GPR119

Summary

GPR119 (G protein-coupled receptor 119, HGNC:19060) is a protein-coding gene on chromosome Xq26.1, encoding Glucose-dependent insulinotropic receptor (Q8TDV5). Receptor for the endogenous fatty-acid ethanolamide oleoylethanolamide (OEA) and lysophosphatidylcholine (LPC).

This gene encodes a member of the rhodopsin subfamily of G-protein-coupled receptors that is expressed in the pancreas and gastrointestinal tract. The encoded protein is activated by lipid amides including lysophosphatidylcholine and oleoylethanolamide and may be involved in glucose homeostasis. This protein is a potential drug target in the treatment of type 2 diabetes.

Source: NCBI Gene 139760 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 27 total
• Druggable target: yes — 11 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_178471

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:19060
Approved symbol	GPR119
Name	G protein-coupled receptor 119
Location	Xq26.1
Locus type	gene with protein product
Status	Approved
Aliases	hGPCR2, GPCR2
Ensembl gene	ENSG00000147262
Ensembl biotype	protein_coding
OMIM	300513
Entrez	139760

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000276218, ENST00000682440

RefSeq mRNA: 1 — MANE Select: NM_178471 NM_178471

CCDS: CCDS14625

Canonical transcript exons

ENST00000682440 — 2 exons

Exon	Start	End
ENSE00003917670	130384436	130385674
ENSE00003921057	130379449	130382551

Expression profiles

Bgee: expression breadth broad, 14 present calls, max score 88.82.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0429 / max 71.5385, expressed in 3 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
200477	0.0429	3

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
islet of Langerhans	UBERON:0000006	88.82	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	84.35	gold quality
pancreas	UBERON:0001264	61.39	gold quality
duodenum	UBERON:0002114	51.56	gold quality
rectum	UBERON:0001052	48.47	gold quality
body of pancreas	UBERON:0001150	47.44	gold quality
mucosa of transverse colon	UBERON:0004991	37.27	silver quality
colonic epithelium	UBERON:0000397	37.20	gold quality
ventricular zone	UBERON:0003053	36.48	gold quality
cortical plate	UBERON:0005343	36.47	gold quality
bone marrow cell	CL:0002092	36.16	gold quality
ganglionic eminence	UBERON:0004023	35.49	gold quality
skeletal muscle tissue	UBERON:0001134	33.38	gold quality
hindlimb stylopod muscle	UBERON:0004252	32.15	gold quality
bone marrow	UBERON:0002371	31.74	gold quality
muscle tissue	UBERON:0002385	31.06	gold quality
small intestine	UBERON:0002108	30.54	gold quality
stromal cell of endometrium	CL:0002255	29.87	gold quality
prefrontal cortex	UBERON:0000451	29.36	gold quality
fundus of stomach	UBERON:0001160	28.98	silver quality
stomach	UBERON:0000945	28.31	gold quality
lymph node	UBERON:0000029	27.57	gold quality
tonsil	UBERON:0002372	27.05	gold quality
intestine	UBERON:0000160	26.83	gold quality
leukocyte	CL:0000738	26.61	gold quality
monocyte	CL:0000576	26.51	gold quality
vermiform appendix	UBERON:0001154	26.42	gold quality
blood	UBERON:0000178	26.37	gold quality
gall bladder	UBERON:0002110	25.98	gold quality
transverse colon	UBERON:0001157	25.92	gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 5.

Experiment	Marker?	Max mean expression
E-GEOD-83139	yes	174.80
E-MTAB-5061	yes	31.72
E-GEOD-81547	yes	19.74
E-GEOD-81608	yes	18.03
E-ENAD-27	yes	10.48
E-ANND-3	no	3.45

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 15)

• GPR119 therefore represents a novel and attractive potential target for the therapy of obesity and related metabolic disorders. (PMID:16517404)
• findings show that N-oleoyldopamine (OLDA)& structurally related hydroxybenzyl amides are robust activators of GPR119; studies indicate that multiple, distinct classes of lipid amides, acting via GPR119, may be important modulators of glucose homeostasis (PMID:19901198)
• Data show that Phe-V:13 can serve as an aromatic lock for the proposed active conformation of the Trp-VI:13 rotameric switch, being involved in the global movement of TM-V and TM-VI in 7TM receptor activation. (PMID:19920139)
• Results provide evidence of an islet-gastrointestinal distribution of GPR119, its expression in pancreatic beta and alpha cells, and its possible involvement in islet function. (PMID:22883930)
• Data suggest that GPR119 activation/up-regulation in skeletal muscle impairs fatty acid and glucose oxidation; diet-induced obesity appears to up-regulate skeletal muscle GPR119. (PMID:23069642)
• Replacement of the three methyl groups in 1 with metabolically stable moieties led to the identification of compound 34, a potent and efficacious GPR119 agonist with improved pharmacokinetic (PK) properties. (PMID:23648181)
• transfection of GLUTag cells with recombinant human GPR119 results in a constitutive and apparently ligand-independent increase of proglucagon gene promoter activity and proglucagon mRNA content. (PMID:23798572)
• The GPR119 agonist, HD0471042 increased intracellular cAMP levels in stably human GPR119 expressing CHO cells. (PMID:23897163)
• Oxidized-LDL significantly induces lincRNA-DYNLRB2-2 expression, which promotes ABCA1-mediated cholesterol efflux and inhibits inflammation through GPR119 in THP-1 cells. (PMID:24493833)
• Describe novel small-molecule GPR119 agonists with high receptor selectivity and capacity to induce glucose-stimulated insulin secretion. (PMID:24681896)
• Angelica dahurica extract-treated cells showed significant increases in GPR119 activation, intracellular cAMP levels, GLP-1 levels and glucose-stimulated insulin secretion as compared with controls (PMID:27391814)
• GPR119 is the oleoyl-lysophosphatidylinositol receptor that is required for GLP-1 secretion in enteroendocrine cells. (PMID:29883799)
• GPR119 Is a Potent Regulator of Human Sebocyte Biology. (PMID:32142797)
• Screening for bacterial enzymes synthesizing GPR119 agonist in cAMP-responsive cells. (PMID:33242325)
• GPR116 overexpression correlates with poor prognosis in gastric cancer. (PMID:35049225)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio		ENSDARG00000077746
mus_musculus	Gpr119	ENSMUSG00000051209
rattus_norvegicus	Gpr119	ENSRNOG00000024517

Paralogs (18): LPAR2 (ENSG00000064547), CNR1 (ENSG00000118432), MC3R (ENSG00000124089), S1PR4 (ENSG00000125910), GPR12 (ENSG00000132975), GPR6 (ENSG00000146360), MC4R (ENSG00000166603), S1PR1 (ENSG00000170989), LPAR3 (ENSG00000171517), MC5R (ENSG00000176136), S1PR5 (ENSG00000180739), GPR3 (ENSG00000181773), MC2R (ENSG00000185231), CNR2 (ENSG00000188822), LPAR1 (ENSG00000198121), S1PR3 (ENSG00000213694), MC1R (ENSG00000258839), S1PR2 (ENSG00000267534)

Protein

Protein identifiers

Glucose-dependent insulinotropic receptor — Q8TDV5 (reviewed: Q8TDV5)

Alternative names: G-protein coupled receptor 119

All UniProt accessions (1): Q8TDV5

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for the endogenous fatty-acid ethanolamide oleoylethanolamide (OEA) and lysophosphatidylcholine (LPC). Functions as a glucose-dependent insulinotropic receptor. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Seems to act through a G(s) mediated pathway.

Subcellular location. Cell membrane.

Tissue specificity. Predominantly expressed in the pancreas, especially in the islets.

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

RefSeq proteins (1): NP_848566* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain
IPR028336	GPR119	Family

Pfam: PF00001

UniProt features (38 total): helix 15, topological domain 8, transmembrane region 7, turn 3, strand 2, chain 1, sequence variant 1, sequence conflict 1

Structure

Experimental structures (PDB)

10 structures.

PDB	Method	Resolution (Å)
7WCM	ELECTRON MICROSCOPY	2.33
9XJW	ELECTRON MICROSCOPY	2.53
7XZ6	ELECTRON MICROSCOPY	2.8
8ZRK	ELECTRON MICROSCOPY	2.82
7WCN	ELECTRON MICROSCOPY	2.87
9L79	ELECTRON MICROSCOPY	2.98
7XZ5	ELECTRON MICROSCOPY	3.1
8ZR5	ELECTRON MICROSCOPY	3.31
9L80	ELECTRON MICROSCOPY	3.33
8VHF	ELECTRON MICROSCOPY	3.51

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q8TDV5-F1	86.81	0.67

Antibody-complex structures (SAbDab): 7 — 7WCM, 7WCN, 7XZ5, 7XZ6, 8VHF, 8ZR5, 8ZRK

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-381771	Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1)
R-HSA-400511	Synthesis, secretion, and inactivation of Glucose-dependent Insulinotropic Polypeptide (GIP)

MSigDB gene sets: 48 (showing top): RRAGTTGT_UNKNOWN, GOBP_INSULIN_SECRETION, GOBP_REGULATION_OF_HORMONE_LEVELS, AREB6_01, GOBP_HORMONE_TRANSPORT, GGGTGGRR_PAX4_03, ACEVEDO_LIVER_CANCER_WITH_H3K27ME3_UP, EFC_Q6, GOBP_CELL_CELL_SIGNALING, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, TGCTGAY_UNKNOWN, OCT1_03, GGARNTKYCCA_UNKNOWN, GOBP_SECRETION, GOBP_SIGNAL_RELEASE

GO Biological Process (5): adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), insulin secretion (GO:0030073), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), regulation of metabolic process (GO:0019222)

GO Molecular Function (4): G protein-coupled receptor activity (GO:0004930), phosphatidylcholine binding (GO:0031210), protein binding (GO:0005515), lipid binding (GO:0008289)

GO Cellular Component (4): cytoplasm (GO:0005737), plasma membrane (GO:0005886), signaling receptor complex (GO:0043235), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Incretin synthesis, secretion, and inactivation	2

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
regulation of cellular process	2
binding	2
cellular anatomical structure	2
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase activator activity	1
protein secretion	1
peptide hormone secretion	1
cell communication	1
cellular process	1
signaling	1
cellular response to stimulus	1
G protein-coupled receptor activity	1
signal transduction	1
metabolic process	1
transmembrane signaling receptor activity	1
G protein-coupled receptor signaling pathway	1
phospholipid binding	1
cation binding	1
quaternary ammonium group binding	1
intracellular anatomical structure	1
membrane	1
cell periphery	1
protein-containing complex	1

Protein interactions and networks

STRING

634 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GPR119	GPR55	Q9Y2T6	923
GPR119	GPR18	Q14330	866
GPR119	FFAR1	O14842	814
GPR119	GCG	P01275	793
GPR119	FFAR4	Q5NUL3	780
GPR119	RHO	P08100	750
GPR119	GIP	P09681	740
GPR119	GPBAR1	Q8TDU6	734
GPR119	GPR84	Q9NQS5	732
GPR119	FFAR2	O15552	718
GPR119	PPARA	Q07869	706
GPR119	GPR142	Q7Z601	691
GPR119	FFAR3	O14843	690
GPR119	NAPEPLD	Q6IQ20	685
GPR119	FAAH	O00519	682

IntAct

5 interactions, top by confidence:

A	B	Type	Score
ASPH	GPR119	psi-mi:“MI:0915”(physical association)	0.560
GPR119	IFITM3	psi-mi:“MI:0914”(association)	0.350
GPR119	ASPH	psi-mi:“MI:0915”(physical association)	0.000
ASPH	GPR119	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (4): ASPH (Two-hybrid), CMIP (Affinity Capture-MS), IFITM3 (Affinity Capture-MS), GPR119 (Affinity Capture-Luminescence)

ESM2 similar proteins: C8YUV0, O19037, O77616, P31392, P43142, P55167, P56442, P56445, P56447, P56448, Q01726, Q29154, Q2AC31, Q5NUL3, Q6A155, Q7TMA4, Q7TQP3, Q80SS9, Q864F4, Q864F6, Q864F7, Q864F8, Q864H5, Q864H7, Q864H8, Q864H9, Q864I4, Q864I6, Q864I7, Q864J1, Q864J2, Q864J3, Q864J4, Q864J5, Q864J7, Q864J8, Q864J9, Q864K0, Q864K2, Q864K3

Diamond homologs: E7EM37, O08530, O08890, O42384, O42385, O77408, O95136, O95977, P08483, P08908, P11483, P19020, P19327, P20309, P21453, P21917, P24628, P28285, P28286, P28565, P30728, P30729, P30939, P30940, P32745, P35345, P35413, P35462, P41149, P41983, P41984, P46089, P46628, P47752, P48303, P51436, P52592, P52703, P53453, P61793

SIGNOR signaling

10 interactions.

A	Effect	B	Mechanism
GSK1292263	up-regulates	GPR119	“chemical activation”
GPR119	“up-regulates activity”	GNAS	binding
GPR119	“up-regulates activity”	GNAL	binding
GPR119	“up-regulates activity”	GNAI1	binding
GPR119	“up-regulates activity”	GNAI3	binding
GPR119	“up-regulates activity”	GNAO1	binding
GPR119	“up-regulates activity”	GNAZ	binding
GPR119	“up-regulates activity”	GNAQ	binding
GPR119	“up-regulates activity”	GNA14	binding
GSK1292263	“up-regulates activity”	GPR119	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	22
Likely benign	4
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

299 predictions. Top by Δscore:

Variant	Effect	Δscore
X:130384818:T:TA	donor_gain	0.9400
X:130384812:A:AC	donor_gain	0.7300
X:130384773:A:AC	donor_gain	0.7200
X:130384774:C:CC	donor_gain	0.7200
X:130384770:A:AC	donor_gain	0.7000
X:130384775:G:C	donor_gain	0.6900
X:130384889:CGCAG:C	acceptor_gain	0.6800
X:130384989:C:A	donor_gain	0.6800
X:130384769:CA:C	donor_gain	0.6500
X:130384893:G:GC	acceptor_gain	0.6500
X:130384893:G:C	acceptor_gain	0.6300
X:130384752:C:CA	donor_gain	0.6200
X:130384814:A:T	donor_gain	0.6100
X:130384594:T:TA	donor_gain	0.6000
X:130384780:G:C	donor_gain	0.6000
X:130384830:T:TA	donor_gain	0.6000
X:130384916:TGG:T	acceptor_gain	0.6000
X:130384914:CATGG:C	acceptor_gain	0.5900
X:130384919:C:CC	acceptor_gain	0.5800
X:130384767:CACA:C	donor_gain	0.5700
X:130385056:A:T	donor_gain	0.5700
X:130384700:C:CT	donor_gain	0.5600
X:130384701:C:CT	donor_gain	0.5500
X:130385330:TGA:T	donor_gain	0.5500
X:130384891:CAG:C	acceptor_gain	0.5300
X:130385094:A:AC	donor_gain	0.5300
X:130385095:C:CC	donor_gain	0.5300
X:130384777:AGAG:A	donor_gain	0.5200
X:130384663:C:CT	donor_gain	0.4900
X:130384656:CAG:C	donor_gain	0.4600

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000032537 (X:130381059 T>A), RS1001134688 (X:130383534 G>T), RS1002103492 (X:130386673 G>T), RS1002539558 (X:130386178 C>A), RS1002553917 (X:130381211 C>A,T), RS1003310680 (X:130383999 T>C), RS1004925992 (X:130382695 C>A,T), RS1007725109 (X:130380083 C>T), RS1008487083 (X:130385170 A>G), RS1008772990 (X:130381631 C>A), RS1008823861 (X:130382126 T>A), RS1009115247 (X:130382460 AG>A), RS1009351971 (X:130383050 A>G), RS1009437218 (X:130386741 G>A), RS1009488188 (X:130387140 G>A)

Disease associations

OMIM: gene MIM:300513 | 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): CHEMBL5652 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

11 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 91,155 (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
CHEMBL1200517	DIHYDROERGOTAMINE MESYLATE	4	2,704
CHEMBL1707	LOPERAMIDE HYDROCHLORIDE	4	59,532
CHEMBL344159	TOLVAPTAN	4	3,645
CHEMBL502182	ELAGOLIX SODIUM	4	214
CHEMBL567	PERPHENAZINE	4	21,883
CHEMBL3187503	GSK-1292263	2	346
CHEMBL3260505	MBX-2982	2	591
CHEMBL405355	NIGULDIPINE	2	1,802
CHEMBL5314955	FIRUGLIPEL	2	38
CHEMBL1951032	ADP-597	1	388
CHEMBL3338194	BMS-903452	1	12

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — GPR18, GPR55 and GPR119

Most potent curated ligand interactions (38 total), top 25:

Ligand	Action	Affinity	Parameter
compound 8g [PMID: 21444206]	Agonist	9.3	pEC50
compound 23 [PMID: 21444206]	Agonist	9.22	pEC50
compound 29a [PMID: 21444206]	Agonist	9.15	pEC50
compound 3j [PMID: 21444206]	Agonist	9.05	pEC50
compound 3a [PMID: 21444206]	Agonist	8.96	pEC50
compound 2 [PMID: 21939274]	Agonist	8.77	pEC50
APD668	Agonist	8.57	pEC50
YH18968	Agonist	8.55	pEC50
compound 36j [PMID: 21536438]	Agonist	8.52	pEC50
compound 58 [PMID: 21273063]	Agonist	8.4	pEC50
AR231453	Agonist	8.2	pEC50
compound 42 [PMID: 22545772]	Agonist	8.1	pEC50
vanoglipel	Agonist	7.83	pEC50
compound 20f [PMID: 21536438]	Agonist	7.74	pEC50
compound 36 [PMID: 21273063]	Agonist	7.72	pEC50
JNJ-38431055	Agonist	7.3	pEC50
DS-8500a	Agonist	7.29	pEC50
compound 3 [PMID: 21310611]	Agonist	7.1	pEC50
N-oleoylethanolamide	Agonist	6.3	pEC50
(R)-N-oleoyltyrosinol	Agonist	6.3	pEC50
(S)-N-oleoyltyrosinol	Agonist	6.2	pEC50
compound 1 [PMID: 21939274]	Agonist	6.1	pEC50
AS1907417	Agonist	6.0	pEC50
AS1535907	Agonist	5.9	pEC50
oleoyl-lysophosphatidylcholine	Agonist	5.8	pEC50

Binding affinities (BindingDB)

450 measured of 471 human assays (477 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
CHEMBL3893596	EC50	0.6 nM
CHEMBL4098760	EC50	1.2 nM
CHEMBL3912040	EC50	1.3 nM
CHEMBL3982536	EC50	1.4 nM
CHEMBL3914281	EC50	1.5 nM
CHEMBL3951013	EC50	1.5 nM
CHEMBL2322841	EC50	1.5 nM
CHEMBL3904015	EC50	1.6 nM
tert-butyl (3R,4S)-4-[cyclopropyl-[4-(1,3-oxazol-5-yl)benzoyl]amino]-3-fluoropiperidine-1-carboxylate	EC50	2 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
CHEMBL4063625	EC50	3.1 nM
CHEMBL3946188	EC50	3.5 nM
CHEMBL4065265	EC50	4.9 nM
CHEMBL4078300	EC50	5.3 nM
CHEMBL4067982	EC50	5.6 nM
CHEMBL3930728	EC50	6.2 nM
CHEMBL4062726	EC50	6.4 nM
tert-butyl (3S,4R)-4-[cyclopropyl-[4-(1,3-oxazol-5-yl)benzoyl]amino]-3-methylpiperidine-1-carboxylate	EC50	7 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
CHEMBL2312159	KI	7 nM
tert-butyl 4-[cyclopropyl-[3-fluoro-4-(1,3-oxazol-5-yl)benzoyl]amino]piperidine-1-carboxylate	EC50	8 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
tert-butyl 4-[cyclopropyl-[3,5-difluoro-4-(1,3-oxazol-5-yl)benzoyl]amino]piperidine-1-carboxylate	EC50	9 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
(1,1,1-trifluoro-2-methylpropan-2-yl) 4-[cyclopropyl-[4-(1,3-oxazol-5-yl)benzoyl]amino]piperidine-1-carboxylate	EC50	10 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
CHEMBL4163003	EC50	10 nM
CHEMBL2322842	EC50	12 nM
tert-butyl 4-[cyclopropyl-[4-(1,3-oxazol-5-yl)benzoyl]amino]-3-methylpiperidine-1-carboxylate	EC50	15 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
tert-butyl 4-[cyclopropyl-[4-(1,3-oxazol-5-yl)benzoyl]amino]-3-methoxypiperidine-1-carboxylate	EC50	15 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
CHEMBL2312158	KI	15 nM
CHEMBL2312506	EC50	16 nM
CHEMBL2312157	KI	18 nM
(1-methylcyclopropyl) 4-[[4-(3-cyano-4-pyridinyl)benzoyl]-cyclopropylamino]piperidine-1-carboxylate	EC50	19 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
tert-butyl 4-[[4-(3-cyano-4-pyridinyl)-3-fluorobenzoyl]-cyclopropylamino]piperidine-1-carboxylate	EC50	21 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
CHEMBL2312156	KI	21 nM
(4R)-3-[2-[4-[2-[di(propan-2-yl)amino]ethoxy]phenyl]-1,3-benzoxazol-6-yl]-4-ethyl-4,5-dihydro-1H-pyridazin-6-one	EC50	22 nM	US-8772323: Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists
(4R,5R)-4-methyl-3-[2-(4-propan-2-yloxyphenyl)-1,3-benzoxazol-6-yl]-5-propyl-4,5-dihydro-1H-pyridazin-6-one	EC50	24 nM	US-8772323: Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists
tert-butyl 4-[[4-(5-cyanothiophen-2-yl)benzoyl]-cyclopropylamino]piperidine-1-carboxylate	EC50	24 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
(6R)-6-ethyl-5-(2-phenyl-6,7-dihydro-4H-[1,3]oxazolo[5,4-c]pyridin-5-yl)-3,6-dihydro-1,3,4-oxadiazin-2-one	EC50	27 nM	US-8772323: Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists
tert-butyl 4-[[4-(3-cyano-4-pyridinyl)benzoyl]-cyclopropylamino]piperidine-1-carboxylate	EC50	27 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
(4R)-4-ethyl-3-[2-(4-propan-2-yloxyphenyl)-1,3-benzoxazol-6-yl]-4,5-dihydro-1H-pyridazin-6-one	EC50	30 nM	US-8772323: Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists
tert-butyl (3S,4R)-4-[cyclopropyl-[4-(1,3-oxazol-5-yl)benzoyl]amino]-3-fluoropiperidine-1-carboxylate	EC50	30 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
6-methyl-5-(2-phenyl-1,3-benzoxazol-6-yl)-3,6-dihydro-1,3,4-oxadiazin-2-one	EC50	31 nM	US-8772323: Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists
tert-butyl 4-[cyclopropyl-[4-(1,3-thiazol-5-yl)benzoyl]amino]piperidine-1-carboxylate	EC50	32 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
tert-butyl 4-[cyclopropyl-[4-(1,3-oxazol-5-yl)benzoyl]amino]piperidine-1-carboxylate	EC50	33 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
CHEMBL2312161	KI	33 nM
tert-butyl 4-[[4-(6-cyano-3-pyridinyl)benzoyl]-cyclopropylamino]piperidine-1-carboxylate	EC50	34 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
cyclopentyl 4-[cyclopropyl-[4-(1,3-oxazol-5-yl)benzoyl]amino]piperidine-1-carboxylate	EC50	34 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
3-[2-[4-[2-[di(propan-2-yl)amino]ethoxy]phenyl]-1,3-benzoxazol-6-yl]-4-ethyl-4,5-dihydro-1H-pyridazin-6-one	EC50	37 nM	US-8772323: Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists
(4S,5S)-4-methyl-3-[2-(4-propan-2-yloxyphenyl)-1,3-benzoxazol-6-yl]-5-propyl-4,5-dihydro-1H-pyridazin-6-one	EC50	37 nM	US-8772323: Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists
(4R,5R)-4-methyl-3-(2-phenyl-1,3-benzoxazol-6-yl)-5-propyl-4,5-dihydro-1H-pyridazin-6-one	EC50	39 nM	US-8772323: Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists
tert-butyl 4-[[4-(4-carbamoylphenyl)benzoyl]-cyclopropylamino]piperidine-1-carboxylate	EC50	39 nM	US-9469631: N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
CHEMBL2312524	EC50	40 nM
(6R)-6-ethyl-5-(2-phenyl-1,3-benzoxazol-6-yl)-3,6-dihydro-1,3,4-oxadiazin-2-one	EC50	41 nM	US-8772323: Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists

ChEMBL bioactivities

1822 potent at pChembl≥5 of 1824 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.70	EC50	0.2	nM	CHEMBL4104464
9.70	EC50	0.2	nM	CHEMBL4093284
9.70	EC50	0.2	nM	CHEMBL1771104
9.52	EC50	0.3	nM	CHEMBL1771098
9.40	EC50	0.4	nM	CHEMBL4098051
9.30	EC50	0.5	nM	CHEMBL3354778
9.30	EC50	0.5	nM	CHEMBL1773283
9.22	EC50	0.6	nM	CHEMBL3893596
9.22	EC50	0.6	nM	CHEMBL1773292
9.19	EC50	0.65	nM	CHEMBL461384
9.17	EC50	0.68	nM	CHEMBL461384
9.15	EC50	0.7	nM	CHEMBL4077033
9.15	EC50	0.7	nM	CHEMBL1773293
9.10	EC50	0.8	nM	CHEMBL3622182
9.10	EC50	0.8	nM	CHEMBL4080222
9.10	EC50	0.8	nM	CHEMBL4060838
9.05	EC50	0.9	nM	CHEMBL1775178
9.00	IC50	1	nM	CHEMBL2382410
9.00	IC50	1	nM	CHEMBL2086684
9.00	EC50	1	nM	CHEMBL3260536
9.00	EC50	1	nM	CHEMBL3354774
9.00	EC50	1	nM	CHEMBL1771081
8.96	EC50	1.1	nM	CHEMBL3622179
8.96	EC50	1.1	nM	CHEMBL1775169
8.92	EC50	1.2	nM	CHEMBL3598101
8.92	EC50	1.2	nM	CHEMBL4098760
8.89	EC50	1.3	nM	CHEMBL3912040
8.85	EC50	1.4	nM	CHEMBL3084479
8.85	EC50	1.4	nM	CHEMBL3982536
8.85	EC50	1.4	nM	CHEMBL5630362
8.82	EC50	1.5	nM	CHEMBL3084479
8.82	EC50	1.5	nM	CHEMBL3084483
8.82	EC50	1.5	nM	CHEMBL3622166
8.82	EC50	1.5	nM	CHEMBL3951013
8.82	EC50	1.5	nM	CHEMBL3914281
8.82	EC50	1.5	nM	CHEMBL4070965
8.82	EC50	1.5	nM	CHEMBL518819
8.80	EC50	1.6	nM	CHEMBL3904015
8.77	EC50	1.7	nM	CHEMBL3622171
8.77	EC50	1.7	nM	CHEMBL3622168
8.77	EC50	1.7	nM	CHEMBL3622181
8.77	EC50	1.7	nM	CHEMBL4639701
8.74	EC50	1.8	nM	CHEMBL4083676
8.74	EC50	1.8	nM	CHEMBL4078300
8.72	EC50	1.9	nM	CHEMBL5630965
8.70	EC50	2	nM	CHEMBL2086693
8.70	EC50	2	nM	CHEMBL2204979
8.70	EC50	2	nM	CHEMBL2204975
8.70	EC50	2	nM	CHEMBL3261136
8.70	EC50	2	nM	CHEMBL3354779

PubChem BioAssay actives

1335 with measured affinity, of 2745 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
4-[3-[2-[3-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]propyl]cyclopropyl]propoxy]-N-cyclopropyl-2-fluorobenzamide	595042: Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay	ec50	0.0002	uM
1-(azetidin-1-yl)-2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]-2-fluorophenyl]ethanone	1430354: Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay	ec50	0.0002	uM
1-(azetidin-1-yl)-2-[2,6-difluoro-4-[2-[(1S,2R)-2-[1-[5-(methoxymethyl)pyrimidin-2-yl]piperidin-4-yl]cyclopropyl]ethoxy]phenyl]ethanone	1430354: Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay	ec50	0.0002	uM
4-[2-[2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]-N-cyclopropyl-2-fluorobenzamide	595042: Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay	ec50	0.0003	uM
1-(azetidin-1-yl)-2-[4-[2-[(1S,2R)-2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]-2-fluorophenyl]ethanone	1430354: Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay	ec50	0.0004	uM
ethyl (3R)-3-benzyl-10-[4-(trifluoromethyl)phenyl]-1,8,12-triazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate	1173651: Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method	ec50	0.0005	uM
tert-butyl 4-[1-(2-fluoro-4-methylsulfonylphenyl)pyrazolo[5,4-d]pyrimidin-4-yl]sulfanylpiperidine-1-carboxylate	596023: Agonist activity at human GPR119 by melanophore assay	ec50	0.0005	uM
propan-2-yl (1R,5R)-3-[6-(2-fluoro-4-methylsulfonylanilino)-5-nitropyrimidin-4-yl]oxy-8-azabicyclo[3.2.1]octane-8-carboxylate	1329812: Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay	ec50	0.0006	uM
N-(2-fluoro-4-methylsulfonylphenyl)-5-nitro-6-[4-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]pyrimidin-4-amine	596023: Agonist activity at human GPR119 by melanophore assay	ec50	0.0006	uM
tert-butyl 4-[[9-(2-fluoro-4-methylsulfonylphenyl)-8-oxo-7H-purin-6-yl]oxy]piperidine-1-carboxylate	596023: Agonist activity at human GPR119 by melanophore assay	ec50	0.0006	uM
tert-butyl 4-[[3-(4-methylsulfonylphenyl)-[1,2]oxazolo[4,5-d]pyrimidin-7-yl]oxy]piperidine-1-carboxylate	596023: Agonist activity at human GPR119 by melanophore assay	ec50	0.0007	uM
1-(azetidin-1-yl)-2-[2-fluoro-4-[2-[(1S,2R)-2-[1-[5-(methoxymethyl)pyrimidin-2-yl]piperidin-4-yl]cyclopropyl]ethoxy]phenyl]ethanone	1430354: Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay	ec50	0.0007	uM
5-[4-[(1R,2R)-2-[(4-ethylsulfonyl-2-fluorophenyl)methoxymethyl]cyclopropyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole	1250113: Agonist activity at human GPR119 expressed in CHO cells by cAMP assay	ec50	0.0008	uM
1-(azetidin-1-yl)-2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]phenyl]ethanone	1430354: Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay	ec50	0.0008	uM
2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]-2-fluorophenyl]-1-(3-hydroxyazetidin-1-yl)ethanone	1430354: Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay	ec50	0.0008	uM
tert-butyl 4-[1-(2-fluoro-4-methylsulfonylphenyl)pyrazolo[5,4-d]pyrimidin-4-yl]oxypiperidine-1-carboxylate	596023: Agonist activity at human GPR119 by melanophore assay	ec50	0.0009	uM
tert-butyl 4-[1-(2-cyano-6-methylpyrimidin-4-yl)piperidin-4-yl]piperidine-1-carboxylate	595042: Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay	ec50	0.0010	uM
ethyl (2R)-2-methyl-2-[6-methyl-3-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]-3-phenylpropanoate	1173651: Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method	ec50	0.0010	uM
tert-butyl (3R)-4-[5-[(3-cyano-4-pyridinyl)methoxy]pyrimidin-2-yl]-3-methylpiperazine-1-carboxylate	747657: Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis	ic50	0.0010	uM
N-(2-methoxyethyl)-N,2-dimethyl-3-phenyl-2-[3-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]propanamide	1141037: Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay	ec50	0.0010	uM
tert-butyl 3-[5-[(3-cyano-4-pyridinyl)methoxy]pyrimidin-2-yl]-3,8-diazabicyclo[3.2.1]octane-8-carboxylate	747657: Displacement of [3H]-N-(2-fluoro-4-methylsulfonyl-phenyl)-6-[4-(3-isopropyl-1,2,4-oxadiazol-5-yl)-1-piperidyl]-5-nitro-pyrimidin-4-amine from human GPR119 overexpressed in baculovirus infected Sf21 cell membranes after 120 mins by scintillation counting analysis	ic50	0.0010	uM
tert-butyl 4-[1-(4-methylsulfonylphenyl)pyrazolo[5,4-d]pyrimidin-4-yl]oxypiperidine-1-carboxylate	596023: Agonist activity at human GPR119 by melanophore assay	ec50	0.0011	uM
2-[4-[(1R,2R)-2-[[3-fluoro-4-(tetrazol-1-yl)phenyl]methoxymethyl]cyclopropyl]piperidin-1-yl]-5-(methoxymethyl)pyrimidine	1250113: Agonist activity at human GPR119 expressed in CHO cells by cAMP assay	ec50	0.0011	uM
tert-butyl (1R,4S,5S)-5-[6-(2-fluoro-4-methylsulfonylanilino)-5-nitropyrimidin-4-yl]oxy-2-azabicyclo[2.2.2]octane-2-carboxylate	1450123: Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay	ec50	0.0012	uM
1,1,1,3,3,3-hexafluoropropan-2-yl 4-[4-(5-methylsulfonylpyrazin-2-yl)oxycyclohexyl]oxypiperidine-1-carboxylate	1237174: Agonist activity at human GPR119 by HTRF cAMP assay	ec50	0.0012	uM
tert-butyl (1R,5R)-3-[[6-(4-cyano-2-fluoroanilino)-5-nitropyrimidin-4-yl]amino]-8-azabicyclo[3.2.1]octane-8-carboxylate	1329812: Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay	ec50	0.0013	uM
ethyl (1R,5R)-3-[6-(2-fluoro-4-methylsulfonylanilino)-5-nitropyrimidin-4-yl]oxy-8-azabicyclo[3.2.1]octane-8-carboxylate	1329812: Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay	ec50	0.0014	uM
tert-butyl 4-[7-(2-fluoro-4-methylsulfonylphenyl)thieno[3,2-d]pyrimidin-4-yl]oxypiperidine-1-carboxylate	2133464: Agonist activity at human GPR119 expressed in CHO-K1 cells preincubated for 5 hrs followed by substrate addition measured after 2 hrs by fluorescence based assay	ec50	0.0014	uM
tert-butyl (1R,5S)-3-[6-(2-fluoro-4-methylsulfonylanilino)-5-nitropyrimidin-4-yl]oxy-8-azabicyclo[3.2.1]octane-8-carboxylate	727514: Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine	ec50	0.0014	uM
tert-butyl (1R,5R)-3-[[6-(2-fluoro-4-methylsulfonylanilino)-5-nitropyrimidin-4-yl]amino]-8-azabicyclo[3.2.1]octane-8-carboxylate	1329812: Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay	ec50	0.0015	uM
tert-butyl (1R,5R)-3-[6-(2-fluoro-4-methylsulfonylanilino)-5-nitropyrimidin-4-yl]oxy-8-azabicyclo[3.2.1]octane-8-carboxylate	1329812: Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay	ec50	0.0015	uM
6-[4-(3-tert-butyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]-N-(4-methylsulfonylphenyl)-5-nitropyrimidin-4-amine	364147: Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation	ec50	0.0015	uM
5-ethyl-2-[4-[(1R,2R)-2-[(5-methylsulfonyl-2-pyridinyl)methoxymethyl]cyclopropyl]piperidin-1-yl]pyrimidine	1250113: Agonist activity at human GPR119 expressed in CHO cells by cAMP assay	ec50	0.0015	uM
tert-butyl (1R,5S)-3-[[6-(2-fluoro-4-methylsulfonylanilino)-5-nitropyrimidin-4-yl]amino]-8-azabicyclo[3.2.1]octane-8-carboxylate	727514: Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine	ec50	0.0015	uM
2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]-2-fluorophenyl]-1-piperidin-1-ylethanone	1430354: Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay	ec50	0.0015	uM
N-(2-fluoro-4-methylsulfonylphenyl)-6-[[(1R,5R)-8-methylsulfonyl-8-azabicyclo[3.2.1]octan-3-yl]oxy]-5-nitropyrimidin-4-amine	1329812: Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay	ec50	0.0016	uM
5-[4-[(1R,2S)-2-[2-(4-ethylsulfonyl-2-fluorophenoxy)ethyl]cyclopropyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole	1250113: Agonist activity at human GPR119 expressed in CHO cells by cAMP assay	ec50	0.0017	uM
4-methyl-6-[6-[4-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]-3-pyridinyl]benzene-1,3-dicarbonitrile	1654496: Agonist activity at human GPR119 expressed in HEK293 cells preincubated for 30 mins followed by d2 cAMP addition and measured after 60 mins by HTRF assay	ec50	0.0017	uM
5-ethoxy-2-[4-[(1R,2R)-2-[(3-fluoro-4-methylsulfonylphenyl)methoxymethyl]cyclopropyl]piperidin-1-yl]pyrimidine	1250113: Agonist activity at human GPR119 expressed in CHO cells by cAMP assay	ec50	0.0017	uM
5-[4-[(1R,2R)-2-[[2-fluoro-4-(tetrazol-1-yl)phenyl]methoxymethyl]cyclopropyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole	1250113: Agonist activity at human GPR119 expressed in CHO cells by cAMP assay	ec50	0.0017	uM
tert-butyl 5-[[6-(2-fluoro-4-methylsulfonylanilino)-5-nitropyrimidin-4-yl]amino]-2-azabicyclo[2.2.2]octane-2-carboxylate	1450123: Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay	ec50	0.0018	uM
2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]phenyl]-N-cyclopropylacetamide	1430354: Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay	ec50	0.0018	uM
3-cyclopentyl-5-[1-[7-(2-fluoro-4-methylsulfonylphenyl)thieno[3,2-d]pyrimidin-4-yl]piperidin-4-yl]-1,2,4-oxadiazole	2133464: Agonist activity at human GPR119 expressed in CHO-K1 cells preincubated for 5 hrs followed by substrate addition measured after 2 hrs by fluorescence based assay	ec50	0.0019	uM
methyl 3-benzyl-10-[4-(trifluoromethyl)phenyl]-1,8,12-triazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate	1173651: Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method	ec50	0.0020	uM
(3S)-3-[(3-fluorophenyl)methyl]-N-(2-methoxyethyl)-N-methyl-10-[4-(trifluoromethyl)phenyl]-1,4,8,12-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxamide	1173651: Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method	ec50	0.0020	uM
methyl (3S)-11-[dideuterio(hydroxy)methyl]-3-[(3-fluorophenyl)methyl]-10-[4-(trifluoromethyl)phenyl]-1,4,8,12-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate	1173651: Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method	ec50	0.0020	uM
[(3R)-3-cyclopropyl-3-[(3-fluorophenyl)methyl]-10-[4-(trifluoromethyl)phenyl]-1,4,8,12-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraen-11-yl]methanol	1173651: Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method	ec50	0.0020	uM
N-ethyl-4-[3-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]triazolo[4,5-c]pyridin-6-yl]-2,5-difluorobenzamide	1487280: Agonist activity at human GPR119 expressed in Flp-In-T-Rex-HEK293 cells assessed as stimulation of cAMP level measured after 30 mins by HTRF assay	ec50	0.0020	uM
4-[[2-[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]piperazin-1-yl]pyrimidin-5-yl]oxymethyl]pyridine-3-carbonitrile	1392145: Agonist activity at GPR119 (unknown origin)	ec50	0.0020	uM
4-[4-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]piperidin-1-yl]-6-methylpyrimidine-2-carbonitrile	595042: Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay	ec50	0.0020	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
beta-lapachone	decreases expression	1
4-aminophenylarsenoxide	decreases reaction, affects binding	1
CGP 52608	affects binding, increases reaction	1
oleoylethanolamide	increases activity, affects binding, decreases reaction	1
Arsenic Trioxide	affects binding, decreases reaction	1
Benzo(a)pyrene	affects methylation, decreases methylation	1
Cadmium	decreases expression	1
Quinoxalines	affects binding, increases activity	1
Aflatoxin B1	decreases methylation	1
Endocannabinoids	affects binding, decreases reaction, increases activity	1

ChEMBL screening assays

184 unique, capped per target: 155 functional, 29 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1107065	Functional	Agonist activity at human GPR119 receptor expressed in CHO-K1 cells co-transfected with 6CRE-Luc after 5 hrs by luciferase reporter gene assay	2,5-Disubstituted pyridines as potent GPR119 agonists. — Bioorg Med Chem Lett
CHEMBL1769549	Binding	Displacement of [3H]isopropyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate/tert-butyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate from GPR119 i	Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response. — J Med Chem

Cellosaurus cell lines

5 cell lines: 2 transformed cell line, 2 cancer cell line, 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_C0SS	ACTOne GPR119	Transformed cell line	Female
CVCL_KZ50	PathHunter HEK 293 GPR119 beta-arrestin	Transformed cell line	Female
CVCL_LA40	PathHunter U2OS GPR119 beta-arrestin	Cancer cell line	Female
CVCL_ZK90	GeneBLAzer T-Rex GPR119-CRE-bla CHO-K1	Spontaneously immortalized cell line	Female
CVCL_ZL13	Tango GPR119-bla U2OS	Cancer cell line	Female

Clinical trials (associated diseases)

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