TAS2R8

Summary

TAS2R8 (taste 2 receptor member 8, HGNC:14915) is a protein-coding gene on chromosome 12p13.2, encoding Taste receptor type 2 member 8 (Q9NYW2). Receptor that may play a role in the perception of bitterness and is gustducin-linked.

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 50836 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 44 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_023918

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:14915
Approved symbol	TAS2R8
Name	taste 2 receptor member 8
Location	12p13.2
Locus type	gene with protein product
Status	Approved
Aliases	T2R8, TRB5
Ensembl gene	ENSG00000121314
Ensembl biotype	protein_coding
OMIM	604794
Entrez	50836

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000240615

RefSeq mRNA: 1 — MANE Select: NM_023918 NM_023918

CCDS: CCDS8632

Canonical transcript exons

ENST00000240615 — 1 exons

Exon	Start	End
ENSE00000821985	10806051	10807286

Expression profiles

Bgee: expression breadth tissue_specific, 8 present calls, max score 40.63.

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
cortical plate	UBERON:0005343	40.63	silver quality
bone marrow cell	CL:0002092	38.90	gold quality
colonic epithelium	UBERON:0000397	37.20	gold quality
granulocyte	CL:0000094	36.86	gold quality
primary visual cortex	UBERON:0002436	36.50	silver quality
ventricular zone	UBERON:0003053	36.48	gold quality
mucosa of transverse colon	UBERON:0004991	35.96	gold quality
skeletal muscle tissue	UBERON:0001134	35.34	gold quality
cerebellar hemisphere	UBERON:0002245	33.83	gold quality
right hemisphere of cerebellum	UBERON:0014890	33.82	gold quality
cerebellar cortex	UBERON:0002129	33.75	gold quality
cerebellum	UBERON:0002037	33.70	gold quality
prefrontal cortex	UBERON:0000451	33.64	silver quality
duodenum	UBERON:0002114	33.21	silver quality
bone marrow	UBERON:0002371	33.14	gold quality
muscle tissue	UBERON:0002385	32.50	gold quality
hindlimb stylopod muscle	UBERON:0004252	32.15	gold quality
corpus callosum	UBERON:0002336	31.77	gold quality
endometrium	UBERON:0001295	31.58	gold quality
metanephros cortex	UBERON:0010533	31.25	gold quality
frontal cortex	UBERON:0001870	31.24	silver quality
sural nerve	UBERON:0015488	30.93	gold quality
islet of Langerhans	UBERON:0000006	30.60	silver quality
liver	UBERON:0002107	30.60	gold quality
stromal cell of endometrium	CL:0002255	29.87	gold quality
cortex of kidney	UBERON:0001225	29.73	gold quality
right adrenal gland cortex	UBERON:0035827	29.73	gold quality
right adrenal gland	UBERON:0001233	29.70	silver quality
leukocyte	CL:0000738	29.62	gold quality
gall bladder	UBERON:0002110	29.35	silver quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 3)

• Human bitter taste receptors hTAS2R8 and hTAS2R39 display differential functions to recognize bitter peptides. (PMID:21670512)
• targets cancer stem cells by suppressing cancer stemness characteristics and neuroblastoma cell invasion (PMID:28467517)
• Intracellular zinc-dependent TAS2R8 gene expression through CTCF activation. (PMID:33071257)

Cross-species orthologs

0 orthologs

Paralogs (23): TAS2R10 (ENSG00000121318), TAS2R7 (ENSG00000121377), TAS2R9 (ENSG00000121381), TAS2R3 (ENSG00000127362), TAS2R4 (ENSG00000127364), TAS2R5 (ENSG00000127366), 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)

Protein

Protein identifiers

Taste receptor type 2 member 8 — Q9NYW2 (reviewed: Q9NYW2)

Alternative names: Taste receptor family B member 5

All UniProt accessions (1): Q9NYW2

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_076407* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR007960	TAS2R	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF05296

UniProt features (18 total): topological domain 8, transmembrane region 7, chain 1, glycosylation site 1, sequence variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9NYW2-F1	81.73	0.30

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): 167

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: 33 (showing top): GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_MCMV_INFECTION_DN, 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, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_DETECTION_OF_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION, GOBP_SENSORY_PERCEPTION_OF_BITTER_TASTE, GSE13411_IGM_VS_SWITCHED_MEMORY_BCELL_DN, REACTOME_SENSORY_PERCEPTION

GO Biological Process (4): detection of chemical stimulus involved in sensory perception of bitter taste (GO:0001580), 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

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
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
G protein-coupled receptor activity	1
signal transduction	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
binding	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

232 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
TAS2R8	GNAT3	A8MTJ3	811
TAS2R8	WBP2NL	Q6ICG8	324
TAS2R8	TAS1R2	Q8TE23	294
TAS2R8	PLCB2	Q00722	290
TAS2R8	TRPM5	Q9NZQ8	282
TAS2R8	SSTR3	P32745	271
TAS2R8	CCDC93	Q567U6	270
TAS2R8	PPHLN1	Q8NEY8	266
TAS2R8	TAS1R3	Q7RTX0	264
TAS2R8	TAS1R1	Q7RTX1	264
TAS2R8	SLC13A2	Q13183	260
TAS2R8	PIP4K2C	Q8TBX8	255
TAS2R8	TAS2R4	Q9NYW5	241
TAS2R8	TAS2R5	Q9NYW4	237
TAS2R8	TAS2R16	Q9NYV7	236

IntAct

6 interactions, top by confidence:

A	B	Type	Score
NHERF4	TAS2R8	psi-mi:“MI:0915”(physical association)	0.560
TAS2R8	SERPINB8	psi-mi:“MI:0915”(physical association)	0.400
TAS2R8	NEIL1	psi-mi:“MI:0914”(association)	0.350
TAS2R8	NHERF4	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (4): SERPINB8 (Affinity Capture-MS), PDZD3 (Two-hybrid), ITFG3 (Affinity Capture-MS), NEIL1 (Affinity Capture-MS)

ESM2 similar proteins: Q2AB83, Q5J3E5, Q5J3F6, Q5J3G9, Q5J3K5, Q5J3K9, Q5J3L4, Q5J3L6, Q5J3L7, Q5J3M3, Q5J3M4, Q5J3M9, Q5J3N1, Q62850, Q646A3, Q646C5, Q646E5, Q646G4, Q646G6, Q646G9, Q646H0, Q67ET7, Q7M709, Q7M722, Q7M724, Q7TQA7, Q7TQA8, Q7YRP3, Q8R2E6, Q8TDU5, Q8VBS7, Q8VIC6, Q8VIC7, Q8VIC9, Q8WN92, Q9BXE9, Q9EP51, Q9EP79, Q9EP93, Q9EPB8

Diamond homologs: P0DSN6, P0DTE0, P59528, P59530, P59537, P59538, P59539, P59540, P59541, P59542, P59543, P59544, Q5Y4Y8, Q5Y4Y9, Q5Y4Z5, Q5Y4Z8, Q5Y500, Q645T2, Q645T3, Q645T4, Q645T6, Q645T7, Q645U8, Q645V1, Q645V2, Q645V3, Q645V4, Q645V6, Q645V7, Q645V8, Q645Z2, Q645Z5, Q645Z6, Q645Z7, Q645Z9, Q646A0, Q646A1, Q646A2, Q646B4, Q646B5

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	38
Likely benign	5
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

224 predictions. Top by Δscore:

Variant	Effect	Δscore
12:10806368:C:CC	acceptor_gain	0.7500
12:10806364:CTTA:C	acceptor_gain	0.7300
12:10806460:A:AC	donor_gain	0.6900
12:10806461:C:CC	donor_gain	0.6900
12:10807164:CTC:C	acceptor_gain	0.6500
12:10806365:TTA:T	acceptor_gain	0.6400
12:10807162:CACTC:C	acceptor_gain	0.6200
12:10806461:CAT:C	donor_gain	0.6000
12:10806456:A:AC	donor_gain	0.5900
12:10806457:C:CC	donor_gain	0.5900
12:10806458:TCA:T	donor_loss	0.5600
12:10806459:CACA:C	donor_loss	0.5600
12:10806460:ACATG:A	donor_loss	0.5600
12:10806461:C:A	donor_loss	0.5600
12:10806453:TTTAC:T	donor_loss	0.5500
12:10806454:TTACT:T	donor_loss	0.5500
12:10806455:TAC:T	donor_loss	0.5500
12:10806456:AC:A	donor_loss	0.5500
12:10806593:C:CT	donor_gain	0.5500
12:10806461:CA:C	donor_gain	0.5200
12:10806461:CATG:C	donor_gain	0.5200
12:10806524:TCAG:T	donor_gain	0.5200
12:10806619:C:CT	acceptor_gain	0.5200
12:10807247:TGATA:T	donor_loss	0.5100
12:10807248:GATAC:G	donor_loss	0.5100
12:10807249:ATACC:A	donor_loss	0.5100
12:10807250:TAC:T	donor_loss	0.5100
12:10807251:A:AC	donor_loss	0.5100
12:10807252:C:CG	donor_loss	0.5100
12:10807253:C:A	donor_loss	0.4800

AlphaMissense

2056 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:10806546:G:C	S145R	0.915
12:10806546:G:T	S145R	0.915
12:10806548:T:G	S145R	0.915
12:10806801:A:C	S60R	0.848
12:10806801:A:T	S60R	0.848
12:10806803:T:G	S60R	0.848
12:10806624:A:C	F119L	0.806
12:10806624:A:T	F119L	0.806
12:10806626:A:G	F119L	0.806
12:10806663:G:C	F106L	0.776
12:10806663:G:T	F106L	0.776
12:10806665:A:G	F106L	0.776
12:10806261:A:C	F240L	0.772
12:10806261:A:T	F240L	0.772
12:10806263:A:G	F240L	0.772
12:10806816:T:A	R55S	0.730
12:10806816:T:G	R55S	0.730
12:10806812:A:G	C57R	0.729
12:10806213:A:C	F256L	0.723
12:10806213:A:T	F256L	0.723
12:10806215:A:G	F256L	0.723
12:10806909:A:C	N24K	0.704
12:10806909:A:T	N24K	0.704
12:10806572:A:G	C137R	0.692
12:10806923:C:G	G20R	0.684
12:10806923:C:T	G20R	0.684
12:10806693:A:C	N96K	0.678
12:10806693:A:T	N96K	0.678
12:10806507:A:C	F158L	0.664
12:10806507:A:T	F158L	0.664

dbSNP variants (sampled 300 via entrez): RS1000073345 (12:10807127 G>A,T), RS1000444586 (12:10807966 G>T), RS1001130935 (12:10807474 C>G), RS1002122124 (12:10808641 G>T), RS1002409368 (12:10806628 A>G), RS1002424854 (12:10808462 G>C), RS1003061166 (12:10806025 T>A,C), RS1004117875 (12:10805652 T>C), RS1006352063 (12:10809042 T>C,G), RS1006575469 (12:10807295 G>A,T), RS1008740374 (12:10805665 A>G), RS1010001241 (12:10807618 T>C), RS1010024965 (12:10808424 C>G,T), RS1011163456 (12:10807025 G>A,T), RS1012223866 (12:10807971 G>A)

Disease associations

OMIM: gene MIM:604794 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3988599 (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)

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Taste 2 receptors

Most potent curated ligand interactions (4 total), top 4:

Ligand	Action	Affinity	Parameter
S6821	Antagonist	7.7	pIC50
S7958	Antagonist	7.22	pIC50
oleuropein	Agonist	4.24	pEC50
andrographolide	Agonist	3.96	pEC50

Binding affinities (BindingDB)

306 measured of 307 human assays (307 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
4-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[2-(4-fluorophenyl)ethyl]-2-methyl-1,2,4-triazolidine-3,5-dione	IC50	10 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[2-(4-fluorophenyl)ethyl]imidazolidine-2,4-dione	IC50	10 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-[(3,5-dihydroxyphenyl)methyl]-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-5,5-dimethylimidazolidine-2,4-dione	IC50	10 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
(5S)-1-benzyl-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-5-methylimidazolidine-2,4-dione	IC50	10 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(4-fluoro-3-hydroxyphenyl)methyl]-5,5-dimethylimidazolidine-2,4-dione	IC50	10 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
(5R)-1-benzyl-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-5-methylimidazolidine-2,4-dione	IC50	10 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-[(2-aminophenyl)methyl]-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]imidazolidine-2,4-dione	IC50	20 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-benzyl-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-5-methylimidazolidine-2,4-dione	IC50	20 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-benzyl-4-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2-methyl-1,2,4-triazolidine-3,5-dione	IC50	20 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-benzyl-4-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2-(methoxymethyl)-1,2,4-triazolidine-3,5-dione	IC50	20 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
(5S)-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-hydroxyphenyl)methyl]-5-methylimidazolidine-2,4-dione	IC50	20 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
(5R)-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-hydroxyphenyl)methyl]-5-methylimidazolidine-2,4-dione	IC50	20 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
6-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-4-[(3-hydroxy-4-methoxyphenyl)methyl]-4,6-diazaspiro[2.4]heptane-5,7-dione	IC50	20 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]-6-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-4,6-diazaspiro[2.4]heptane-5,7-dione	IC50	20 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
6-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-4-[(3-hydroxyphenyl)methyl]-4,6-diazaspiro[2.4]heptane-5,7-dione	IC50	20 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-hydroxy-5-methoxyphenyl)methyl]-5,5-dimethylimidazolidine-2,4-dione	IC50	20 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
(10aS)-2-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-7-hydroxy-10,10a-dihydro-5H-imidazo[1,5-b]isoquinoline-1,3-dione	IC50	20 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-hydroxyphenyl)methyl]imidazolidine-2,4-dione	IC50	30 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(2-methylsulfanylphenyl)methyl]imidazolidine-2,4-dione	IC50	30 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-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-5-[(3-hydroxyphenyl)methyl]-5,7-diazaspiro[3.4]octane-6,8-dione	IC50	30 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
6-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-4-[[3-(methoxymethyl)phenyl]methyl]-4,6-diazaspiro[2.4]heptane-5,7-dione	IC50	30 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
(10aR)-2-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-7-hydroxy-10,10a-dihydro-5H-imidazo[1,5-b]isoquinoline-1,3-dione	IC50	30 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
2-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-8-hydroxy-10,10a-dihydro-5H-imidazo[1,5-b]isoquinoline-1,3-dione	IC50	30 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-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-methyl-2-(2-phenoxyethyl)-1,2,4-triazolidine-3,5-dione	IC50	31 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-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]imidazolidine-2,4-dione	IC50	40 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[2-(4-methoxyphenyl)ethyl]imidazolidine-2,4-dione	IC50	40 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-benzyl-4-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2-ethyl-1,2,4-triazolidine-3,5-dione	IC50	40 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
(5S)-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-5-(hydroxymethyl)-1-[(3-hydroxyphenyl)methyl]imidazolidine-2,4-dione	IC50	40 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-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-5,5-dimethyl-2,4-dioxoimidazolidin-1-yl]methyl]benzonitrile	IC50	40 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(4-fluorophenyl)methyl]imidazolidine-2,4-dione	IC50	50 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-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2,4-dioxoimidazolidin-1-yl]methyl]benzonitrile	IC50	50 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-hydroxyphenyl)methyl]-5,5-dimethylimidazolidine-2,4-dione	IC50	50 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-(2-phenoxyethyl)imidazolidine-2,4-dione	IC50	60 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(4-hydroxyphenyl)methyl]imidazolidine-2,4-dione	IC50	60 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(2-methoxyphenyl)methyl]imidazolidine-2,4-dione	IC50	60 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-fluorophenyl)methyl]imidazolidine-2,4-dione	IC50	60 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(4-methylphenyl)methyl]imidazolidine-2,4-dione	IC50	60 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-[(3,4-dimethoxyphenyl)methyl]-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]imidazolidine-2,4-dione	IC50	60 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[2-(3-fluorophenyl)ethyl]imidazolidine-2,4-dione	IC50	60 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-benzyl-4-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2-(2-methoxyethyl)-1,2,4-triazolidine-3,5-dione	IC50	60 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-benzyl-4-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2-propyl-1,2,4-triazolidine-3,5-dione	IC50	60 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-hydroxy-4-methoxyphenyl)methyl]-5,5-dimethylimidazolidine-2,4-dione	IC50	60 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-methoxyphenyl)methyl]imidazolidine-2,4-dione	IC50	70 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(2-hydroxyphenyl)methyl]imidazolidine-2,4-dione	IC50	70 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[[3-(2-methoxyethoxy)phenyl]methyl]imidazolidine-2,4-dione	IC50	70 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(2-nitrophenyl)methyl]imidazolidine-2,4-dione	IC50	70 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(4-methoxyphenyl)methyl]imidazolidine-2,4-dione	IC50	70 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-(1,3-benzodioxol-5-ylmethyl)-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]imidazolidine-2,4-dione	IC50	70 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-hydroxyphenyl)methyl]-1,3-diazaspiro[4.4]nonane-2,4-dione	IC50	70 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
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(4-hydroxyphenyl)methyl]-5,5-dimethylimidazolidine-2,4-dione	IC50	70 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

366 potent at pChembl≥5 of 371 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
8.00	IC50	10	nM	CHEMBL3950223
8.00	IC50	10	nM	CHEMBL3976506
8.00	IC50	10	nM	CHEMBL3898803
8.00	IC50	10	nM	CHEMBL3923956
8.00	IC50	10	nM	CHEMBL3939399
8.00	IC50	10	nM	CHEMBL4112934
7.70	IC50	20	nM	CHEMBL3890262
7.70	IC50	20	nM	CHEMBL3979194
7.70	IC50	20	nM	CHEMBL3935648
7.70	IC50	20	nM	CHEMBL3939695
7.70	IC50	20	nM	CHEMBL3933031
7.70	IC50	20	nM	CHEMBL4108527
7.70	IC50	20	nM	CHEMBL3902192
7.70	IC50	20	nM	CHEMBL3939063
7.70	IC50	20	nM	CHEMBL3961116
7.70	IC50	20	nM	CHEMBL3949830
7.70	IC50	20	nM	CHEMBL3964034
7.70	IC50	20	nM	CHEMBL3924866
7.52	IC50	30	nM	CHEMBL3911337
7.52	IC50	30	nM	CHEMBL3970005
7.52	IC50	30	nM	CHEMBL3911969
7.52	IC50	30	nM	CHEMBL4113151
7.52	IC50	30	nM	CHEMBL3935598
7.52	IC50	30	nM	CHEMBL3924866
7.51	IC50	31	nM	CHEMBL3945679
7.46	IC50	35	nM	CHEMBL3924866
7.40	IC50	40	nM	CHEMBL3941028
7.40	IC50	40	nM	CHEMBL3896760
7.40	IC50	40	nM	CHEMBL3948447
7.40	IC50	40	nM	CHEMBL3915586
7.40	IC50	40	nM	CHEMBL3892490
7.40	IC50	40	nM	CHEMBL3948082
7.40	IC50	40	nM	CHEMBL3970005
7.30	IC50	50	nM	CHEMBL3908407
7.30	IC50	50	nM	CHEMBL3979603
7.30	IC50	50	nM	CHEMBL3907822
7.30	IC50	50	nM	CHEMBL3892490
7.22	IC50	60	nM	CHEMBL3919358
7.22	IC50	60	nM	CHEMBL3948082
7.22	IC50	60	nM	CHEMBL3979660
7.22	IC50	60	nM	CHEMBL3900806
7.22	IC50	60	nM	CHEMBL3932834
7.22	IC50	60	nM	CHEMBL3955923
7.22	IC50	60	nM	CHEMBL3932036
7.22	IC50	60	nM	CHEMBL3926125
7.22	IC50	60	nM	CHEMBL3953765
7.22	IC50	60	nM	CHEMBL3981387
7.22	IC50	60	nM	CHEMBL3907822
7.16	IC50	70	nM	CHEMBL3897715

PubChem BioAssay actives

55 with measured affinity, of 62 total; 50 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
6-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-4-[(3-hydroxyphenyl)methyl]-4,6-diazaspiro[2.4]heptane-5,7-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.0200	uM
(5S)-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-hydroxyphenyl)methyl]-5-methylimidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.0200	uM
(5R)-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-hydroxyphenyl)methyl]-5-methylimidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.0200	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-hydroxyphenyl)methyl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.0200	uM
7-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-5-[(3-hydroxyphenyl)methyl]-5,7-diazaspiro[3.4]octane-6,8-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.0400	uM
(5S)-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-5-(hydroxymethyl)-1-[(3-hydroxyphenyl)methyl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.0400	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(4-hydroxyphenyl)methyl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.0400	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(3-hydroxyphenyl)methyl]-5,5-dimethylimidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.0600	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-5-(hydroxymethyl)-1-[(3-hydroxyphenyl)methyl]-5-methylimidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.1000	uM
methyl 3-[[3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2,4-dioxoimidazolidin-1-yl]methyl]benzoate	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.1000	uM
3-[[3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2,4-dioxoimidazolidin-1-yl]methyl]-N-methylbenzamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.1000	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(2-hydroxyphenyl)methyl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.1000	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(2-methoxyphenyl)methyl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.1000	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(2-methylphenyl)methyl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.1000	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(2-fluorophenyl)methyl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.1000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1,3-benzodioxole-5-carboxamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.2000	uM
2-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]isoindole-1,3-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.2000	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[(2,5-dimethylpyrazol-3-yl)methyl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.2000	uM
1-benzyl-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.2000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1H-indole-5-carboxamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.3000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2,5-dimethoxybenzamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.3000	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-[[3-(hydroxymethyl)phenyl]methyl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.3000	uM
1-(cyclohexylmethyl)-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.3000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-3-hydroxybenzamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.4000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-3-phenylpropanamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.4000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2,3-dihydro-1,4-benzodioxine-6-carboxamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.4000	uM
1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.4000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-4-hydroxybenzamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.5000	uM
2-[[3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2,4-dioxoimidazolidin-1-yl]methyl]benzonitrile	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.5000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-6-methoxypyridine-2-carboxamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.7000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-3-methoxybenzamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.7000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-4-methoxybenzamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.7000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-5-methoxypyridine-3-carboxamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.8000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2-phenylacetamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.8000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-4-phenylbutanamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.8000	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	0.9000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2-hydroxybenzamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	1.0000	uM
1-benzyl-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]urea	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	1.0000	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-(pyridin-2-ylmethyl)imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	1.0000	uM
1-benzyl-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]imidazolidin-2-one	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	1.0000	uM
3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-1-(oxolan-2-ylmethyl)imidazolidine-2,4-dione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	1.0000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-3,4-dimethoxybenzamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	1.0000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2-methoxypyridine-3-carboxamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	1.1000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]pyridine-3-carboxamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	1.1000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]benzamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	1.7000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2-methoxybenzamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	1.9000	uM
1-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-3-phenylurea	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	2.0000	uM
3-[[3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2,4-dioxoimidazolidin-1-yl]methyl]benzoic acid	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	2.0000	uM
1-benzyl-3-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]imidazolidine-2,4,5-trione	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	2.0000	uM
N-[1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]pyrazol-4-yl]-2-ethylsulfanylpyridine-3-carboxamide	1549014: Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay	ic50	2.3000	uM

CTD chemical–gene interactions

7 total (human), top 7 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
perfluorooctanoic acid	increases expression	1
CGP 52608	affects binding, increases reaction	1
perfluoro-n-nonanoic acid	increases expression	1
Acetaminophen	increases expression	1
Benzo(a)pyrene	increases methylation	1
Phthalic Acids	decreases methylation	1
Asbestos, Crocidolite	affects expression	1

ChEMBL screening assays

14 unique, capped per target: 12 functional, 2 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3888094	Binding	Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization (“FP”) based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium	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
CHEMBL4346403	Functional	Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level at 10 uM measured for 100 secs by fluo-4 dye based FLIPR as	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.