broadly Tuned Human Bitter Taste Receptor TAS2R14 by Chemical Modification of Cognate Agonists. (PMID:26825540)
• Thus the beta2AR acts as a double-edged sword: increasing TAS2R14 cell surface expression, but when activated by beta-agonist, partially offsetting the expression phenotype by direct receptor:receptor desensitization of TAS2R14 function. (PMID:27342779)
• These data indicate that, unlike in taste cells, TAS2Rs couple to the prevalent G proteins, Galphai1, Galphai2, and Galphai3, with no evidence for functional coupling to Galphagust. (PMID:28145731)
• Heterologously expressed T2R14 responds to multiple flavones. These flavones also activate T2R14-driven calcium signals in primary cells that activate nitric oxide production to increase ciliary beating and mucociliary clearance. (PMID:28373278)
• We observed that the homozygous carriers of the (G) allele of the TAS2R14-rs3741843 polymorphism showed a decreased sperm progressive motility compared to heterozygotes and (A) homozygotes. (PMID:29040583)
• results show that cholesterol influences the T2R14 signaling efficacy by forming direct interactions with the receptor and consequently plays a regulatory role in T2R14-mediated signaling in human airway cells. (PMID:30358435)
• TAS2R14 is subject to beta-arrestin-mediated internalization and subsequent down-regulation with chronic exposure to most agonists. (PMID:31430434)
• these results demonstrate that in contrast to membrane cholesterol, sphingomyelin does not affect the agonist-induced T2R14 signaling, however it may play a role in other aspects of T2R14 function. (PMID:31541354)
• Chemosensory bitter taste receptors T2R4 and T2R14 activation attenuates proliferation and migration of breast cancer cells. (PMID:31894529)
• The bitter taste receptor TAS2R14 regulates resveratrol transport across the human blood-cerebrospinal fluid barrier. (PMID:32272108)
• Identification of two bitter components in Zanthoxylum bungeanum Maxim. and exploration of their bitter taste mechanism through receptor hTAS2R14. (PMID:32818866)
• Functionally expressed bitter taste receptor TAS2R14 in human epidermal keratinocytes serves as a chemosensory receptor. (PMID:33253444)
• The short third intracellular loop and cytoplasmic tail of bitter taste receptors provide functionally relevant GRK phosphorylation sites in TAS2R14. (PMID:33465377)
• Bitter taste receptor T2R14 detects quorum sensing molecules from cariogenic Streptococcus mutans and mediates innate immune responses in gingival epithelial cells. (PMID:33559200)
• Neuropeptide Y Reduces Nasal Epithelial T2R Bitter Taste Receptor-Stimulated Nitric Oxide Production. (PMID:34684394)
• Identification and molecular docking of peptides from Mizuhopecten yessoensis myosin as human bitter taste receptor T2R14 blockers. (PMID:34747964)
• A Par3/LIM Kinase/Cofilin Pathway Mediates Human Airway Smooth Muscle Relaxation by TAS2R14. (PMID:36662576)
• Bitter taste TAS2R14 activation by intracellular tastants and cholesterol. (PMID:38776963)

Cross-species orthologs

22 orthologs

Organism	Symbol	Gene ID
mus_musculus	Tas2r116	ENSMUSG00000030194
mus_musculus	Tas2r103	ENSMUSG00000030196
mus_musculus	Tas2r113	ENSMUSG00000056926
mus_musculus	Tas2r123	ENSMUSG00000057381
mus_musculus	Tas2r117	ENSMUSG00000058349
mus_musculus	Tas2r125	ENSMUSG00000059410
mus_musculus	Tas2r109	ENSMUSG00000062528
mus_musculus	Tas2r110	ENSMUSG00000062952
mus_musculus	Tas2r129	ENSMUSG00000063762
mus_musculus	Tas2r140	ENSMUSG00000071147
mus_musculus	Tas2r115	ENSMUSG00000071149
rattus_norvegicus	Tas2r116	ENSRNOG00000021366
rattus_norvegicus	Tas2r125	ENSRNOG00000021397
rattus_norvegicus	Tas2r113	ENSRNOG00000030752
rattus_norvegicus	Tas2r129	ENSRNOG00000031107
rattus_norvegicus	Tas2r109	ENSRNOG00000032724
rattus_norvegicus	Tas2r140	ENSRNOG00000063462
rattus_norvegicus		ENSRNOG00000070504
rattus_norvegicus	Tas2r123	ENSRNOG00000080141
rattus_norvegicus	Tas2r117	ENSRNOG00000083980
rattus_norvegicus	Tas2r110	ENSRNOG00000086522
rattus_norvegicus		ENSRNOG00000090555

Paralogs (23): TAS2R8 (ENSG00000121314), TAS2R10 (ENSG00000121318), TAS2R7 (ENSG00000121377), TAS2R9 (ENSG00000121381), TAS2R3 (ENSG00000127362), TAS2R4 (ENSG00000127364), TAS2R5 (ENSG00000127366), TAS2R16 (ENSG00000128519), TAS2R1 (ENSG00000169777), TAS2R60 (ENSG00000185899), TAS2R42 (ENSG00000186136), TAS2R19 (ENSG00000212124), TAS2R50 (ENSG00000212126), 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 14 — Q9NYV8 (reviewed: Q9NYV8)

Alternative names: Taste receptor family B member 1

All UniProt accessions (1): Q9NYV8

UniProt curated annotations — full annotation on UniProt →

Function. Gustducin-linked G-protein coupled receptor that plays a role in the perception of bitterness. The activity of this receptor stimulates GNAT3, activating the gustducin G-protein pathway. Likely plays a role in sensing the chemical composition of the gastrointestinal content and other extra-oral tissues via the inhibitory G-protein pathways.

Subunit / interactions. Core component of the TAS2R14-GNAI1 complex, consisting of TAS2R14, GNAI1, GNB1 and GNG2; within the complex interacts with GNAI1. Core component of the TAS2R14-GNAT3 complex, consisting of TAS2R14, GNAT3, GNB1 and GNG2; within the complex interacts with GNAT3. Core component of the TAS2R14-GNAS2 complex, consisting of TAS2R14, GNAS2, GNB1 and GNG2; within the complex interacts with GNAS2.

Subcellular location. Membrane.

Tissue specificity. Highly expressed in cerebellum, pancreas, small intestine and thymus; also expressed in adipose, aorta, skin and tongue, but at significantly lower levels. Expressed in subsets of taste receptor cells of the tongue and palate epithelium and exclusively in gustducin-positive cells. Expressed in testis.

Activity regulation. Basal activity is enhanced by binding to bitter tastants, such as flufenamic acid and aristolochic acid. Regulated by cholesterol in a concentration-dependent manner.

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_076411* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR007960	TAS2R	Family

Pfam: PF05296

Catalyzed reactions (Rhea), 2 shown:

• Ca(2+)(in) = Ca(2+)(out) (RHEA:29671)
• 3’,5’-cyclic AMP(in) = 3’,5’-cyclic AMP(out) (RHEA:76223)

UniProt features (62 total): mutagenesis site 22, helix 13, topological domain 8, transmembrane region 7, binding site 5, glycosylation site 3, sequence variant 2, chain 1, strand 1

Structure

Experimental structures (PDB)

17 structures.

PDB	Method	Resolution (Å)
8VY7	ELECTRON MICROSCOPY	2.68
9IJ9	ELECTRON MICROSCOPY	2.7
8XQO	ELECTRON MICROSCOPY	2.77
8VY9	ELECTRON MICROSCOPY	2.88
9IIX	ELECTRON MICROSCOPY	2.89
8XQT	ELECTRON MICROSCOPY	2.94
8XQL	ELECTRON MICROSCOPY	2.99
8YKY	ELECTRON MICROSCOPY	2.99
8RQL	ELECTRON MICROSCOPY	3.03
8XQN	ELECTRON MICROSCOPY	3.05
9IJA	ELECTRON MICROSCOPY	3.05
9IIW	ELECTRON MICROSCOPY	3.15
8XQR	ELECTRON MICROSCOPY	3.2
9W0Q	ELECTRON MICROSCOPY	3.2
8XQP	ELECTRON MICROSCOPY	3.29
8XQS	ELECTRON MICROSCOPY	3.3
9W0P	ELECTRON MICROSCOPY	3.6

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9NYV8-F1	81.88	0.38

Antibody-complex structures (SAbDab): 11 — 8RQL, 8VY7, 8VY9, 8XQL, 8XQN, 8XQO, 8XQP, 8XQR, 8XQS, 8XQT, 8YKY

Functional residue map

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

Ligand- & substrate-binding residues (5): 86; 89; 180; 265; 268

Glycosylation sites (3): 153, 162, 171

Mutagenesis-validated functional residues (22):

Position	Phenotype
55	abolishes calcium mobilization induced by aristolochic acid and flufenamic acid.
65	impairs calcium mobilization induced by aristolochic acid and flufenamic acid. impairs calcium mobilization; when associ
82	impairs calcium mobilization induced by aristolochic acid and flufenamic acid.
89	abolishes basal activities of tas2r14-gnai1 and tas2r14-gnat3. abolishes activation of tas2r14-gnat3 by flufenamic acid
104	impairs calcium mobilization induced by aristolochic acid, flufenamic acid and flufenamic acid derivative cmpd28.1.
107	attenuates activation of tas2r14-gnat3 and tas2r14-gnai1 by flufenamic acid derivative cmpd28.1. abolishes calcium mobil
124	impairs calcium mobilization induced by aristolochic acid and flufenamic acid.
180	impairs calcium mobilization induced by aristolochic acid and flufenamic acid. impairs calcium mobilization; when associ
194	attenuates activation of tas2r14-gnat3 and tas2r14-gnai1 by flufenamic acid derivative cmpd28.1. impairs calcium mobiliz
198	impairs calcium mobilization induced by aristolochic acid, flufenamic acid and flufenamic acid derivative cmpd28.1.
205	impairs calcium mobilization induced by aristolochic acid and flufenamic acid. impairs calcium mobilization; when associ
208	impairs calcium mobilization induced by aristolochic acid and flufenamic acid.
229	abolishes calcium mobilization induced by aristolochic acid. impairs calcium mobilization induced by flufenamic acid and
230	impairs calcium mobilization induced by aristolochic acid and flufenamic acid. impairs calcium mobilization; when associ
233	impairs calcium mobilization induced by aristolochic acid, flufenamic acid and flufenamic acid derivative cmpd28.1.
236	attenuates activation of tas2r14-gnat3 and tas2r14-gnai1 flufenamic acid derivative cmpd28.1.
237	impairs calcium mobilization induced by aristolochic acid and flufenamic acid.
240	attenuates activation of tas2r14-gnat3 and tas2r14-gnai1 by flufenamic acid derivative cmpd28.1. abolishes calcium mobil
266	impairs calcium mobilization induced by aristolochic acid and flufenamic acid.
269	impairs calcium mobilization induced by aristolochic acid and flufenamic acid.
272	impairs calcium mobilization induced by aristolochic acid and flufenamic acid.
276	attenuates activation of tas2r14-gnat3 and tas2r14-gnai1 by flufenamic acid derivative cmpd28.1. abolishes calcium mobil

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: 89 (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, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_BITTER_TASTE_RECEPTOR_ACTIVITY, GOMF_TASTE_RECEPTOR_ACTIVITY, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, GREGORY_SYNTHETIC_LETHAL_WITH_IMATINIB, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_DETECTION_OF_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION, GOBP_SENSORY_PERCEPTION_OF_BITTER_TASTE, RAO_BOUND_BY_SALL4_ISOFORM_A, PGF_UP.V1_DN

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), taste receptor activity (GO:0008527), bitter taste receptor activity (GO:0033038)

GO Cellular Component (2): plasma membrane (GO:0005886), 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	2
transmembrane signaling receptor activity	2
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
G protein-coupled receptor signaling pathway	1
detection of chemical stimulus involved in sensory perception of bitter taste	1
taste receptor activity	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

468 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
TAS2R14	GNAT3	A8MTJ3	774
TAS2R14	TAS1R2	Q8TE23	513
TAS2R14	TAS1R3	Q7RTX0	505
TAS2R14	OR4F4	Q96R69	480
TAS2R14	OR2T33	Q8NG76	447
TAS2R14	OR10G8	Q8NGN5	444
TAS2R14	FAM229A	H3BQW9	433
TAS2R14	EDARADD	Q8WWZ3	425
TAS2R14	OR2D2	Q9H210	419
TAS2R14	OR52L1	Q8NGH7	419
TAS2R14	TRPM5	Q9NZQ8	412
TAS2R14	TAS1R1	Q7RTX1	408
TAS2R14	PLCB2	Q00722	400
TAS2R14	VN1R1	Q9GZP7	394
TAS2R14	HBE1	P02100	393

IntAct

3 interactions, top by confidence:

A	B	Type	Score
TAS2R14	ACP5	psi-mi:“MI:0915”(physical association)	0.400
TAS2R14	ATP5MG	psi-mi:“MI:0914”(association)	0.350

BioGRID (5): TAS2R14 (Affinity Capture-RNA), ACP5 (Affinity Capture-MS), ATP5B (Affinity Capture-MS), ATP5O (Affinity Capture-MS), ATP5L (Affinity Capture-MS)

ESM2 similar proteins: P59528, P59530, Q5Y4Z2, Q645T9, Q645U9, Q645V1, Q645Y5, Q645Z3, Q645Z5, Q646A7, Q646B6, Q646B8, Q646C6, Q646D2, Q646D8, Q646D9, Q646F7, Q646G3, Q646G5, Q675B7, Q675B8, Q675B9, Q675C0, Q67ER8, Q67ES1, Q67ES5, Q67ES6, Q67ES9, Q67ET3, Q67ET5, Q7M707, Q7M711, Q7M712, Q7M713, Q7M715, Q7M717, Q7M718, Q7M720, Q7M725, Q7RTR8

Diamond homologs: P0DSN6, P0DTE0, P59528, P59530, P59537, P59538, P59539, P59540, P59541, P59542, P59543, P59544, Q5Y4Y8, Q5Y4Y9, Q5Y4Z5, Q5Y4Z8, Q5Y500, Q645T0, Q645T2, Q645T3, Q645T4, Q645T6, Q645T7, Q645U8, Q645V1, Q645V2, Q645V3, Q645V4, Q645V6, Q645V7, Q645V8, Q645V9, Q645Z2, Q645Z5, Q645Z6, Q645Z7, Q645Z9, Q646A0, Q646A1, Q646A2

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	1
Likely benign	0
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

4259 predictions. Top by Δscore:

Variant	Effect	Δscore
12:10973719:CAG:C	acceptor_gain	1.0000
12:10973721:GC:G	acceptor_loss	1.0000
12:10973722:C:CC	acceptor_gain	1.0000
12:10973722:CTA:C	acceptor_loss	1.0000
12:11121181:C:CC	acceptor_gain	1.0000
12:10973650:GTTAC:G	donor_loss	0.9900
12:10973651:TTAC:T	donor_loss	0.9900
12:10973652:TACCT:T	donor_loss	0.9900
12:10973653:AC:A	donor_loss	0.9900
12:10973654:C:CT	donor_loss	0.9900
12:10973666:T:TA	donor_gain	0.9900
12:10973718:GCAG:G	acceptor_gain	0.9900
12:10973719:CAGC:C	acceptor_gain	0.9900
12:10973720:AG:A	acceptor_gain	0.9900
12:10973727:A:AC	acceptor_gain	0.9900
12:11124204:CAT:C	acceptor_gain	0.9900
12:11124206:T:TC	acceptor_gain	0.9900
12:11168611:G:C	donor_gain	0.9900
12:10969151:T:TA	donor_gain	0.9800
12:10969152:C:A	donor_gain	0.9800
12:10973655:C:A	donor_loss	0.9800
12:10973727:A:C	acceptor_gain	0.9800
12:10979962:A:AC	donor_gain	0.9800
12:10979963:G:C	donor_gain	0.9800
12:11048650:A:C	acceptor_gain	0.9800
12:11121185:G:C	acceptor_gain	0.9800
12:11171265:ACCGT:A	donor_gain	0.9800
12:11171266:CCGTC:C	donor_gain	0.9800
12:10973717:AGCAG:A	acceptor_gain	0.9700
12:10974789:CAGG:C	acceptor_gain	0.9700

AlphaMissense

2085 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:10938851:A:C	F119L	0.877
12:10938851:A:T	F119L	0.877
12:10938853:A:G	F119L	0.877
12:10939044:C:G	R55P	0.860
12:10939037:G:C	S57R	0.859
12:10939037:G:T	S57R	0.859
12:10939039:T:G	S57R	0.859
12:10938920:A:C	S96R	0.842
12:10938920:A:T	S96R	0.842
12:10938922:T:G	S96R	0.842
12:10939133:A:C	S25R	0.831
12:10939133:A:T	S25R	0.831
12:10939135:T:G	S25R	0.831
12:10939130:G:C	F26L	0.817
12:10939130:G:T	F26L	0.817
12:10939132:A:G	F26L	0.817
12:10938866:A:C	F114L	0.810
12:10938866:A:T	F114L	0.810
12:10938868:A:G	F114L	0.810
12:10939030:A:G	W60R	0.809
12:10939030:A:T	W60R	0.809
12:10938650:G:C	F186L	0.806
12:10938650:G:T	F186L	0.806
12:10938652:A:G	F186L	0.806
12:10938916:A:G	W98R	0.782
12:10938916:A:T	W98R	0.782
12:10938479:G:C	F243L	0.768
12:10938479:G:T	F243L	0.768
12:10938481:A:G	F243L	0.768
12:10939136:A:C	N24K	0.764

dbSNP variants (sampled 300 via entrez): RS1000493235 (12:10939423 C>T), RS1001238713 (12:10936946 C>T), RS1001964815 (12:10941139 G>A,T), RS1004678250 (12:10940199 A>C,G), RS1005544393 (12:10940228 A>G), RS1007683570 (12:10936947 T>A), RS1008843475 (12:10940227 C>A,T), RS1008972095 (12:10939547 G>T), RS1009269184 (12:10941047 C>G), RS1009402811 (12:10937808 C>G,T), RS1009508976 (12:10937296 A>G), RS1010518434 (12:10938715 A>T), RS1011612819 (12:10940018 GAAAA>G), RS1012162575 (12:10937629 C>T), RS1012499290 (12:10938820 C>T)

Disease associations

OMIM: gene MIM:604790 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST011124_22	Caffeine consumption from tea	7.000000e-13

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0010091	tea consumption measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3309105 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 75,031 (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
CHEMBL23588	FLUFENAMIC ACID	2	34,797

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Taste 2 receptors

Most potent curated ligand interactions (22 total), top 22:

Ligand	Action	Affinity	Parameter
flufenamic acid	Agonist	6.62	pEC50
aristolochic acid	Agonist	6.31	pEC50
lupulone	Agonist	5.89	pIC50
nobiletin	Agonist	5.68	pEC50
luteolin	Agonist	5.22	pEC50
santonin	Agonist	5.04	pEC50
datiscetin	Agonist	5.0	pEC50
parthenolide	Agonist	4.99	pEC50
(-)-α-thujone	Agonist	4.82	pEC50
picrotoxinin	Agonist	4.74	pEC50
N-octanoyl-L-homoserine lactone	Agonist	4.71	pEC50
phloretin	Agonist	4.52	pEC50
resveratrol	Agonist	4.52	pEC50
tributyrin	Agonist	4.49	pEC50
eriodictyol chalcone	Agonist	4.39	pEC50
(±)-Equol	Agonist	4.33	pEC50
silibinin	Agonist	4.25	pEC50
(+/-)-Eriodictyol	Agonist	4.21	pEC50
homoeriodictyol	Agonist	4.19	pEC50
genistein	Agonist	4.19	pEC50
coumestrol	Agonist	3.45	pEC50
vanillin	Agonist	3.24	pEC50

Binding affinities (BindingDB)

116 measured of 116 human assays (116 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
4-[[benzyl-(4-methylphenyl)sulfonylamino]methyl]cyclohexane-1-carboxylic acid	IC50	14 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(3-methoxyphenyl)methyl-(4-methylphenyl)sulfonylamino]methyl]cyclohexane-1-carboxylic acid	IC50	36 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(4-fluorophenyl)methyl-(4-methylphenyl)sulfonylamino]methyl]benzoic acid	IC50	54 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(4-fluorophenyl)methyl-(4-methylphenyl)sulfonylamino]methyl]cyclohexane-1-carboxylic acid	IC50	83 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(4-fluorophenyl)methyl-(4-methoxyphenyl)sulfonylamino]methyl]cyclohexane-1-carboxylic acid	IC50	92 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(4-methylphenyl)methyl-(4-methylphenyl)sulfonylamino]methyl]cyclohexane-1-carboxylic acid	IC50	109 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(4-hydroxyphenyl)sulfonyl-[(3-methoxyphenyl)methyl]amino]methyl]benzoic acid	IC50	188 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
BDBM50443972	IC50	220 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[benzenesulfonyl-[(4-fluorophenyl)methyl]amino]methyl]cyclohexane-1-carboxylic acid	IC50	240 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
MLS000052401	IC50	264 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
1,3,7-trimethyl-5-(2-oxo-2-piperidin-1-ylethyl)sulfanyl-4aH-pyrimido[4,5-d]pyrimidin-1-ium-2,4-dione	IC50	292 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
ethyl 4-[[(4-acetamidophenyl)sulfonyl-benzylamino]methyl]cyclohexane-1-carboxylate	IC50	334 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(4-fluorophenyl)methyl-thiophen-2-ylsulfonylamino]methyl]cyclohexane-1-carboxylic acid	IC50	342 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[benzenesulfonyl-[(3-methoxyphenyl)methyl]amino]methyl]benzoic acid	IC50	345 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-((N-benzyl-4-chlorophenylsulfonamido)methyl)benzoicacid	IC50	394 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[benzenesulfonyl-[(3-fluorophenyl)methyl]amino]methyl]benzoic acid	IC50	406 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[benzenesulfonyl-[(2-fluorophenyl)methyl]amino]methyl]benzoic acid	IC50	429 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(3-fluorophenyl)methyl-(4-hydroxyphenyl)sulfonylamino]methyl]benzoic acid	IC50	459 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(4-cyanophenyl)methyl-(4-methylphenyl)sulfonylamino]methyl]cyclohexane-1-carboxylic acid	IC50	499 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
(E)-2-cyano-3-(furan-2-yl)-N-(5-phenyl-1,3,4-thiadiazol-2-yl)prop-2-enamide	IC50	499 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[furan-2-ylmethyl-[(4-methoxyphenyl)methyl]sulfamoyl]benzoic acid	IC50	590 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
ethyl 4-[[benzyl-(4-chlorophenyl)sulfonylamino]methyl]cyclohexane-1-carboxylate	IC50	672 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[benzyl-[(3,4-dimethoxyphenyl)methyl]sulfamoyl]benzoic acid	IC50	678 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-1,3-dimethyl-2,4-dioxo-4a,5,6,7,8,8a-hexahydroquinazoline-6-sulfonamide	IC50	706 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
N-benzyl-2-[(1,3-dimethyl-2,4-dioxo-4a,5,6,7,8,8a-hexahydropyrido[2,3-d]pyrimidin-5-yl)sulfanyl]acetamide	IC50	710 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
7-ethyl-1,3-dimethyl-5-[2-(4-methylpiperidin-1-yl)-2-oxoethyl]sulfanyl-4aH-pyrimido[4,5-d]pyrimidin-1-ium-2,4-dione	IC50	721 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
ethyl 4-[2-[(7-ethyl-1,3-dimethyl-2,4-dioxo-4aH-pyrimido[4,5-d]pyrimidin-1-ium-5-yl)sulfanyl]acetyl]piperazine-1-carboxylate	IC50	763 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(4-acetamidophenyl)sulfonyl-[(4-fluorophenyl)methyl]amino]methyl]cyclohexane-1-carboxylic acid	IC50	842 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
N-ethyl-N-methyl-2-[(1,3,7-trimethyl-2,4-dioxo-4aH-pyrimido[4,5-d]pyrimidin-1-ium-5-yl)sulfanyl]acetamide	IC50	861 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[benzenesulfonyl-[(4-fluorophenyl)methyl]amino]methyl]benzoic acid	IC50	935 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
N-(3-fluoro-2-methylphenyl)-1,3-dimethyl-2,4-dioxo-4a,5,6,7,8,8a-hexahydroquinazoline-6-sulfonamide	IC50	935 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
1,3,7-trimethyl-5-(2-morpholin-4-yl-2-oxoethyl)sulfanyl-4aH-pyrimido[4,5-d]pyrimidin-1-ium-2,4-dione	IC50	1010 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[(3-fluoro-4-methoxyphenyl)methyl-[(4-methoxyphenyl)methyl]sulfamoyl]benzoic acid	IC50	1110 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[(2,4-difluorophenyl)methyl-[(4-methoxyphenyl)methyl]sulfamoyl]benzoic acid	IC50	1260 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[benzenesulfonyl-[(2-methoxyphenyl)methyl]amino]methyl]benzoic acid	IC50	1290 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[(4-methoxyphenyl)methyl-(1-phenylethyl)sulfamoyl]benzoic acid	IC50	1400 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[(3,4-dimethoxyphenyl)methyl-[(4-methoxyphenyl)methyl]sulfamoyl]benzoic acid	IC50	1470 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(4-acetamidophenyl)sulfonyl-benzylamino]methyl]cyclohexane-1-carboxylic acid	IC50	1620 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[(4-fluoro-3-methoxyphenyl)methyl-[(4-methoxyphenyl)methyl]sulfamoyl]benzoic acid	IC50	1650 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[(4-aminophenyl)sulfonyl-[(4-fluorophenyl)methyl]amino]methyl]cyclohexane-1-carboxylic acid	IC50	1650 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
1,3-dimethyl-N-(2-methylphenyl)-2,4-dioxo-4a,5,6,7,8,8a-hexahydroquinazoline-6-sulfonamide	IC50	1730 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[benzyl-[(4-cyanophenyl)methyl]sulfamoyl]benzoic acid	IC50	1850 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[(3-chlorophenyl)methyl-[(4-methoxyphenyl)methyl]sulfamoyl]benzoic acid	IC50	1880 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
N-(2-cyano-3,5-dimethylphenyl)-1,3-dimethyl-2,4-dioxo-4a,5,6,7,8,8a-hexahydroquinazoline-6-sulfonamide	IC50	1950 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[(4-fluorophenyl)methyl-[(4-methoxyphenyl)methyl]sulfamoyl]benzoic acid	IC50	1970 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[benzyl-[(4-methoxy-3-methylphenyl)methyl]sulfamoyl]benzoic acid	IC50	2000 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[1,3-benzodioxol-5-ylmethyl(benzyl)sulfamoyl]benzoic acid	IC50	2170 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[[benzenesulfonyl-[(4-methoxyphenyl)methyl]amino]methyl]benzoic acid	IC50	2220 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
N-benzyl-3-methoxy-N-[(4-methoxyphenyl)methyl]benzenesulfonamide	IC50	2220 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
4-[benzyl-[(3-methylphenyl)methyl]sulfamoyl]benzoic acid	IC50	2290 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof

ChEMBL bioactivities

177 potent at pChembl≥5 of 184 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.31	EC50	4.9	nM	ISOPROTERENOL
7.85	IC50	14	nM	CHEMBL3895068
7.44	IC50	36	nM	CHEMBL3909546
7.27	IC50	54	nM	CHEMBL3907785
7.14	EC50	72	nM	CHEMBL5279691
7.08	IC50	83	nM	CHEMBL3930803
7.04	IC50	92	nM	CHEMBL3905445
7.01	EC50	98	nM	CHEMBL5285591
7.00	EC50	100	nM	CHEMBL5275180
6.96	IC50	109	nM	CHEMBL3904387
6.82	EC50	150	nM	CHEMBL5273955
6.80	EC50	160	nM	CHEMBL5274304
6.77	EC50	170	nM	CHEMBL5277615
6.75	EC50	180	nM	CHEMBL5280542
6.73	IC50	188	nM	CHEMBL3901989
6.72	EC50	190	nM	CHEMBL3623735
6.72	EC50	190	nM	CHEMBL5279381
6.70	IC50	200	nM	CHEMBL3092287
6.66	IC50	220	nM	CHEMBL3092287
6.64	EC50	230	nM	CHEMBL3088246
6.62	IC50	240	nM	CHEMBL3946036
6.58	IC50	264	nM	CHEMBL1401915
6.54	IC50	292	nM	CHEMBL3962122
6.52	EC50	300	nM	CHEMBL5278834
6.52	EC50	300	nM	CHEMBL5277281
6.48	IC50	334	nM	CHEMBL3917592
6.48	EC50	330	nM	CHEMBL5278171
6.47	IC50	342	nM	CHEMBL3972175
6.46	IC50	345	nM	CHEMBL3954153
6.44	EC50	360	nM	CHEMBL5274470
6.42	EC50	380	nM	CHEMBL5278477
6.41	IC50	394	nM	CHEMBL1082389
6.41	EC50	390	nM	CHEMBL5275001
6.39	IC50	406	nM	CHEMBL3892321
6.38	EC50	420	nM	CHEMBL5289590
6.37	IC50	429	nM	CHEMBL3907807
6.37	EC50	430	nM	FLUFENAMIC ACID
6.34	IC50	459	nM	CHEMBL3976457
6.30	IC50	499	nM	CHEMBL3982886
6.30	IC50	499	nM	CHEMBL3908011
6.27	EC50	540	nM	CHEMBL5280688
6.23	IC50	590	nM	CHEMBL3894540
6.19	EC50	640	nM	CHEMBL5286379
6.19	EC50	640	nM	CHEMBL5268924
6.17	IC50	678	nM	CHEMBL3978302
6.17	IC50	672	nM	CHEMBL1356858
6.17	EC50	670	nM	CHEMBL5279341
6.15	IC50	706	nM	CHEMBL3945665
6.15	IC50	710	nM	CHEMBL3965603
6.14	IC50	721	nM	CHEMBL1499181

PubChem BioAssay actives

33 with measured affinity, of 77 total; 33 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
4-methyl-N-[2-(2H-tetrazol-5-yl)phenyl]-6-(trifluoromethyl)pyrimidin-2-amine	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.0720	uM
N-[2-(2H-tetrazol-5-yl)phenyl]-6-(trifluoromethyl)pyridin-2-amine	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.0980	uM
N-[2-(2H-tetrazol-5-yl)phenyl]-3,5-bis(trifluoromethyl)aniline	1947586: Partial agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.1000	uM
2-[3-ethynyl-5-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.1500	uM
N-[2-(2H-tetrazol-5-yl)phenyl]-4-(trifluoromethyl)pyrimidin-2-amine	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.1600	uM
2-[4-cyano-3-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.1700	uM
2-[3-cyano-5-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.1800	uM
2-[3-(pentafluoro-lambda6-sulfanyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.1900	uM
2-[3-methyl-5-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.1900	uM
2-[3-bromo-5-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.2300	uM
2-[2-(2H-tetrazol-5-yl)anilino]-6-(trifluoromethyl)pyrimidine-4-carbonitrile	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.3000	uM
2-[4-bromo-3-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.3000	uM
2-[4-methyl-3-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.3300	uM
N-[2-(2H-tetrazol-5-yl)phenyl]-4-(trifluoromethyl)pyridin-2-amine	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.3600	uM
2-[3-prop-1-ynyl-5-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.3800	uM
2-[2-methyl-5-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.3900	uM
2-[2-cyano-5-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.4200	uM
2-[3-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.4300	uM
4-chloro-N-[2-(2H-tetrazol-5-yl)phenyl]-6-(trifluoromethyl)pyrimidin-2-amine	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.5400	uM
4-tert-butyl-N-[2-(2H-tetrazol-5-yl)phenyl]-6-(trifluoromethyl)pyrimidin-2-amine	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.6400	uM
2-[2-bromo-5-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.6400	uM
2-[[6-(trifluoromethyl)-2-pyridinyl]amino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.6700	uM
4-iodo-N-[2-(2H-tetrazol-5-yl)phenyl]-6-(trifluoromethyl)pyrimidin-2-amine	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.7500	uM
2-[3-(difluoromethoxy)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.9300	uM
2-(3-chloroanilino)benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	0.9500	uM
N-[2-(2H-tetrazol-5-yl)phenyl]-2-(trifluoromethyl)pyrimidin-4-amine	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	1.1000	uM
2-[[5-(trifluoromethyl)-3-pyridinyl]amino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	1.2000	uM
4-ethynyl-N-[2-(2H-tetrazol-5-yl)phenyl]-6-(trifluoromethyl)pyrimidin-2-amine	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	1.4000	uM
2-[[4-(trifluoromethyl)pyrimidin-2-yl]amino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	1.6000	uM
2-[2-methyl-3-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	1.8000	uM
2-[2-bromo-3-(trifluoromethyl)anilino]benzoic acid	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	2.1000	uM
N-[2-(2H-tetrazol-5-yl)phenyl]-2-(trifluoromethyl)pyridin-4-amine	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	3.5000	uM
2-[2-(2H-tetrazol-5-yl)anilino]-4-(trifluoromethyl)-1H-pyrimidin-6-one	1947576: Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay	ec50	6.8000	uM

CTD chemical–gene interactions

20 total (human), top 20 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	decreases methylation, affects expression	2
Hydrogen Peroxide	affects cotreatment, increases expression, decreases expression	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Valproic Acid	increases expression	2
decabromobiphenyl ether	affects expression	1
butyraldehyde	decreases expression	1
pentanal	decreases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
dorsomorphin	decreases expression, affects cotreatment	1
jinfukang	affects cotreatment, decreases expression	1
Sunitinib	increases expression	1
Cisplatin	affects cotreatment, decreases expression	1
Dimethyl Sulfoxide	affects expression	1
Selenium	affects cotreatment, decreases expression	1
Silicon Dioxide	increases expression	1
Dronabinol	decreases expression	1
Theophylline	increases expression, affects cotreatment	1
Vitamin E	decreases expression, affects cotreatment	1
Asbestos, Crocidolite	affects expression	1
S-Nitrosoglutathione	increases expression	1

ChEMBL screening assays

20 unique, capped per target: 12 binding, 8 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3361952	Binding	Agonist activity at human TAS2R14 expressed in U2OS cells by Ga16gust44 Clone 7A FLIPR/summary (Abse5) assay	Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). — Bioorg Med Chem Lett
CHEMBL4346430	Functional	Antagonist activity at recombinant human TAS2R14 transiently expressed in HEK293T co-expressing Galpha16gust44 assessed as inhibition of aristolochic acid-induced intracellular calcium level by measuring remaining activity at 25 uM by fluo-	Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists. — J Med Chem

Clinical trials (associated diseases)

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