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GPR142

gene
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Also known as PGR2

Summary

GPR142 (G protein-coupled receptor 142, HGNC:20088) is a protein-coding gene on chromosome 17q25.1, encoding G protein-coupled receptor 142 (Q7Z601). Highly selective G protein-coupled receptor for aromatic amino acids specifically L-Tryptophan (L-Trp) and L-Phenylalanine (L-Phe), with L-Trp being the most potent and efficacious agonist.

GPR142 is a member of the rhodopsin family of G protein-coupled receptors (GPRs) (Fredriksson et al., 2003 [PubMed 14623098]).

Source: NCBI Gene 350383 — RefSeq curated summary.

At a glance

  • Clinical variants (ClinVar): 105 total
  • Druggable target: yes
  • MANE Select transcript: NM_001331076

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:20088
Approved symbolGPR142
NameG protein-coupled receptor 142
Location17q25.1
Locus typegene with protein product
StatusApproved
AliasesPGR2
Ensembl geneENSG00000257008
Ensembl biotypeprotein_coding
OMIM609046
Entrez350383

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000335666, ENST00000582579, ENST00000585308

RefSeq mRNA: 3 — MANE Select: NM_001331076 NM_001331076, NM_001331077, NM_181790

CCDS: CCDS11698, CCDS92387

Canonical transcript exons

ENST00000582579 — 4 exons

ExonStartEnd
ENSE000026879627437172974372600
ENSE000027127177436750674367794
ENSE000036737967437052174370679
ENSE000039305867436946874369634

Expression profiles

Bgee: expression breadth broad, 80 present calls, max score 65.85.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.1140 / max 48.0399, expressed in 31 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter IDTPM avgSamples expressed
1625990.080919
1625980.033110

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
islet of LangerhansUBERON:000000665.85gold quality
spleenUBERON:000210658.23gold quality
duodenumUBERON:000211457.11gold quality
granulocyteCL:000009455.46gold quality
lymph nodeUBERON:000002953.57gold quality
pancreasUBERON:000126453.28gold quality
mucosa of stomachUBERON:000119953.00gold quality
left uterine tubeUBERON:000130351.83gold quality
right lobe of thyroid glandUBERON:000111951.37gold quality
vermiform appendixUBERON:000115448.82gold quality
thyroid glandUBERON:000204647.97gold quality
endocervixUBERON:000045847.55gold quality
fundus of stomachUBERON:000116047.39gold quality
gall bladderUBERON:000211047.21gold quality
ectocervixUBERON:001224946.83gold quality
cerebellar cortexUBERON:000212946.53gold quality
cerebellumUBERON:000203746.52gold quality
cerebellar hemisphereUBERON:000224546.40gold quality
uterine cervixUBERON:000000246.26gold quality
right hemisphere of cerebellumUBERON:001489046.15gold quality
left lobe of thyroid glandUBERON:000112045.73gold quality
body of pancreasUBERON:000115045.57silver quality
vaginaUBERON:000099644.12gold quality
tonsilUBERON:000237243.69silver quality
myometriumUBERON:000129643.34gold quality
tibial nerveUBERON:000132343.19gold quality
fallopian tubeUBERON:000388943.11gold quality
left coronary arteryUBERON:000162642.91gold quality
lower esophagus muscularis layerUBERON:003583342.89gold quality
lower esophagusUBERON:001347342.79gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3no1.64
E-MTAB-6142no0.52

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 1)

  • e developed GPR142 agonists as insulin secretagogues. In this report, we show the discovery of a selective, potent small-molecule GPR142 antagonist, CLP-3094, and its pharmacological characteristics. These data support targeting this receptor for the treatment of chronic inflammatory diseases. (PMID:27807998)

Cross-species orthologs

138 orthologs

OrganismSymbolGene ID
danio_reriogpr142ENSDARG00000102491
mus_musculusGpr142ENSMUSG00000034677
rattus_norvegicusGpr142ENSRNOG00000024446
drosophila_melanogasterProc-RFBGN0029723
drosophila_melanogasterSPRFBGN0029768
drosophila_melanogasterCG15614FBGN0034168
drosophila_melanogasterFMRFaRFBGN0035385
drosophila_melanogasterCG33639FBGN0053639
drosophila_melanogasterCNMaRFBGN0053696
caenorhabditis_elegansWBGENE00005748
caenorhabditis_elegansWBGENE00005749
caenorhabditis_elegansWBGENE00005750
caenorhabditis_elegansWBGENE00005751
caenorhabditis_elegansWBGENE00005753
caenorhabditis_elegansWBGENE00005754
caenorhabditis_elegansWBGENE00005755
caenorhabditis_elegansWBGENE00005756
caenorhabditis_elegansWBGENE00005757
caenorhabditis_elegansWBGENE00005758
caenorhabditis_elegansWBGENE00005759
caenorhabditis_elegansWBGENE00005760
caenorhabditis_elegansWBGENE00005761
caenorhabditis_elegansWBGENE00005762
caenorhabditis_elegansWBGENE00005763
caenorhabditis_elegansWBGENE00005764
caenorhabditis_elegansWBGENE00005766
caenorhabditis_elegansWBGENE00005767
caenorhabditis_elegansWBGENE00005768
caenorhabditis_elegansWBGENE00005769
caenorhabditis_elegansWBGENE00005770
caenorhabditis_elegansWBGENE00005771
caenorhabditis_elegansWBGENE00005773
caenorhabditis_elegansWBGENE00005776
caenorhabditis_elegansWBGENE00005778
caenorhabditis_elegansWBGENE00005779
caenorhabditis_elegansWBGENE00005780
caenorhabditis_elegansWBGENE00005781
caenorhabditis_elegansWBGENE00005782
caenorhabditis_elegansWBGENE00005785
caenorhabditis_elegansWBGENE00005787
caenorhabditis_elegansWBGENE00005788
caenorhabditis_elegansWBGENE00005789
caenorhabditis_elegansWBGENE00005790
caenorhabditis_elegansWBGENE00005791
caenorhabditis_elegansWBGENE00005795
caenorhabditis_elegansWBGENE00005798
caenorhabditis_elegansWBGENE00005800
caenorhabditis_elegansWBGENE00005801
caenorhabditis_elegansWBGENE00005802
caenorhabditis_elegansWBGENE00005803
caenorhabditis_elegansWBGENE00005804
caenorhabditis_elegansWBGENE00005806
caenorhabditis_elegansWBGENE00005807
caenorhabditis_elegansWBGENE00005808
caenorhabditis_elegansWBGENE00005809
caenorhabditis_elegansWBGENE00005810
caenorhabditis_elegansWBGENE00005813
caenorhabditis_elegansWBGENE00005814
caenorhabditis_elegansWBGENE00005815
caenorhabditis_elegansWBGENE00005816
caenorhabditis_elegansWBGENE00005818
caenorhabditis_elegansWBGENE00005820
caenorhabditis_elegansWBGENE00005823
caenorhabditis_elegansWBGENE00005824
caenorhabditis_elegansWBGENE00005826
caenorhabditis_elegansWBGENE00005829
caenorhabditis_elegansWBGENE00005830
caenorhabditis_elegansWBGENE00005831
caenorhabditis_elegansWBGENE00005832
caenorhabditis_elegansWBGENE00005834
caenorhabditis_eleganssrw-88WBGENE00005835
caenorhabditis_elegansWBGENE00005836
caenorhabditis_elegansWBGENE00005837
caenorhabditis_elegansWBGENE00005838
caenorhabditis_elegansWBGENE00005841
caenorhabditis_elegansWBGENE00005842
caenorhabditis_elegansWBGENE00005844
caenorhabditis_elegansWBGENE00005845
caenorhabditis_elegansWBGENE00005846
caenorhabditis_elegansWBGENE00005847
caenorhabditis_elegansWBGENE00005848
caenorhabditis_elegansWBGENE00005849
caenorhabditis_elegansWBGENE00005850
caenorhabditis_elegansWBGENE00005854
caenorhabditis_elegansWBGENE00005856
caenorhabditis_eleganssrw-111WBGENE00005858
caenorhabditis_elegansWBGENE00005859
caenorhabditis_elegansWBGENE00005860
caenorhabditis_elegansWBGENE00005862
caenorhabditis_elegansWBGENE00005864
caenorhabditis_elegansWBGENE00005865
caenorhabditis_elegansWBGENE00005866
caenorhabditis_elegansWBGENE00005867
caenorhabditis_elegansWBGENE00005868
caenorhabditis_elegansWBGENE00005869
caenorhabditis_elegansWBGENE00005870
caenorhabditis_elegansWBGENE00005871
caenorhabditis_elegansWBGENE00005874
caenorhabditis_elegansWBGENE00005876
caenorhabditis_elegansWBGENE00005877
caenorhabditis_elegansWBGENE00005880
caenorhabditis_elegansWBGENE00005881
caenorhabditis_elegansWBGENE00005883
caenorhabditis_elegansWBGENE00005884
caenorhabditis_elegansWBGENE00005885
caenorhabditis_elegansWBGENE00005886
caenorhabditis_elegansWBGENE00005887
caenorhabditis_elegansWBGENE00005888
caenorhabditis_elegansWBGENE00005889
caenorhabditis_elegansWBGENE00005890
caenorhabditis_elegansWBGENE00005891
caenorhabditis_elegansWBGENE00008300
caenorhabditis_elegansWBGENE00010375
caenorhabditis_elegansWBGENE00010986
caenorhabditis_elegansWBGENE00012083
caenorhabditis_elegansWBGENE00015263
caenorhabditis_elegansWBGENE00015323
caenorhabditis_elegansWBGENE00016909
caenorhabditis_elegansWBGENE00017015
caenorhabditis_elegansWBGENE00017040
caenorhabditis_elegansWBGENE00017614
caenorhabditis_elegansWBGENE00017661
caenorhabditis_elegansWBGENE00019262
caenorhabditis_elegansWBGENE00019444
caenorhabditis_elegansWBGENE00019445
caenorhabditis_elegansWBGENE00019448
caenorhabditis_elegansWBGENE00020008
caenorhabditis_elegansWBGENE00020523
caenorhabditis_elegansWBGENE00020524
caenorhabditis_elegansWBGENE00020525
caenorhabditis_elegansWBGENE00022086
caenorhabditis_elegansWBGENE00022604
caenorhabditis_elegansWBGENE00022605
caenorhabditis_elegansWBGENE00022606
caenorhabditis_elegansWBGENE00045413
caenorhabditis_elegansWBGENE00189957
caenorhabditis_elegansWBGENE00194821
caenorhabditis_elegansWBGENE00303233

Paralogs (1): GPR139 (ENSG00000180269)

Protein

Protein identifiers

G protein-coupled receptor 142 — Q7Z601 (reviewed: Q7Z601)

Alternative names: G protein-coupled receptor PGR2

All UniProt accessions (3): Q7Z601, J3QLF2, J3QSD0

UniProt curated annotations — full annotation on UniProt →

Function. Highly selective G protein-coupled receptor for aromatic amino acids specifically L-Tryptophan (L-Trp) and L-Phenylalanine (L-Phe), with L-Trp being the most potent and efficacious agonist. GPR142 agonists triggers the activation of both GNAQ/G(q) and GNAI1/G(i)-coupled signaling pathways. L-Trp stimulates glucose-induced insulin secretion and triggers G(q)-mediated signaling. GPR142 appears to have a role as a sensor of aromatic essential amino acids controlling the secretion of both insulin in the pancreas and other gastrointestinal hormones including glucagon but also CCK and incretin in the gastrointestinal-tract, contributing to the control of glucose homeostasis by coordinating pancreatic and gut hormone secretion.

Subcellular location. Cell membrane.

Tissue specificity. Expressed mainly in pancreatic islet and enteroendocrine cells. Expressed in the central nervous system, most abundantly in the ventrolateral region of caudate putamen, the habenular nucleus, the zona incerta, and the medial mammillary nucleus.

Similarity. Belongs to the G-protein coupled receptor 1 family.

Isoforms (2)

UniProt IDNamesCanonical?
Q7Z601-11yes
Q7Z601-22

RefSeq proteins (3): NP_001318005, NP_001318006, NP_861455 (=MANE)

Domains & families (InterPro)

IDNameType
IPR000276GPCR_RhodpsnFamily
IPR017452GPCR_Rhodpsn_7TMDomain
IPR052477Orphan_GPCR1Family

Pfam: PF00001

UniProt features (20 total): topological domain 8, transmembrane region 7, chain 1, region of interest 1, compositionally biased region 1, splice variant 1, sequence variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q7Z601-F163.680.13

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 16 (showing top): HFH8_01, HFH3_01, LYF1_01, NIKOLSKY_BREAST_CANCER_17Q21_Q25_AMPLICON, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, BLANCO_MELO_COVID19_SARS_COV_2_LOW_MOI_INFECTION_A594_ACE2_EXPRESSING_CELLS_UP, STAT_Q6, RTAAACA_FREAC2_01, XIE_ST_HSC_S1PR3_OE_UP, NOURUZI_NEPC_ASCL1_TARGETS, LI_STAD_HIGH_RISK_UP, GOMF_MOLECULAR_TRANSDUCER_ACTIVITY, AAAYWAACM_HFH4_01

GO Biological Process (2): G protein-coupled receptor signaling pathway (GO:0007186), signal transduction (GO:0007165)

GO Molecular Function (1): G protein-coupled receptor activity (GO:0004930)

GO Cellular Component (4): cytosol (GO:0005829), plasma membrane (GO:0005886), cell junction (GO:0030054), membrane (GO:0016020)

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure3
G protein-coupled receptor activity1
signal transduction1
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
transmembrane signaling receptor activity1
G protein-coupled receptor signaling pathway1
cytoplasm1
membrane1
cell periphery1

Protein interactions and networks

STRING

444 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
GPR142RHOP08100733
GPR142GPR119Q8TDV5691
GPR142FFAR1O14842689
GPR142GPR35Q9HC97649
GPR142TAS1R1Q7RTX1599
GPR142GPBAR1Q8TDU6592
GPR142INSL5Q9Y5Q6566
GPR142TAAR1Q96RJ0556
GPR142GNAQP50148539
GPR142GHRLQ9UBU3535
GPR142GPR160Q9UJ42535
GPR142GPR82Q96P67528
GPR142CASRP41180528
GPR142GPR22Q99680503
GPR142GPRC6AQ5T6X5491

IntAct

0 interactions, top by confidence:

BioGRID (2): GPR142 (Affinity Capture-MS), GPR142 (Two-hybrid)

ESM2 similar proteins: A2RRU4, A3KFU9, A6QM06, D3YYI7, O60346, P29590, P51810, P70259, P97260, Q12770, Q16538, Q17QQ5, Q2T9K0, Q3TAA7, Q3UN16, Q3ZCA1, Q5MNU5, Q69Z89, Q6GQT6, Q6NS60, Q6NV75, Q6QHK4, Q6UXU4, Q70EL4, Q7Z5H3, Q7Z601, Q80ZW0, Q86SQ6, Q8BGE9, Q8BUM9, Q8C010, Q8C4G9, Q8CE64, Q8CHE4, Q8K0Z9, Q8N1F8, Q8NC44, Q8TC41, Q8TDR2, Q8TF61

Diamond homologs: O19037, P0C0W8, P30560, P37288, P47798, P48043, P56444, P56447, Q62463, Q6DWJ6, Q7TQN9, Q7Z601, Q80UC8, Q9WTV8, Q9WTV9, P56446, P79166, Q864F7, Q864F8, P16395, Q9NPC1

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance87
Likely benign11
Benign2

Top pathogenic / likely-pathogenic (0)

SpliceAI

912 predictions. Top by Δscore:

VariantEffectΔscore
17:74370516:TCTA:Tacceptor_loss1.0000
17:74370517:CTAGC:Cacceptor_loss1.0000
17:74370518:TAGCT:Tacceptor_loss1.0000
17:74370519:A:AGacceptor_gain1.0000
17:74370519:AGCT:Aacceptor_gain1.0000
17:74370520:G:GAacceptor_loss1.0000
17:74370520:G:GGacceptor_gain1.0000
17:74370520:GCT:Gacceptor_gain1.0000
17:74370520:GCTG:Gacceptor_gain1.0000
17:74367605:G:GTdonor_gain0.9900
17:74370512:A:AGacceptor_gain0.9900
17:74370513:C:Gacceptor_gain0.9900
17:74370519:AGCTG:Aacceptor_gain0.9900
17:74370520:GC:Gacceptor_gain0.9900
17:74370520:GCTGG:Gacceptor_gain0.9900
17:74370675:GCCTG:Gdonor_gain0.9900
17:74370676:CCTGG:Cdonor_loss0.9900
17:74370680:G:Cdonor_loss0.9900
17:74370680:G:GGdonor_gain0.9900
17:74370681:T:Adonor_loss0.9900
17:74370682:GA:Gdonor_loss0.9900
17:74371712:ACCTC:Aacceptor_gain0.9900
17:74371716:C:Aacceptor_gain0.9900
17:74372189:T:TAacceptor_gain0.9900
17:74370520:G:Tacceptor_gain0.9800
17:74370678:TG:Tdonor_gain0.9800
17:74370679:GG:Gdonor_gain0.9800
17:74371727:A:AGacceptor_gain0.9800
17:74371728:G:GGacceptor_gain0.9800
17:74370518:TAGC:Tacceptor_gain0.9700

AlphaMissense

3046 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
17:74371926:T:CF239L0.982
17:74371928:T:AF239L0.982
17:74371928:T:GF239L0.982
17:74370652:A:CS164R0.976
17:74370654:T:AS164R0.976
17:74370654:T:GS164R0.976
17:74371854:T:CF215L0.964
17:74371856:C:AF215L0.964
17:74371856:C:GF215L0.964
17:74372088:T:CF293L0.951
17:74372090:C:AF293L0.951
17:74372090:C:GF293L0.951
17:74372472:T:CF421L0.938
17:74372474:C:AF421L0.938
17:74372474:C:GF421L0.938
17:74372307:T:CF366L0.936
17:74372309:C:AF366L0.936
17:74372309:C:GF366L0.936
17:74371950:T:AW247R0.926
17:74371950:T:CW247R0.926
17:74372407:C:AA399D0.921
17:74372463:A:CS418R0.911
17:74372465:C:AS418R0.911
17:74372465:C:GS418R0.911
17:74372210:C:AN333K0.908
17:74372210:C:GN333K0.908
17:74370646:T:GY162D0.900
17:74371731:A:CS174R0.895
17:74371733:C:AS174R0.895
17:74371733:C:GS174R0.895

dbSNP variants (sampled 300 via entrez): RS1000021398 (17:74368612 G>A), RS1000536324 (17:74366588 G>A), RS1001198560 (17:74368383 C>T), RS1001346651 (17:74365901 G>A), RS1001654456 (17:74368005 G>T), RS1001859139 (17:74371233 T>C), RS1003695815 (17:74371997 C>A,T), RS1003878676 (17:74368959 G>A), RS1004051616 (17:74366344 G>A), RS1004370194 (17:74369333 C>A,G,T), RS1004731523 (17:74372949 G>A,T), RS1004922146 (17:74371603 A>G), RS1005117714 (17:74368293 G>T), RS1005956824 (17:74369574 A>G), RS1006338446 (17:74366949 AT>A)

Disease associations

OMIM: gene MIM:609046 | 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): CHEMBL2069161 (SINGLE PROTEIN)

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Class A Orphans with emerging pharmacology

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

LigandActionAffinityParameter
compound 33 [Toda et al., 2013]Agonist7.66pEC50

Binding affinities (BindingDB)

3 measured of 3 human assays (3 total across all organisms); most potent 3 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
3-chloro-N-[(2S,4R)-2-[3-(3,5-dimethylimidazol-4-yl)-1H-1,2,4-triazol-5-yl]oxan-4-yl]-N-methylbenzamideEC5027.2 nMUS-10196385: Tetrahydropyranyl benzamide derivatives
N-[(2S,4R)-2-[3-(3,5-dimethylimidazol-4-yl)-1H-1,2,4-triazol-5-yl]oxan-4-yl]-N-methyl-3-(trifluoromethoxy)benzamideEC5030.1 nMUS-10196385: Tetrahydropyranyl benzamide derivatives
N-[(2S,4R)-2-[3-(3,5-dimethylimidazol-4-yl)-1H-1,2,4-triazol-5-yl]oxan-4-yl]-N-methyl-3-(trifluoromethyl)benzamideEC5043.5 nMUS-10196385: Tetrahydropyranyl benzamide derivatives

ChEMBL bioactivities

216 potent at pChembl≥5 of 221 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
10.30EC500.05nMCHEMBL4764444
9.70EC500.2nMCHEMBL2409014
9.68EC500.21nMCHEMBL4751520
9.68EC500.21nMCHEMBL4755970
9.43EC500.37nMCHEMBL4764882
9.43EC500.37nMCHEMBL4751970
9.40EC500.4nMCHEMBL4741429
9.35EC500.45nMCHEMBL4746958
9.33EC500.47nMCHEMBL4790120
9.20EC500.63nMCHEMBL4760780
9.19EC500.64nMCHEMBL4785317
9.19EC500.64nMCHEMBL4741522
9.14EC500.73nMCHEMBL4744201
9.13EC500.74nMCHEMBL4799308
9.07EC500.85nMCHEMBL4797569
9.07EC500.86nMCHEMBL4791730
9.02EC500.95nMCHEMBL4764060
9.00EC501nMCHEMBL2409011
9.00EC501nMCHEMBL2409009
8.89EC501.3nMCHEMBL2409019
8.30EC505nMCHEMBL2409031
8.15EC507nMCHEMBL2409027
7.96EC5011nMCHEMBL4647745
7.92EC5012nMCHEMBL3905835
7.85EC5014nMCHEMBL2409023
7.85EC5014nMCHEMBL3967871
7.85EC5014nMCHEMBL4647456
7.85EC5014nMCHEMBL4646017
7.84EC5014.4nMCHEMBL4647456
7.80EC5016nMCHEMBL3976574
7.80EC5016nMCHEMBL4637374
7.66EC5022nMCHEMBL2409007
7.62EC5024nMCHEMBL3965469
7.60EC5025nMCHEMBL2409021
7.60EC5025nMCHEMBL3905835
7.58EC5026nMCHEMBL2430979
7.58EC5026nMCHEMBL3976574
7.57EC5027nMCHEMBL4636686
7.57EC5027.2nMCHEMBL4636686
7.55EC5028nMCHEMBL2409022
7.52EC5030nMCHEMBL2409012
7.52EC5030nMCHEMBL2409030
7.52EC5030nMCHEMBL4647315
7.52EC5030nMCHEMBL4634933
7.52EC5030.1nMCHEMBL4634933
7.50EC5032nMCHEMBL3903475
7.50EC5032nMCHEMBL4641575
7.47EC5034nMCHEMBL3967871
7.46EC5035nMCHEMBL4641984
7.44EC5036nMCHEMBL2164857

PubChem BioAssay actives

196 with measured affinity, of 325 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.

CompoundAssayTypeValueUnit
2-[5-[[[5-butyl-1-(5-methyl-4-thiophen-2-ylpyrimidin-2-yl)pyrazole-4-carbonyl]amino]methyl]imidazol-1-yl]acetic acid760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0002uM
5-butyl-N-[(3-methylimidazol-4-yl)methyl]-1-(5-methyl-4-thiophen-2-ylpyrimidin-2-yl)pyrazole-4-carboxamide760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0010uM
5-butyl-N-[(3,5-dimethylimidazol-4-yl)methyl]-1-(5-methyl-4-thiophen-2-ylpyrimidin-2-yl)pyrazole-4-carboxamide760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0010uM
5-(ethoxymethyl)-N-[(3-methylimidazol-4-yl)methyl]-1-(5-methyl-4-thiophen-2-ylpyrimidin-2-yl)pyrazole-4-carboxamide760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0013uM
1-(5-methyl-4-thiophen-2-ylpyrimidin-2-yl)-5-propyl-N-(2-pyridin-4-ylpropan-2-yl)pyrazole-4-carboxamide760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0050uM
5-butyl-1-(5-methyl-4-thiophen-2-ylpyrimidin-2-yl)-N-(pyridin-4-ylmethyl)pyrazole-4-carboxamide760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0070uM
N-[(1R,3S)-3-[3-(3,5-dimethylimidazol-4-yl)-1H-1,2,4-triazol-5-yl]cyclohexyl]-N-methyl-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0110uM
N-(2,3-dichlorophenyl)-2-[4-[4-(2-methylimidazol-1-yl)phenyl]triazol-1-yl]acetamide1326004: Agonist activity at human GPR142 expressed in CHO cells measured after 30 to 60 mins by IP-One assayec500.0120uM
N-(2,3-dichlorophenyl)-2-[4-[4-(4-methylimidazol-1-yl)phenyl]triazol-1-yl]acetamide1326004: Agonist activity at human GPR142 expressed in CHO cells measured after 30 to 60 mins by IP-One assayec500.0140uM
3-chloro-N-[(1R,3S)-3-[3-(3,5-dimethylimidazol-4-yl)-1H-1,2,4-triazol-5-yl]cyclohexyl]-N-methylbenzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0140uM
N-[(2S,4R)-2-[3-[3-(cyclopropylmethyl)-5-methylimidazol-4-yl]-1H-1,2,4-triazol-5-yl]oxan-4-yl]-N-methyl-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0140uM
5-(ethoxymethyl)-N-[(3-methylimidazol-4-yl)methyl]-1-(5-methyl-4-pyrrolidin-1-ylpyrimidin-2-yl)pyrazole-4-carboxamide760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0140uM
N-(2,3-dichlorophenyl)-2-[4-(4-imidazol-1-ylphenyl)triazol-1-yl]acetamide1326004: Agonist activity at human GPR142 expressed in CHO cells measured after 30 to 60 mins by IP-One assayec500.0160uM
N-[(2S,4R)-2-[3-(3-cyclobutyl-5-methylimidazol-4-yl)-1H-1,2,4-triazol-5-yl]oxan-4-yl]-N-methyl-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0160uM
5-(ethoxymethyl)-N-[(3-methylimidazol-4-yl)methyl]-1-(5-methyl-4-piperidin-1-ylpyrimidin-2-yl)pyrazole-4-carboxamide760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0220uM
N-(2,3-dichlorophenyl)-2-[4-[6-(2-methylimidazol-1-yl)-3-pyridinyl]triazol-1-yl]acetamide1326002: Agonist activity at human GPR142 expressed in CHO cells measured for 3 to 5 mins by Fluo-4AM dye-based FLIPR assayec500.0240uM
1-[4-(cyclobutylamino)-5-methylpyrimidin-2-yl]-5-(ethoxymethyl)-N-[(3-methylimidazol-4-yl)methyl]pyrazole-4-carboxamide760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0250uM
(2S)-3-(4-fluorophenyl)-N-[1-methyl-3-[2-(methylamino)-4-pyridinyl]pyrazol-5-yl]-2-(2H-triazol-4-ylmethylamino)propanamide772142: Agonist activity at human GPR142 expressed in HEK293 cells assessed as inositol phosphate accumulation using [3H]-inositol after 1 hr by scintillation countingec500.0260uM
3-chloro-N-[(2S,4R)-2-[3-(3,5-dimethylimidazol-4-yl)-1H-1,2,4-triazol-5-yl]oxan-4-yl]-N-methylbenzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0270uM
1-[4-(azetidin-1-yl)-5-methylpyrimidin-2-yl]-5-(ethoxymethyl)-N-[(3-methylimidazol-4-yl)methyl]pyrazole-4-carboxamide760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0280uM
N-[(2S,4R)-2-[3-(3,5-dimethylimidazol-4-yl)-1H-1,2,4-triazol-5-yl]oxan-4-yl]-N-methyl-3-(trifluoromethoxy)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0300uM
N-[(1R,3S)-3-[(3,5-dimethylimidazol-4-yl)carbamoyl]cyclohexyl]-N-methyl-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0300uM
5-butyl-N-[(2,3-dimethylimidazol-4-yl)methyl]-1-(5-methyl-4-thiophen-2-ylpyrimidin-2-yl)pyrazole-4-carboxamide760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0300uM
5-(ethoxymethyl)-1-(5-methyl-4-thiophen-2-ylpyrimidin-2-yl)-N-(pyridin-4-ylmethyl)pyrazole-4-carboxamide760556: Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assayec500.0300uM
N-(2,3-dichlorophenyl)-2-[4-[3-fluoro-4-(4-methylimidazol-1-yl)phenyl]triazol-1-yl]acetamide1326004: Agonist activity at human GPR142 expressed in CHO cells measured after 30 to 60 mins by IP-One assayec500.0320uM
N-[(1R,3S)-3-[3-(6,8-dihydro-5H-imidazo[2,1-c][1,4]oxazin-3-yl)-1H-1,2,4-triazol-5-yl]cyclohexyl]-N-methyl-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0320uM
3-chloro-N-[(2S,4R)-2-(3-imidazo[1,2-a]pyridin-3-yl-1H-1,2,4-triazol-5-yl)oxan-4-yl]-N-methylbenzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0350uM
(2S)-N-[5-[2-(methylamino)-4-pyridinyl]-1,3,4-thiadiazol-2-yl]-3-phenyl-2-(1,3-thiazol-4-ylmethylamino)propanamide699506: Agonist activity at human GPR142 expressed in HEK293 cells assessed as inositol phosphate accumulation after 1 hr by scintillation countingec500.0360uM
N-(3-chlorophenyl)-10-(2-methyl-4-pyridinyl)-5,6-dihydro-[1,2,4]triazolo[4,3-d][1,4]benzoxazepin-3-amine1712063: Agonist activity at human GPR142 expressed in CHO cells measured for 3 mins by Fluo-4M dye based FLIPR assayic500.0370uM
(2S)-N-(1-methyl-3-pyridin-4-ylpyrazol-5-yl)-3-phenyl-2-(1,3-thiazol-5-ylmethylamino)propanamide772142: Agonist activity at human GPR142 expressed in HEK293 cells assessed as inositol phosphate accumulation using [3H]-inositol after 1 hr by scintillation countingec500.0370uM
(2S)-N-[1-methyl-3-[2-(methylamino)-4-pyridinyl]pyrazol-5-yl]-3-phenyl-2-(1,3-thiazol-5-ylmethylamino)propanamide772142: Agonist activity at human GPR142 expressed in HEK293 cells assessed as inositol phosphate accumulation using [3H]-inositol after 1 hr by scintillation countingec500.0370uM
N-(2,3-dichlorophenyl)-2-[4-[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]triazol-1-yl]acetamide1326004: Agonist activity at human GPR142 expressed in CHO cells measured after 30 to 60 mins by IP-One assayec500.0400uM
N-[(1R,3S)-3-[3-[3-(2,2-difluoroethyl)-5-methylimidazol-4-yl]-1H-1,2,4-triazol-5-yl]cyclohexyl]-N-methyl-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0410uM
2-[[(2S)-3-(4-fluorophenyl)-1-[[1-methyl-3-[2-(methylamino)-4-pyridinyl]pyrazol-5-yl]amino]-1-oxopropan-2-yl]amino]acetic acid772142: Agonist activity at human GPR142 expressed in HEK293 cells assessed as inositol phosphate accumulation using [3H]-inositol after 1 hr by scintillation countingec500.0420uM
N-[(2S,4R)-2-[3-(3,5-dimethylimidazol-4-yl)-1H-1,2,4-triazol-5-yl]oxan-4-yl]-N-methyl-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0430uM
10-(2-methyl-4-pyridinyl)-N-[3-(trifluoromethoxy)phenyl]-5,6-dihydro-[1,2,4]triazolo[4,3-d][1,4]benzoxazepin-3-amine1712063: Agonist activity at human GPR142 expressed in CHO cells measured for 3 mins by Fluo-4M dye based FLIPR assayic500.0450uM
N-[(1R,3S)-3-[3-(2,3-dimethylimidazol-4-yl)-1H-1,2,4-triazol-5-yl]cyclohexyl]-N-methyl-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0460uM
10-pyridin-4-yl-N-[3-(trifluoromethyl)phenyl]-5,6-dihydro-[1,2,4]triazolo[4,3-d][1,4]benzoxazepin-3-amine1712063: Agonist activity at human GPR142 expressed in CHO cells measured for 3 mins by Fluo-4M dye based FLIPR assayic500.0480uM
(2S)-3-(4-fluorophenyl)-N-[1-methyl-3-[2-(methylamino)-4-pyridinyl]pyrazol-5-yl]-2-(1,3-thiazol-5-ylmethylamino)propanamide772142: Agonist activity at human GPR142 expressed in HEK293 cells assessed as inositol phosphate accumulation using [3H]-inositol after 1 hr by scintillation countingec500.0490uM
N-methyl-N-[(1R,3S)-3-[[5-methyl-3-(2-morpholin-4-ylethyl)imidazol-4-yl]carbamoyl]cyclohexyl]-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0510uM
N-[(1R,3S)-3-[[3-(cyclopropylmethyl)-5-methylimidazol-4-yl]carbamoyl]cyclohexyl]-N-methyl-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0520uM
2-[[(2S)-1-[(1-methyl-3-pyridin-4-ylpyrazol-5-yl)amino]-1-oxo-3-phenylpropan-2-yl]amino]acetic acid772142: Agonist activity at human GPR142 expressed in HEK293 cells assessed as inositol phosphate accumulation using [3H]-inositol after 1 hr by scintillation countingec500.0520uM
(2S)-N-[3-(2-methyl-4-pyridinyl)phenyl]-3-phenyl-2-(1,3-thiazol-4-ylmethylamino)propanamide678285: Agonist activity at human GPR142 expressed in HEK293 cells assessed as inositol phosphate accumulation using [3H]-inositol after 1 hr by scintillation countingec500.0520uM
N-[(2S,4R)-2-[3-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-3-yl)-1H-1,2,4-triazol-5-yl]oxan-4-yl]-N-methyl-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0530uM
(2S)-N-(3-methoxy-5-pyridin-4-ylphenyl)-3-phenyl-2-(1,3-thiazol-4-ylmethylamino)propanamide678285: Agonist activity at human GPR142 expressed in HEK293 cells assessed as inositol phosphate accumulation using [3H]-inositol after 1 hr by scintillation countingec500.0530uM
(2S)-N-(2-oxo-5-pyridin-4-yl-1H-pyridin-3-yl)-3-phenyl-2-[(1-pyridin-2-ylcyclopropyl)amino]propanamide699506: Agonist activity at human GPR142 expressed in HEK293 cells assessed as inositol phosphate accumulation after 1 hr by scintillation countingec500.0540uM
3-(3-chloro-2-fluorophenoxy)-10-(2-methyl-4-pyridinyl)-5,6-dihydro-[1,2,4]triazolo[4,3-d][1,4]benzoxazepine1712063: Agonist activity at human GPR142 expressed in CHO cells measured for 3 mins by Fluo-4M dye based FLIPR assayic500.0560uM
3-(3-chlorophenoxy)-10-(2-methyl-4-pyridinyl)-5,6-dihydro-[1,2,4]triazolo[4,3-d][1,4]benzoxazepine1712063: Agonist activity at human GPR142 expressed in CHO cells measured for 3 mins by Fluo-4M dye based FLIPR assayic500.0580uM
N-[(1R,3S)-3-[[3-(2,2-difluoroethyl)-5-methylimidazol-4-yl]carbamoyl]cyclohexyl]-N-methyl-3-(trifluoromethyl)benzamide1666608: Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assayec500.0630uM
10-pyridin-4-yl-N-[3-(trifluoromethoxy)phenyl]-5,6-dihydro-[1,2,4]triazolo[4,3-d][1,4]benzoxazepin-3-amine1712063: Agonist activity at human GPR142 expressed in CHO cells measured for 3 mins by Fluo-4M dye based FLIPR assayic500.0630uM

CTD chemical–gene interactions

8 total (human), top 8 by PubMed support.

ChemicalActions (top 5)PubMed papers
bisphenol Aincreases expression1
ethyl-p-hydroxybenzoatedecreases expression1
o,p’-DDTincreases expression1
abrineincreases expression1
Resveratrolincreases expression1
Valproic Acidincreases methylation1
Zearalenoneincreases expression1
1-Methyl-4-phenylpyridiniumincreases expression1

ChEMBL screening assays

25 unique, capped per target: 19 functional, 6 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL2072130FunctionalAgonist activity at human GPR142 expressed in HEK293 cells assessed as inositol phosphate accumulation using [3H]-inositol after 1 hr by scintillation countingDiscovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus. — Bioorg Med Chem Lett
CHEMBL3865477BindingAgonist activity at human GPR142 expressed in CHO cells measured for 3 to 5 mins by Fluo-4AM dye-based FLIPR assayDiscovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes. — ACS Med Chem Lett

Cellosaurus cell lines

1 cell lines: 1 spontaneously immortalized cell line

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_KX34PathHunter CHO-K1 GPR142 beta-arrestinSpontaneously immortalized cell lineFemale

Clinical trials (associated diseases)

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

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

About this page

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

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 79

This page pulls from 79 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatentpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomerefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot