GPR17

Summary

GPR17 (G protein-coupled receptor 17, HGNC:4471) is a protein-coding gene on chromosome 2q14.3, encoding Uracil nucleotide/cysteinyl leukotriene receptor (Q13304). Dual specificity receptor for uracil nucleotides and cysteinyl leukotrienes (CysLTs).

Predicted to enable G protein-coupled receptor activity. Predicted to be involved in G protein-coupled receptor signaling pathway. Predicted to act upstream of or within negative regulation of inflammatory response to antigenic stimulus. Predicted to be located in membrane. Predicted to be active in plasma membrane.

Source: NCBI Gene 2840 — automated summary from GO annotations (Alliance of Genome Resources).

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 72 total
• GTEx eGene: eQTL in 38 tissues, sQTL in 7 (q < 0.05)
• ChEMBL bioactivity: 5 clinical-phase molecules tested; no curated mechanism-of-action drug
• Constraint (gnomAD): pLI 0.01 (LoF-tolerant), LOEUF 1.89 (unconstrained)
• MANE Select transcript: NM_001161417
• Notable: 72 clinical variants but no curated precision-oncology (CIViC) evidence yet

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4471
Approved symbol	GPR17
Name	G protein-coupled receptor 17
Location	2q14.3
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000144230
Ensembl biotype	protein_coding
OMIM	603071
Entrez	2840

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 7 protein_coding, 1 protein_coding_CDS_not_defined

MANE Select: ENST00000486700

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 3, TSL 3: 1, TSL 4: 1, TSL 5: 1

ENST00000486700, ENST00000272644, ENST00000393018, ENST00000423019, ENST00000496086, ENST00000544369, ENST00000957151, ENST00001143314

RefSeq mRNA: 4 — MANE Select: NM_001161417 NM_001161415, NM_001161416, NM_001161417, NM_005291

CCDS: CCDS2148, CCDS92862

Canonical transcript exons

ENST00000486700 — 2 exons

Exon	Start	End
ENSE00003694249	127650716	127652639
ENSE00003921171	127646153	127646244

Expression profiles

Bgee: expression breadth ubiquitous, 182 present calls, max score 93.60.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 2.6557 / max 524.3901, expressed in 153 samples.

Highest expression (Bgee): apex of heart, sural nerve, mucosa of stomach, muscle layer of sigmoid colon, amygdala.

Genetic regulation across tissues (GTEx eQTL / sQTL)

GPR17 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 38 tissues and its splicing (sQTL) in 7 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 45 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Thyroid	eqtl	6.7e-93	+1.75	2:127648067:C:T
Artery Tibial	eqtl	6.3e-88	+1.94	2:127648067:C:T
Nerve Tibial	eqtl	2.5e-84	+1.44	2:127648067:C:T
Muscle Skeletal	eqtl	5.3e-84	+1.61	2:127648067:C:T
Esophagus Mucosa	eqtl	6.3e-83	+1.56	2:127648067:C:T
Colon Transverse	eqtl	3.4e-79	+1.22	2:127648067:C:T
Adipose Visceral Omentum	eqtl	3.6e-77	+1.74	2:127648067:C:T
Adipose Subcutaneous	eqtl	3.3e-75	+1.56	2:127648067:C:T
Esophagus Muscularis	eqtl	4.2e-75	+1.78	2:127648067:C:T
Lung	eqtl	1.4e-73	+1.68	2:127648067:C:T
Colon Sigmoid	eqtl	2.6e-70	+1.73	2:127648067:C:T
Breast Mammary Tissue	eqtl	1.5e-62	+1.66	2:127648067:C:T
Heart Left Ventricle	eqtl	2.2e-59	+1.57	2:127648067:C:T
Skin Sun Exposed Lower leg	eqtl	1.2e-57	+1.19	2:127648067:C:T
Skin Not Sun Exposed Suprapubic	eqtl	2.0e-56	+1.35	2:127648067:C:T
Heart Atrial Appendage	eqtl	4.7e-56	+1.68	2:127648067:C:T
Esophagus Gastroesophageal Junction	eqtl	2.0e-54	+1.92	2:127648067:C:T
Stomach	eqtl	7.3e-46	+1.24	2:127648067:C:T
Artery Aorta	eqtl	5.4e-45	+1.76	2:127648067:C:T
Testis	eqtl	6.0e-38	+1.55	2:127648067:C:T

FANTOM5 promoters

7 alternative TSS:

Promoter ID	TPM avg	Samples expressed
22447	1.6199	93
22445	0.4593	99
22443	0.3210	105
22446	0.1012	68
22444	0.0606	38
22448	0.0585	18
202380	0.0352	20

Top tissues by expression

showing 100 of 293 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
apex of heart	UBERON:0002098	93.60	gold quality
sural nerve	UBERON:0015488	92.14	gold quality
mucosa of stomach	UBERON:0001199	90.26	gold quality
muscle layer of sigmoid colon	UBERON:0035805	89.52	gold quality
amygdala	UBERON:0001876	87.69	gold quality
lower esophagus muscularis layer	UBERON:0035833	87.31	gold quality
lower esophagus	UBERON:0013473	87.27	gold quality
tibial nerve	UBERON:0001323	87.11	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	86.72	gold quality
right atrium auricular region	UBERON:0006631	86.47	gold quality
body of uterus	UBERON:0009853	86.31	gold quality
left coronary artery	UBERON:0001626	86.24	gold quality
heart left ventricle	UBERON:0002084	85.18	gold quality
descending thoracic aorta	UBERON:0002345	85.09	gold quality
lower esophagus mucosa	UBERON:0035834	85.03	gold quality
thoracic aorta	UBERON:0001515	84.75	gold quality
ascending aorta	UBERON:0001496	84.47	gold quality
aorta	UBERON:0000947	84.04	gold quality
popliteal artery	UBERON:0002250	83.94	gold quality
tibial artery	UBERON:0007610	83.88	gold quality
cardiac ventricle	UBERON:0002082	83.72	gold quality
right lung	UBERON:0002167	83.57	gold quality
cardiac atrium	UBERON:0002081	83.30	gold quality
coronary artery	UBERON:0001621	83.12	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	83.05	gold quality
left uterine tube	UBERON:0001303	82.93	gold quality
temporal lobe	UBERON:0001871	82.49	gold quality
caudate nucleus	UBERON:0001873	82.38	gold quality
spinal cord	UBERON:0002240	82.14	gold quality
inferior vagus X ganglion	UBERON:0005363	81.51	gold quality
Ammon’s horn	UBERON:0001954	81.49	gold quality
nucleus accumbens	UBERON:0001882	81.46	gold quality
heart	UBERON:0000948	81.44	gold quality
upper lobe of left lung	UBERON:0008952	81.28	gold quality
hypothalamus	UBERON:0001898	81.03	gold quality
cingulate cortex	UBERON:0003027	80.98	gold quality
anterior cingulate cortex	UBERON:0009835	80.82	gold quality
prefrontal cortex	UBERON:0000451	80.69	gold quality
right frontal lobe	UBERON:0002810	80.51	gold quality
sigmoid colon	UBERON:0001159	80.45	gold quality
colonic epithelium	UBERON:0000397	80.32	gold quality
omental fat pad	UBERON:0010414	80.32	gold quality
peritoneum	UBERON:0002358	80.21	gold quality
putamen	UBERON:0001874	79.44	gold quality
telencephalon	UBERON:0001893	78.44	gold quality
metanephros cortex	UBERON:0010533	78.29	gold quality
adipose tissue of abdominal region	UBERON:0007808	78.15	gold quality
upper lobe of lung	UBERON:0008948	78.12	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	78.09	gold quality
substantia nigra	UBERON:0002038	78.06	gold quality
right coronary artery	UBERON:0001625	78.05	gold quality
frontal cortex	UBERON:0001870	77.93	gold quality
subcutaneous adipose tissue	UBERON:0002190	77.87	gold quality
gastrocnemius	UBERON:0001388	77.69	gold quality
neocortex	UBERON:0001950	77.67	gold quality
cerebral cortex	UBERON:0000956	77.60	gold quality
esophagus	UBERON:0001043	77.60	gold quality
transverse colon	UBERON:0001157	77.50	gold quality
right lobe of thyroid gland	UBERON:0001119	77.34	gold quality
midbrain	UBERON:0001891	77.03	gold quality
entorhinal cortex	UBERON:0002728	77.02	gold quality
muscle of leg	UBERON:0001383	76.94	gold quality
primary visual cortex	UBERON:0002436	76.83	gold quality
forebrain	UBERON:0001890	76.71	gold quality
Brodmann (1909) area 9	UBERON:0013540	76.54	gold quality
spleen	UBERON:0002106	76.36	gold quality
central nervous system	UBERON:0001017	75.23	gold quality
body of stomach	UBERON:0001161	75.07	gold quality
colon	UBERON:0001155	75.04	gold quality
brain	UBERON:0000955	75.02	gold quality
corpus callosum	UBERON:0002336	74.96	gold quality
endocervix	UBERON:0000458	74.80	gold quality
small intestine Peyer’s patch	UBERON:0003454	74.48	gold quality
left lobe of thyroid gland	UBERON:0001120	73.98	gold quality
large intestine	UBERON:0000059	73.82	gold quality
ectocervix	UBERON:0012249	73.62	gold quality
occipital lobe	UBERON:0002021	72.90	gold quality
intestine	UBERON:0000160	72.75	gold quality
skin of leg	UBERON:0001511	71.98	gold quality
thyroid gland	UBERON:0002046	71.97	gold quality
stomach	UBERON:0000945	71.96	gold quality
small intestine	UBERON:0002108	71.36	gold quality
right lobe of liver	UBERON:0001114	71.07	gold quality
Brodmann (1909) area 46	UBERON:0006483	71.00	silver quality
ventral tegmental area	UBERON:0002691	70.95	gold quality
smooth muscle tissue	UBERON:0001135	70.92	gold quality
vagina	UBERON:0000996	70.81	gold quality
superior frontal gyrus	UBERON:0002661	70.71	gold quality
cranial nerve II	UBERON:0000941	70.38	gold quality
adipose tissue	UBERON:0001013	70.00	gold quality
skin of abdomen	UBERON:0001416	69.96	gold quality
endothelial cell	CL:0000115	69.93	gold quality
esophagus mucosa	UBERON:0002469	69.80	gold quality
skeletal muscle organ	UBERON:0014892	69.62	gold quality
muscle organ	UBERON:0001630	69.61	gold quality
minor salivary gland	UBERON:0001830	69.53	gold quality
Brodmann (1909) area 23	UBERON:0013554	69.34	silver quality
middle temporal gyrus	UBERON:0002771	69.16	gold quality
right hemisphere of cerebellum	UBERON:0014890	68.95	gold quality
gall bladder	UBERON:0002110	68.88	gold quality

Single-cell (SCXA)

Detected in 5 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-HCAD-35	yes	2014.90
E-GEOD-84465	yes	24.53
E-ENAD-17	no	359.21
E-HCAD-30	no	344.13
E-ANND-3	no	1.63

HPA expression

RNA tissue specificity: Tissue enriched

showing 60 of 73 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Caudate putamen	tissue	39.1
Hippocampus	tissue	35.7	medium
Corpus callosum	tissue	35.1
Nucleus accumbens	tissue	31.8
Spinal cord	tissue	31.8
Substantia nigra	tissue	31.0
Frontal cortex	tissue	30.9
Midbrain	tissue	30.0
Thalamus	tissue	29.9
Medulla oblongata	tissue	29.4
Amygdala	tissue	27.5
Hypothalamus	tissue	25.1
Locus coeruleus	tissue	25.1
Ventral forebrain	tissue	24.7
Periaqueductal gray	tissue	24.1
Pons	tissue	23.8
Hippocampal formation	tissue	23.5
Putamen	tissue	23.2
Superior colliculi	tissue	22.7
Septum	tissue	21.5
Olfactory bulb	tissue	18.9
Cerebral cortex	tissue	18.4	medium
Insular cortex	tissue	18.4
Prefrontal cortex	tissue	16.5
Entorhinal cortex	tissue	16.0
Motor cortex	tissue	15.8
Temporal cortex	tissue	15.7
Retrosplenial cortex	tissue	15.6
Basal ganglia	tissue	15.1	medium
Retrosplenial and cingulate cortex	tissue	14.3
Somatosensory cortex	tissue	12.5
Occipital cortex	tissue	12.4
Postcentral gyrus	tissue	10.8
Cerebellum	tissue	10.3	high
Skeletal muscle	tissue	7.9	not detected
Heart muscle	tissue	7.0	not detected
Spleen	tissue	7.0	low
Choroid plexus	tissue	6.9
Endometrium 1	tissue	5.1	not detected
Lung	tissue	4.6	not detected
Skin 1	tissue	3.5	not detected
Appendix	tissue	3.4	not detected
Esophagus	tissue	2.4	not detected
Pancreas	tissue	2.3	not detected
Gallbladder	tissue	2.3	not detected
Vagina	tissue	1.9	not detected
Adipose tissue	tissue	1.9	not detected
Duodenum	tissue	1.7	not detected
Epididymis	tissue	1.4	not detected
Small intestine	tissue	1.3	not detected
Lymph node	tissue	1.2	low
Placenta	tissue	1.2	not detected
Thyroid gland	tissue	1.0	not detected
Adrenal gland	tissue	1.0	not detected
Salivary gland	tissue	0.9	not detected
Prostate	tissue	0.9	not detected
Urinary bladder	tissue	0.8	not detected
Testis	tissue	0.7	not detected
Colon	tissue	0.7	not detected
Stomach 1	tissue	0.6	not detected

Brain sub-regions (HPA Brain Atlas): detected in 189; highest nTPM — Corticomedial amygdala (47.9), Basal amygdala (43.8), Cerebellar white matter (43.8), Ventral medullary reticular nucleus (42.8), Lateral amygdala (41.7).

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

Targeting GPR17 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 71 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-518D-5P	100.00	67.51	979
HSA-MIR-518E-5P	100.00	67.66	954
HSA-MIR-518F-5P	100.00	67.51	979
HSA-MIR-519A-5P	100.00	67.66	954
HSA-MIR-519B-5P	100.00	67.66	954
HSA-MIR-519C-5P	100.00	67.66	954
HSA-MIR-520C-5P	100.00	67.51	979
HSA-MIR-522-5P	100.00	67.66	954
HSA-MIR-523-5P	100.00	67.66	954
HSA-MIR-526A-5P	100.00	67.51	979
HSA-MIR-520G-5P	99.99	66.76	658
HSA-MIR-9-3P	99.96	70.88	2068
HSA-MIR-7-1-3P	99.91	71.53	4384
HSA-MIR-7-2-3P	99.91	71.40	4394
HSA-MIR-4731-5P	99.89	67.23	2537
HSA-MIR-6780A-5P	99.88	66.69	2776
HSA-MIR-4728-5P	99.85	69.39	4718
HSA-MIR-6785-5P	99.82	68.68	4428
HSA-MIR-6515-3P	99.82	68.19	1933
HSA-MIR-1273H-5P	99.77	66.32	2471
HSA-MIR-4658	99.77	64.94	514
HSA-MIR-6790-5P	99.77	65.24	505
HSA-MIR-6752-3P	99.72	66.71	1587
HSA-MIR-149-3P	99.72	68.22	3963
HSA-MIR-4306	99.72	70.50	3630
HSA-MIR-30B-3P	99.70	65.76	2325
HSA-MIR-3689A-3P	99.70	65.73	2306
HSA-MIR-3689B-3P	99.70	65.71	2311
HSA-MIR-3689C	99.70	65.71	2311
HSA-MIR-6779-5P	99.70	65.76	2363

Functional genomics

gnomAD constraint: pLI 0.0138, LOEUF 1.89, missense Z 0.166 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000486700 — one region, missense o/e 1.00.

Literature-anchored findings (GeneRIF, showing 26)

• GPR17, a Gi-coupled orphan receptor at intermediate phylogenetic position between P2Y and CysLT receptors, is specifically activated by both families of endogenous ligands. (PMID:16990797)
• Molecular dynamics simulations suggest that GPR17 nucleotide binding pocket is similar to that described for the other P2Y receptors, although only one of the 3 basic residues that have been typically involved in ligand recognition is conserved (Arg255). (PMID:18533035)
• long-GPR17 isoform is a functional receptor that is stimulated by both uracil nucleotides and cysteinyl leukotrienes (PMID:19625605)
• We present the first isoform-specific characterization of GPR17 and show that differences exist between the isoforms in expression pattern and pharmacological profile; the two human isoforms might serve tissue-specific functions (PMID:20148890)
• REVIEW: functional properties and in vivo biology (PMID:21261596)
• A functional cross-talk exists between cysteinyl-leukotriene and purinergic sites at GPR17; the latter have a hierarchy in producing desensitizing signals. (PMID:21531793)
• analysis of agonist-induced trafficking of native GPR17 in oligodendroglial cells (PMID:23288840)
• Data validate GPR17 as a target for neurorepair (PMID:23801362)
• Nucleotides, nucleotide sugars, and cysteinyl leukotrienes do not promote activation of GPR17 in five different cell lines, nor does GPR17 have signaling properties. (PMID:23908386)
• Data indicate that small molecule MDL29,951 activates human, mouse and rat orphan G protein-coupled receptor GPR17. (PMID:24150254)
• Low levels of GRK2/GRK5 causes a slow and not complete desensitization/down-regulation of GPR17. (PMID:24613411)
• GPR17 gene disruption does not alter food intake or glucose homeostasis in mice. (PMID:25624481)
• This review summarizes knowledge about role of GPR17 receptors in physiology and pathology of nervous system, with special attention to remyelination processes. (PMID:25807830)
• Results show a crucial role of SNX27 in modulating GPR17 levels by means of a post-translational mechanism and highlights the relationship between the trafficking of the receptor through the endomembrane system and oligodendrocyte differentiation; and provide novel evidence of impairment of GPR17 expression and oligodendrocyte maturation in a mouse model of Down syndrome that is characterized by SNX27 down-regulation. (PMID:27270750)
• uracil nucleotides and cysteinyl leukotrienes do not activate human, mouse, or rat GPR17 in various cellular backgrounds. (PMID:28254957)
• In silico and ex vivo validation experiments provided the deep understanding of ligand binding with GPR17 and the present findings reported here may lead to use these two compounds as a potential activator of GPR17 for therapeutic intervention. (PMID:28827203)
• GPR17 may mediate hypoxia injury in RGC-5 cells, while the knockdown of GPR17 can reduce the hypoxia injury (PMID:30693690)
• FLIM-FRET-Based Structural Characterization of a Class-A GPCR Dimer in the Cell Membrane. (PMID:32553728)
• Transcriptomic analysis of glioblastoma multiforme providing new insights into GPR17 signaling communication. (PMID:33140689)
• Microglial vesicles improve post-stroke recovery by preventing immune cell senescence and favoring oligodendrogenesis. (PMID:33309882)
• The Distribution of GPR17-Expressing Cells Correlates with White Matter Inflammation Status in Brain Tissues of Multiple Sclerosis Patients. (PMID:33925469)
• G-protein-coupled receptor GPR17 inhibits glioma development by increasing polycomb repressive complex 1-mediated ROS production. (PMID:34120140)
• Human GPR17 missense variants identified in metabolic disease patients have distinct downstream signaling profiles. (PMID:34144038)
• GPR17 signaling activation by CHBC agonist induced cell death via modulation of MAPK pathway in glioblastoma. (PMID:35016881)
• Insulin-like Growth Factor 1 Promotes Cell Proliferation by Downregulation of G-Protein-Coupled Receptor 17 Expression via PI3K/Akt/FoxO1 Signaling in SK-N-SH Cells. (PMID:35163437)
• Structural analysis of human G-protein-coupled receptor 17 ligand binding sites. (PMID:36791278)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	gpr17	ENSDARG00000062030
mus_musculus	Gpr17	ENSMUSG00000052229
rattus_norvegicus	Gpr17	ENSRNOG00000065480
caenorhabditis_elegans		WBGENE00016570

Paralogs (16): P2RY10 (ENSG00000078589), GPR18 (ENSG00000125245), F2RL3 (ENSG00000127533), GPR55 (ENSG00000135898), LPAR6 (ENSG00000139679), GPR65 (ENSG00000140030), LPAR4 (ENSG00000147145), CYSLTR2 (ENSG00000152207), F2RL2 (ENSG00000164220), F2RL1 (ENSG00000164251), CYSLTR1 (ENSG00000173198), GPR4 (ENSG00000177464), GPR35 (ENSG00000178623), F2R (ENSG00000181104), P2RY8 (ENSG00000182162), GPR20 (ENSG00000204882)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:3584514) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 11 distinct phenotype terms.

Mouse phenotype (MP)	Records
increased neutrophil cell number	1
tremors	1
hindlimb paralysis	1
abnormal myelination	1
abnormal oligodendrocyte morphology	1
seizures	1
postnatal lethality	1
gliosis	1
increased mean platelet volume	1
increased vascular permeability	1
microgliosis	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Pan troglodytes	P60019	100.0%	Diamond
Pan paniscus	Q3SAG9	100.0%	Diamond
Gorilla gorilla gorilla	Q6XCF2	100.0%	Diamond
Gallus gallus	P34996	99.7%	Diamond
Meleagris gallopavo	P49652	99.7%	Diamond
Chlorocebus pygerythrus	Q8HZP3	99.7%	Diamond
Sus scrofa	P79291	99.6%	Diamond
Macaca mulatta	O97664	99.2%	Diamond
Macaca fascicularis	Q95LH1	99.2%	Diamond
Cricetulus griseus	P58825	98.8%	Diamond
Meriones unguiculatus	Q99PE3	98.8%	Diamond
Papio hamadryas	P56488	97.9%	Diamond
Bos taurus	P48042	96.8%	Diamond
Procambarus clarkii	P35356	96.7%	Diamond
Cavia porcellus	P59902	96.2%	Diamond
Cricetulus longicaudatus	Q00991	89.5%	Diamond
Todarodes pacificus	P31356	87.2%	Diamond
Human herpesvirus 5 strain Merlin	F5HDK1	96.0%	Diamond
Human herpesvirus 5 strain AD169	P09703	94.8%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
WDR33	protein-coding	55339
LIMS2	protein-coding	55679
SFT2D3	protein-coding	84826
MYO7B	protein-coding	4648
IWS1	protein-coding	55677
MYO7B-AS1	ncRNA	101927834

Protein

Protein identifiers

Uracil nucleotide/cysteinyl leukotriene receptor — Q13304 (reviewed: Q13304)

Alternative names: G protein-coupled receptor 17, P2Y-like receptor, R12

All UniProt accessions (3): C9JWY5, Q13304, G4XH68

UniProt curated annotations — full annotation on UniProt →

Function. Dual specificity receptor for uracil nucleotides and cysteinyl leukotrienes (CysLTs). Signals through G(i) and inhibition of adenylyl cyclase. May mediate brain damage by nucleotides and CysLTs following ischemia.

Subcellular location. Cell membrane.

Tissue specificity. Expressed in brain, kidney, heart and umbilical vein endothelial cells. Highest level in brain.

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

Isoforms (2)

UniProt ID	Names	Canonical?
Q13304-1	1	yes
Q13304-2	2

RefSeq proteins (4): NP_001154887, NP_001154888, NP_001154889, NP_005282 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (39 total): helix 13, topological domain 8, transmembrane region 7, glycosylation site 3, strand 2, chain 1, region of interest 1, disulfide bond 1, splice variant 1, sequence conflict 1, turn 1

Structure

Experimental structures (PDB)

1 structures by resolution:

PDB	Title	Method	Resolution (Å)
7Y89	Structure of the GPR17-Gi complex	ELECTRON MICROSCOPY	3.02

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q13304-F1	80.73	0.50

Antibody-complex structures (SAbDab)

1 antibodies co-crystallized with this protein: 7Y89

Human Protein Atlas

Protein class: G-protein coupled receptors, GPCRs excl olfactory receptors, Predicted membrane proteins, GPCRHMM predicted membrane proteins

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): vesicles

Antibody reliability (HPA): IH enhanced · IF approved

Functional residue map

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

Disulfide bonds (1)

Type	Positions
Disulfide bond	132–209

Glycosylation sites (3)

Type	Positions
N-linked (glcnac…) asparagine	42, 204, 282

Function

Pathways and Gene Ontology

Reactome pathways

4 curated (TAS) of 11; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

11 pathways:

ID	Pathway	Evidence
R-HSA-418594	G alpha (i) signalling events	curated
R-HSA-416476	G alpha (q) signalling events	curated
R-HSA-391906	Leukotriene receptors	curated
R-HSA-417957	P2Y receptors	curated
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)	—
R-HSA-391903	Eicosanoid ligand-binding receptors	—
R-HSA-388396	GPCR downstream signalling	—
R-HSA-500792	GPCR ligand binding	—
R-HSA-418038	Nucleotide-like (purinergic) receptors	—
R-HSA-162582	Signal Transduction	—
R-HSA-372790	Signaling by GPCR	—

MSigDB gene sets: 115 (showing top): GOBP_REGULATION_OF_INFLAMMATORY_RESPONSE_TO_ANTIGENIC_STIMULUS, GOBP_INFLAMMATORY_RESPONSE, REACTOME_EICOSANOID_LIGAND_BINDING_RECEPTORS, GOBP_RESPONSE_TO_PEPTIDE, REACTOME_P2Y_RECEPTORS, GOBP_NEUROGENESIS, GGGTGGRR_PAX4_03, CAGCTG_AP4_Q5, GOBP_REGULATION_OF_IMMUNE_RESPONSE, MODULE_289, GOBP_REGULATION_OF_RESPONSE_TO_STRESS, GOBP_NEGATIVE_REGULATION_OF_DEFENSE_RESPONSE, GOBP_NEGATIVE_REGULATION_OF_INFLAMMATORY_RESPONSE, GOBP_INFLAMMATORY_RESPONSE_TO_ANTIGENIC_STIMULUS, MODULE_88

GO Biological Process (4): G protein-coupled receptor signaling pathway (GO:0007186), oligodendrocyte differentiation (GO:0048709), signal transduction (GO:0007165), chemokine-mediated signaling pathway (GO:0070098)

GO Molecular Function (4): G protein-coupled receptor activity (GO:0004930), chemokine receptor activity (GO:0004950), receptor serine/threonine kinase binding (GO:0033612), protein binding (GO:0005515)

GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

7 top-level categories:

Category	Pathways
GPCR downstream signalling	2
Signaling by GPCR	2
Class A/1 (Rhodopsin-like receptors)	2
Eicosanoid ligand-binding receptors	1
Nucleotide-like (purinergic) receptors	1
Signal Transduction	1
GPCR ligand binding	1

GO top-level categories

22 GO namespaces:

Category	Terms
G protein-coupled receptor signaling pathway	2
G protein-coupled receptor activity	1
signal transduction	1
central nervous system development	1
glial cell differentiation	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
cytokine-mediated signaling pathway	1
cellular response to chemokine	1
transmembrane signaling receptor activity	1
G protein-coupled chemoattractant receptor activity	1
cytokine receptor activity	1
chemokine binding	1
chemokine-mediated signaling pathway	1
signaling receptor binding	1
binding	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

showing 15 of 900 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GPR17	ITGA4	P13612	702
GPR17	P0DN79	P0DN79	636
GPR17	MBP	P02686	575
GPR17	ITGAL	P20701	547
GPR17	OLIG1	Q8TAK6	546
GPR17	OLIG2	Q13516	545
GPR17	PDGFRA	P16234	544
GPR17	CNP	P09543	509
GPR17	ENPP6	Q6UWR7	502
GPR17	MYRF	Q9Y2G1	497
GPR17	PLP1	P04400	492
GPR17	BCAS1	O75363	485
GPR17	GPR37	O15354	463
GPR17	SOX10	P56693	453
GPR17	SELL	P14151	451

IntAct

Human interaction partners of GPR17 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

5 partners by confidence:

Partner	Interaction type	MIscore	Records
IPO8	association	0.530	1
PDZK1	direct interaction	0.440	1
GPR37	physical association	0.370	1
C1QTNF9B	association	0.350	1
TMEM120B	association	0.350	1

BioGRID (280 interactions; top human partners by supporting records): AARS2 (Affinity Capture-MS), ABCB8 (Affinity Capture-MS), ABHD17B (Affinity Capture-MS), ADCK1 (Affinity Capture-MS), ADCK4 (Affinity Capture-MS), ADRBK1 (Affinity Capture-Luminescence), ALG10 (Affinity Capture-MS), ALG8 (Affinity Capture-MS), ANAPC7 (Affinity Capture-MS), ARFGEF1 (Affinity Capture-MS), ARFGEF2 (Affinity Capture-MS), ARMC6 (Affinity Capture-MS), ARMC9 (Affinity Capture-MS), ATL2 (Affinity Capture-MS), ATL3 (Affinity Capture-MS)

SIGNOR signaling

6 signaling interactions:

A	Effect	B	Mechanism
GPR17	“up-regulates activity”	GNAI1	binding
GPR17	“up-regulates activity”	GNAI3	binding
GPR17	“up-regulates activity”	GNAO1	binding
GPR17	“up-regulates activity”	GNAQ	binding
“3-(2-Carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid”	“up-regulates activity”	GPR17	“chemical activation”
GRK2	“down-regulates activity”	GPR17	phosphorylation

Ligand–receptor pairs (CellPhoneDB) (3)

Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.

3 ligand–receptor pairs:

Partner	This gene’s role	Signaling class
ALOX5AP;ALOX5;LTC4S	receptor	Signaling by Lipoxin/Leukotriene
GGT1;GGT5	receptor	Signaling by Lipoxin/Leukotriene
LTA4H	receptor	Signaling by Lipoxin/Leukotriene

Disease & clinical

Genetic variants

Variant evidence for GPR17: 72 ClinVar records (0 pathogenic / likely pathogenic); 1 GWAS association.

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	56
Likely benign	10
Benign	3

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 24 predictions of 297):

Position(s)	Effect	Δscore	Sites
2:127646245–127646246	donor_loss	0.9900	4
2:127650714–127650715	acceptor_loss	0.9900	6
2:127646245	donor_loss	0.9300
2:127650704	acceptor_loss	0.9300
2:127648220	donor_gain	0.8600
2:127648248	donor_gain	0.8600
2:127648287–127648288	donor_loss	0.8300	6
2:127648286	donor_loss	0.8200	2
2:127649523	donor_gain	0.8100
2:127648286	donor_loss	0.7900

AlphaMissense

727 missense substitutions predicted likely pathogenic (of 2,190 scored), across 212 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
D105	8	0.975	0.989
D321	8	0.958	0.988
D156	8	0.951	0.975
N77	8	0.941	0.986
F229	8	0.923	0.993
F276	8	0.922	0.994
H280	8	0.919	0.982
F84	8	0.901	0.969
F149	8	0.802	0.931
C209	7	0.989	0.995
C132	7	0.987	0.994
W125	7	0.971	0.997
F97	7	0.938	0.972
F272	7	0.935	0.983
F332	7	0.917	0.985
W184	7	0.914	0.995
F139	7	0.893	0.966
F137	7	0.878	0.972
S146	7	0.873	0.994
F158	7	0.866	0.956

HPA cancer prognostics

RNA cancer specificity: Cancer enriched (Glioblastoma Multiforme)

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

1 prognostic cancer types:

Cancer	Prognostic	p-value
Lung Adenocarcinoma (validation)	favorable	0.00072

Disease associations

OMIM: gene MIM:603071 | disease phenotypes:

GWAS associations

1 associations:

Study	Trait	p-value
GCST010916_8	Proportion of activated microglia (inferior temporal cortex)	3e-6

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1075162 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 197,911 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

5 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL1097279	CANGRELOR TETRASODIUM	4	115
CHEMBL6	INDOMETHACIN	4	157,305
CHEMBL787	MONTELUKAST	4	26,923
CHEMBL21333	PRANLUKAST	4	12,846
CHEMBL44793	GAVESTINEL	2	722

PharmGKB: 1 entry (CPIC guideline: no)

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Mas1, BB₃/Brs3, GPR17

Most potent curated ligand interactions (19 total), top 19:

Ligand	Action	Affinity	Parameter
ASN02563583	Agonist	9.96	pEC50
ASN04885796	Agonist	9.96	pEC50
ASN06917370	Agonist	9.57	pEC50
UDP-glucose	Agonist	9.52	pEC50
LTE4	Agonist	9.51	pEC50
LTC4	Agonist	9.48	pEC50
ASN04450772	Agonist	8.93	pEC50
UDP-galactose	Agonist	8.92	pEC50
cangrelor	Antagonist	8.92	pIC50
UDP	Agonist	8.8	pEC50
ASN04421891	Agonist	8.44	pEC50
I-116	Antagonist	8.39	pIC50
LTD4	Agonist	8.36	pEC50
PSB-18422	Agonist	7.55	pEC50
ATP	Agonist	7.43	pEC50
montelukast	Antagonist	7.21	pIC50
PSB-24040	Antagonist	7.08	pKi
MDL 29,951	Full agonist	6.48	pEC50
8-methylamino inosinic acid	Antagonist	6.27	pIC50

Binding affinities (BindingDB)

347 measured of 399 human assays (401 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
((2R,3S,4R,5R)-5-(6-amino-2-(phenylethynyl)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyltriphosphate tetraammonium salt	EC50	0.036 nM
cangrelor	IC50	0.7 nM
((2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyltriphosphate tetraammonium salt	EC50	1.4 nM
((2R,3S,4R,5R)-5-(6-chloro-4-(methylamino)-1H-imidazo[4,5-c]pyridin-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyltriphosphate tetraammonium salt	EC50	1.7 nM
CHEBI:6993	IC50	2.3 nM
6-chloro-N-[5-(3- fluoropropyl)-4,6-dimethoxy- pyrimidin-2-yl]-1H-indole-3- sulfonamide	IC50	7 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-7- (difluoromethylthio)-N-[5-(2- fluoroethoxy)-4,6-dimethoxy- pyrimidin-2-yl]-1H-indole-3- sulfonamide	IC50	7 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
CHEMBL5172549	KD	7.5 nM
6-chloro-N-[5-(2,2- difluoroethyl)-4,6-dimethoxy- pyrimidin-2-yl]-1H-indole-3- sulfonamide	IC50	8 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(2,2- difluoroethyl)-4-methoxy- pyrimidin-2-yl]-7- (difluoromethylsulfanyl)-1H- indole-3-sulfonamide	IC50	8 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(2-cyanoethyl)- 4,6-dimethoxy-pyrimidin-2- yl]-1H-indole-3-sulfonamide	IC50	9 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-bromo-N-[5-(2-cyanoethyl)- 4,6-dimethoxy-pyrimidin-2- yl]-7-fluoro-1H-indole-3- sulfonamide	IC50	9 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-bromo-N-[5-(2-cyanoethyl)- 4,6-dimethoxy-pyrimidin-2- yl]-1H-indole-3-sulfonamide	IC50	10 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
((2R,3S,4R,5R)-5-(2-chloro-6-(methylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyltriphosphate tetraammonium salt	EC50	11 nM
6-chloro-N-[5-(2- fluoroethoxy)-4,6-dimethoxy- pyrimidin-2-yl]-1H-indole-3- sulfonamide	IC50	11 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
N-[5-(2-cyanoethyl)-4,6- dimethoxy-pyrimidin-2-yl]-6- (difluoromethyl)-1H-indole-3- sulfonamide	IC50	11 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-bromo-N-(4,6-dimethoxy-5- methyl-pyrimidin-2-yl)-1H- pyrrolo[2,3-b]pyridine-3- sulfonamide	IC50	11 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(3- fluoropropyl)-4-methoxy- pyrimidin-2-yl]-1H-indole-3- sulfonamide	IC50	12 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(3,3- difluoropropyl)-4,6- dimethoxy-pyrimidin-2-yl]- 1H-indole-3-sulfonamide	IC50	12 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(2-cyanoethyl)- 4,6-dimethoxy-pyrimidin-2- yl]-7-(difluoromethylthio)-1H- indole-3-sulfonamide	IC50	12 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
((2R,3S,4R,5R)-3,4-dihydroxy-5-(5-iodo-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)methyl trihydrogen diphosphate	EC50	13 nM
N-(5-allyl-4,6-dimethoxy- pyrimidin-2-yl)-6-chloro-1H- indole-3-sulfonamide	IC50	13 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(2-fluoroethyl)- 4,6-dimethoxy-pyrimidin-2- yl]-1H-indole-3-sulfonamide	IC50	13 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-bromo-N-[5-(2,3-difluoropropyl)-4,6-dimethoxypyrimidin-2-yl]-1H-pyrrolo[2,3-b]pyridine-3-sulfonamide	IC50	13 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(2,2- difluoroethyl)-4-methoxy- pyrimidin-2-yl]-7-methoxy-1H- indole-3-sulfonamide	IC50	13 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
7-bromo-6-chloro-N-[5-(2,2-difluoroethyl)-4,6-dimethoxypyrimidin-2-yl]-1H-indole-3-sulfonamide	IC50	13 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-(5-cyclopropyl- 4,6-dimethoxy-pyrimidin-2- yl)-1H-indole-3-sulfonamide	IC50	14 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
N-[5-(2,2-difluoroethoxy)-4,6- dimethoxy-pyrimidin-2-yl]-6- (difluoromethyl)-1H-indole-3- sulfonamide	IC50	14 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(2-cyanoethyl)- 4-methoxy-pyrimidin-2-yl]-7- (difluoromethylthio)-1H- indole-3-sulfonamide	IC50	14 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
7-bromo-6-chloro-N-[5-(2- fluoroethoxy)-4-methoxy- pyrimidin-2-yl]-1H-indole-3- sulfonamide	IC50	14 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(3,3- difluoropropyl)-4-methoxy- pyrimidin-2-yl]-7-fluoro-1H- indole-3-sulfonamide	IC50	14 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(2-cyanoethyl)- 4,6-dimethoxy-pyrimidin-2- yl]-7-fluoro-1H-indole-3- sulfonamide	IC50	14 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
N-[5-(2,2-difluoroethyl)-4,6- dimethoxy-pyrimidin-2-yl]-6- (difluoromethyl)-1H-indole-3- sulfonamide	IC50	14 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
N-[5-(2-cyanoethyl)-4,6-dimethoxypyrimidin-2-yl]-6-(difluoromethyl)-7-fluoro-1H-indole-3-sulfonamide	IC50	14 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5- (cyanomethoxy)-4,6- dimethoxy-pyrimidin-2-yl]- 1H-indole-3-sulfonamide	IC50	14 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-bromo-N-[5-(difluoromethoxy)-4,6-dimethoxypyrimidin-2-yl]-1H-pyrrolo[2,3-b]pyridine-3-sulfonamide	IC50	15 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-bromo-N-[5-(3,3- difluoropropyl)-4,6- dimethoxy-pyrimidin-2-yl]- 1H-pyrrolo[2,3-b]pyridine-3- sulfonamide	IC50	16 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(3,3- difluoropropyl)-4,6- dimethoxy-pyrimidin-2-yl]- 1H-pyrrolo[2,3-b]pyridine-3- sulfonamide	IC50	16 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-bromo-N-[5-(2,2- difluoroethyl)-4-methoxy- pyrimidin-2-yl]-7-methoxy-1H- indole-3-sulfonamide	IC50	16 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(2,2- difluoroethyl)-4-methoxy- pyrimidin-2-yl]-7- (methylthio)-1H-indole-3- sulfonamide	IC50	16 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-bromo-N-[5- (cyanomethoxy)-4,6- dimethoxy-pyrimidin-2-yl]-7- fluoro-1H-indole-3- sulfonamide	IC50	16 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(2,2- difluoroethoxy)-4,6- dimethoxy-pyrimidin-2-yl]- 1H-indole-3-sulfonamide	IC50	17 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[4,6-dimethoxy-5- (1,1,2- trifluoroethoxy)pyrimidin-2- yl]-1H-indole-3-sulfonamide	IC50	17 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-(4,6-dimethoxy-5- propyl-pyrimidin-2-yl)-1H- indole-3-sulfonamide	IC50	17 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(2,2- difluoroethyl)-4,6-dimethoxy- pyrimidin-2-yl]-7-fluoro-1H- indole-3-sulfonamide	IC50	17 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-bromo-N-[5-(2,2- difluoroethoxy)-4,6- dimethoxy-pyrimidin-2-yl]- 1H-indole-3-sulfonamide	IC50	18 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5-(3,3- difluoropropyl)-4-methoxy- pyrimidin-2-yl]-7-methoxy-1H- indole-3-sulfonamide	IC50	18 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6,7-dichloro-N-[5-(2,2- difluoroethyl)-4-methoxy- pyrimidin-2-yl]-1H-indole-3- sulfonamide	IC50	18 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-[5- (cyanomethoxy)-4,6- dimethoxy-pyrimidin-2-yl]-7- fluoro-1H-indole-3- sulfonamide	IC50	18 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
6-chloro-N-(4,6-dimethoxy-5- methyl-pyrimidin-2-yl)-1H- indole-3-sulfonamide	IC50	19 nM	US-20240025883: PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES

ChEMBL bioactivities

208 potent at pChembl≥5 of 227 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.44	EC50	0.036	nM	CHEMBL1097652
9.15	IC50	0.7	nM	CANGRELOR TETRASODIUM
8.85	EC50	1.4	nM	CHEMBL1096742
8.77	EC50	1.7	nM	CHEMBL1098419
8.20	EC50	6.31	nM	CHEMBL31344
8.14	IC50	7.244	nM	CHEMBL6103168
8.10	IC50	7.943	nM	CHEMBL6150589
8.05	Ki	8.913	nM	CHEMBL6102166
7.96	EC50	11	nM	CHEMBL1098083
7.87	EC50	13.49	nM	CHEMBL3132880
7.74	IC50	18.2	nM	CHEMBL6102339
7.71	IC50	19.5	nM	CHEMBL6102166
7.69	EC50	20.42	nM	CHEMBL295718
7.55	EC50	27.9	nM	CHEMBL4216761
7.49	EC50	32.1	nM	CHEMBL4205476
7.48	IC50	33.11	nM	CHEMBL6150589
7.40	EC50	39.81	nM	CHEMBL31344
7.38	EC50	41.69	nM	CHEMBL31344
7.35	IC50	45	nM	CHEMBL6165955
7.20	IC50	63.1	nM	CHEMBL6145657
7.17	EC50	67	nM	CHEMBL4215280
7.16	IC50	69	nM	CHEMBL6142632
7.10	IC50	79.43	nM	CHEMBL6102055
7.10	IC50	79.43	nM	CHEMBL6144714
7.10	IC50	79.43	nM	CHEMBL6103168
7.10	IC50	79.43	nM	CHEMBL6102339
7.08	Ki	83.18	nM	CHEMBL6150589
7.07	IC50	85	nM	CHEMBL6143347
7.05	IC50	89.13	nM	CHEMBL6103168
7.05	Ki	89.13	nM	CHEMBL6102339
7.00	IC50	100	nM	CHEMBL6102740
7.00	IC50	100	nM	CHEMBL6102166
7.00	IC50	100	nM	CHEMBL6150589
7.00	IC50	99	nM	CHEMBL6165919
6.99	EC50	103	nM	CHEMBL4203088
6.95	IC50	112	nM	CHEMBL1094109
6.94	EC50	115	nM	CHEMBL4206497
6.93	EC50	117	nM	CHEMBL4209219
6.90	IC50	125.9	nM	CHEMBL6078081
6.90	IC50	125.9	nM	CHEMBL6133052
6.90	IC50	125.9	nM	CHEMBL6149147
6.90	IC50	125.9	nM	CHEMBL6147862
6.90	IC50	125.9	nM	CHEMBL6102166
6.88	IC50	131.8	nM	CHEMBL6144714
6.86	Ki	138	nM	CHEMBL6145658
6.80	IC50	158.5	nM	CHEMBL6145943
6.80	IC50	158.5	nM	CHEMBL6102152
6.79	EC50	162.2	nM	CHEMBL53914
6.79	IC50	162.2	nM	CHEMBL6133618
6.73	EC50	186.2	nM	CHEMBL3921330

PubChem BioAssay actives

188 with measured affinity, of 389 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
[[(2R,3S,4R,5R)-5-[6-amino-2-(2-phenylethynyl)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate;azane	480270: Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay	ec50	<0.0001	uM
tetrasodium;[dichloro(phosphonato)methyl]-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(2-methylsulfanylethylamino)-2-(3,3,3-trifluoropropylsulfanyl)purin-9-yl]oxolan-2-yl]methoxy-oxidophosphoryl]oxyphosphinate	480271: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay	ic50	0.0007	uM
azane;[[(2R,3S,4R,5R)-5-[6-(cyclopentylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	480270: Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay	ec50	0.0014	uM
azane;[[(2R,3S,4R,5R)-5-[6-chloro-4-(methylamino)imidazo[4,5-c]pyridin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	480270: Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay	ec50	0.0017	uM
5-methoxy-2-[[5-(2-phenylphenyl)furan-2-carbonyl]amino]benzoic acid	2207384: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced cAMP decrease preincubated for 30 mins followed by MDL29,951 addition and measured after 60 mins in presence of forskolin by fluorescence based assay	ic50	0.0072	uM
5-methoxy-2-[[5-[2-[3-(trifluoromethyl)phenyl]phenyl]furan-2-carbonyl]amino]benzoic acid	2207384: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced cAMP decrease preincubated for 30 mins followed by MDL29,951 addition and measured after 60 mins in presence of forskolin by fluorescence based assay	ic50	0.0079	uM
5-methoxy-2-[[5-[2-(3-methoxyphenyl)phenyl]furan-2-carbonyl]amino]benzoic acid	2207393: Displacement of [3H]PSB-12150 from human GPR17 expressed in Flp-In T-REx system generated CHO cell membrane incubated for 1 hrs by liquid scintillation counter analysis	ki	0.0089	uM
azane;[[(2R,3S,4R,5R)-5-[2-chloro-6-(methylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	480270: Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay	ec50	0.0110	uM
5-methoxy-2-[[5-[2-(4-methoxyphenyl)phenyl]furan-2-carbonyl]amino]benzoic acid	2207384: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced cAMP decrease preincubated for 30 mins followed by MDL29,951 addition and measured after 60 mins in presence of forskolin by fluorescence based assay	ic50	0.0182	uM
6-bromo-3-(2-carboxyethyl)-4-fluoro-1H-indole-2-carboxylic acid	1385395: Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ec50	0.0279	uM
3-(2-carboxyethyl)-4-fluoro-6-iodo-1H-indole-2-carboxylic acid	1385395: Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ec50	0.0321	uM
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid	2207387: Agonist activity at human GPR17 expressed in HEK293 cells co-expressing Galphai2 assessed as increase in BRET ratio of RLUcII-tagged Galphai/o effector Rap1GAP-RLucII and membrane tethered rGFP-CAAX incubated for 5 mins by G protein effector membrane translocation assay	ec50	0.0398	uM
N-[5-(2-cyanoethyl)-4,6-dimethoxypyrimidin-2-yl]-5-(3-fluoro-2-pyridinyl)-1H-pyrrole-3-sulfonamide	2236111: Antagonist activity at untagged human GPR17S stably expressed in CHO-K1 cells assessed as inhibition of MDL29,951/IBMX-induced cAMP reduction preincubated for 5 mins followed by forskolin addition and measured after 30 mins by TR-FRET assay	ic50	0.0450	uM
5-methoxy-2-[[5-[2-[3-(2-methoxyethoxy)phenyl]phenyl]furan-2-carbonyl]amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.0631	uM
3-(2-carboxyethyl)-4-chloro-6-hexoxy-1H-indole-2-carboxylic acid	1385395: Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ec50	0.0670	uM
N-[5-(2-cyanoethyl)-4,6-dimethoxypyrimidin-2-yl]-5-(1,3-thiazol-2-yl)-1H-pyrrole-3-sulfonamide	2236111: Antagonist activity at untagged human GPR17S stably expressed in CHO-K1 cells assessed as inhibition of MDL29,951/IBMX-induced cAMP reduction preincubated for 5 mins followed by forskolin addition and measured after 30 mins by TR-FRET assay	ic50	0.0690	uM
2-[[5-(2-phenylphenyl)furan-2-carbonyl]amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.0794	uM
5-methoxy-2-[(2-naphthalen-1-yl-1,3-thiazole-4-carbonyl)amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.0794	uM
N-[5-(2-fluoroethoxy)-4,6-dimethoxypyrimidin-2-yl]-5-(3-fluoro-2-pyridinyl)-1H-pyrrole-3-sulfonamide	2236111: Antagonist activity at untagged human GPR17S stably expressed in CHO-K1 cells assessed as inhibition of MDL29,951/IBMX-induced cAMP reduction preincubated for 5 mins followed by forskolin addition and measured after 30 mins by TR-FRET assay	ic50	0.0850	uM
N-[5-(2,2-difluoroethoxy)-4,6-dimethoxypyrimidin-2-yl]-5-(3-fluoro-2-pyridinyl)-1H-pyrrole-3-sulfonamide	2236111: Antagonist activity at untagged human GPR17S stably expressed in CHO-K1 cells assessed as inhibition of MDL29,951/IBMX-induced cAMP reduction preincubated for 5 mins followed by forskolin addition and measured after 30 mins by TR-FRET assay	ic50	0.0990	uM
6-chloro-N-(4-chloro-5-methyl-1,2-thiazol-3-yl)-1H-indole-3-sulfonamide	2264787: Inhibition of full length GPR17 (unknown origin) stably expressed in human 1321N1 cells incubated for 15 mins by cAMP based HTRF assay	ic50	0.1000	uM
6-chloro-N-[1-(2-chloroethyl)-5-cyanopyrazol-4-yl]-1H-indole-3-sulfonamide	2264787: Inhibition of full length GPR17 (unknown origin) stably expressed in human 1321N1 cells incubated for 15 mins by cAMP based HTRF assay	ic50	0.1000	uM
6-chloro-N-(5-cyano-1-propylpyrazol-4-yl)-1H-indole-3-sulfonamide	2264787: Inhibition of full length GPR17 (unknown origin) stably expressed in human 1321N1 cells incubated for 15 mins by cAMP based HTRF assay	ic50	0.1000	uM
6-chloro-N-[5-cyano-1-(3,3,3-trifluoropropyl)pyrazol-4-yl]-1H-indole-3-sulfonamide	2264787: Inhibition of full length GPR17 (unknown origin) stably expressed in human 1321N1 cells incubated for 15 mins by cAMP based HTRF assay	ic50	0.1000	uM
6-chloro-N-[5-(trifluoromethyl)-1,3-thiazol-2-yl]-1H-indole-3-sulfonamide	2264787: Inhibition of full length GPR17 (unknown origin) stably expressed in human 1321N1 cells incubated for 15 mins by cAMP based HTRF assay	ic50	0.1000	uM
2-[[5-[2-(3-methoxyphenyl)phenyl]furan-2-carbonyl]amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1000	uM
5,6-dichloro-N-(4-chloro-5-methyl-1,2-oxazol-3-yl)-1H-indole-3-sulfonamide	2264787: Inhibition of full length GPR17 (unknown origin) stably expressed in human 1321N1 cells incubated for 15 mins by cAMP based HTRF assay	ic50	0.1000	uM
3-(2-carboxyethyl)-4-chloro-6-pentoxy-1H-indole-2-carboxylic acid	1385395: Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ec50	0.1030	uM
azane;[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(methylamino)purin-9-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	480271: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay	ic50	0.1120	uM
3-(2-carboxyethyl)-6-hexoxy-1H-indole-2-carboxylic acid	1385395: Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ec50	0.1150	uM
3-(2-carboxyethyl)-4-chloro-6-octoxy-1H-indole-2-carboxylic acid	1385395: Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ec50	0.1170	uM
5-methoxy-2-[(6-naphthalen-1-ylpyridine-2-carbonyl)amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1259	uM
5-methyl-2-[(5-naphthalen-1-ylfuran-2-carbonyl)amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1259	uM
2-[(5-naphthalen-1-ylfuran-2-carbonyl)amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1259	uM
5-methoxy-2-[[5-[2-(3-propan-2-ylphenyl)phenyl]furan-2-carbonyl]amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1259	uM
5-fluoro-2-[[5-(2-propan-2-ylphenyl)furan-2-carbonyl]amino]benzoic acid	2207393: Displacement of [3H]PSB-12150 from human GPR17 expressed in Flp-In T-REx system generated CHO cell membrane incubated for 1 hrs by liquid scintillation counter analysis	ki	0.1380	uM
2-[[5-[2-(3-cyanophenyl)phenyl]furan-2-carbonyl]amino]-5-methoxybenzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1585	uM
2-[[5-(2-bromophenyl)furan-2-carbonyl]amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1585	uM
5-cyclopropyl-2-[(5-naphthalen-1-ylfuran-2-carbonyl)amino]benzoic acid	2207385: Antagonist activity at wildtype human GPR17 expressed in human 1321N1 cells co-expressing pLVX-IRES assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition and measured immediately by plate reader analysis	ic50	0.1622	uM
4-methoxy-2-[(5-naphthalen-1-ylfuran-2-carbonyl)amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1995	uM
4,5-difluoro-2-[(6-naphthalen-1-ylpyridine-2-carbonyl)amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1995	uM
5-chloro-2-[(6-naphthalen-1-ylpyridine-2-carbonyl)amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1995	uM
5-methoxy-2-[(5-naphthalen-1-ylfuran-2-carbonyl)amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1995	uM
5-methoxy-2-[[5-(2-phenoxyphenyl)furan-2-carbonyl]amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1995	uM
5-fluoro-2-[(2-naphthalen-1-yl-1,3-thiazole-4-carbonyl)amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1995	uM
2-[[5-[2-(3-cyclopropyloxyphenyl)phenyl]furan-2-carbonyl]amino]-5-methoxybenzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.1995	uM
2-[[5-(2-methoxynaphthalen-1-yl)furan-2-carbonyl]amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.2512	uM
2-[[5-[2-(2-phenylethoxy)phenyl]furan-2-carbonyl]amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.2512	uM
4,5-difluoro-2-[(5-naphthalen-1-ylfuran-2-carbonyl)amino]benzoic acid	2207381: Antagonist activity at human GPR17 expressed in Flp-In T-REx system generated CHO cells assessed as inhibition of MDL29,951-induced calcium mobilization preincubated for 30 mins followed by MDL29,951 addition by calcium 5 dye based FLIPR assay	ic50	0.2512	uM
N-[5-(difluoromethoxy)-4,6-dimethoxypyrimidin-2-yl]-5-(1,3-thiazol-2-yl)-1H-pyrrole-3-sulfonamide	2236111: Antagonist activity at untagged human GPR17S stably expressed in CHO-K1 cells assessed as inhibition of MDL29,951/IBMX-induced cAMP reduction preincubated for 5 mins followed by forskolin addition and measured after 30 mins by TR-FRET assay	ic50	0.2560	uM

CTD chemical–gene interactions

16 total (human), top 16 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
ochratoxin A	increases expression	2
Resveratrol	increases expression, decreases expression, affects cotreatment	2
Esketamine	increases expression	1
bisphenol A	affects cotreatment, increases methylation	1
CGP 52608	affects binding, increases reaction	1
enniatins	increases expression	1
Arsenic Trioxide	decreases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Acetaminophen	increases expression	1
Benzo(a)pyrene	increases methylation	1
Copper	affects cotreatment, increases expression	1
Diazinon	decreases expression	1
Estradiol	decreases expression, affects cotreatment	1
Plant Extracts	affects cotreatment, decreases expression	1
Progesterone	affects cotreatment, decreases expression	1
Triclosan	decreases expression	1

ChEMBL screening assays

78 unique, capped per target: 57 functional, 21 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1107397	Functional	Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay	Frontal affinity chromatography-mass spectrometry useful for characterization of new ligands for GPR17 receptor. — *J Med Chem*
CHEMBL3269448	Binding	Binding affinity to human GPR17 expressed in CHO-K1 cell membranes assessed per mg protein after 60 mins by saturation curve study	Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17. — *ACS Med Chem Lett*

Cellosaurus cell lines

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

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

Cellosaurus	Name	Category	Sex
CVCL_KU60	CHO-K1 GPR17 Gq	Spontaneously immortalized cell line	Female
CVCL_LA41	PathHunter U2OS GPR17 beta-arrestin	Cancer cell line	Female

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

showing 60 of 76 trials:

NCT	Phase	Status	Title
NCT00417066	Phase 4	COMPLETED	Flexible GnRH Antagonist vs Flare up GnRH Agonist Protocol in Poor Responders
NCT00732693	Phase 4	COMPLETED	Evaluation of Physiologic and Standard Sex Steroid Replacement Regimens in Women With Premature Ovarian Failure
NCT00837616	Phase 4	COMPLETED	Estrogen Dosing in Turner Syndrome: Pharmacology and Metabolism
NCT01853501	Phase 4	UNKNOWN	Effects of ADSC Therapy in Women With POF
NCT02783937	Phase 4	COMPLETED	Filgrastim for Premature Ovarian Insufficiency
NCT03535480	Phase 4	UNKNOWN	Autologous Bone Marrow Stem Cell Ovarian Transplantation to Restore Ovarian Function in Premature Ovarian Failure
NCT00140998	Phase 3	COMPLETED	Estrogen Treatment (Oral vs. Patches) in Turner Syndrome
NCT00001951	Phase 2	COMPLETED	Hormone Replacement in Young Women With Premature Ovarian Failure
NCT00370019	Phase 2	WITHDRAWN	Effects of an Estrogen Replacement Therapy Skin Patch on Ovulation in Women With Premature Ovarian Failure
NCT00429494	Phase 2	COMPLETED	GnRH Analogue for Ovarian Function Preservation in Hematopoietic Stem Cell Transplantation Patients
NCT03816852	Phase 2	SUSPENDED	The Safety and Efficiency Study of Mesenchymal Stem Cell (19#iSCLife®-POI) in Premature Ovarian Insufficiency
NCT04536467	Phase 2	UNKNOWN	Prevention of Chemotherapy-Induced Ovarian Failure With Goserelin in Premenopausal Lymphoma Patients
NCT06117982	Phase 2	COMPLETED	The Impact of Granulocyte Colony Stimulating Factor on Premature Ovarian Insufficiency
NCT02912104	Phase 1	COMPLETED	A Therapeutic Trial of Human Amniotic Epithelial Cells Transplantation for Primary Ovarian Failure
NCT03178695	Phase 1	COMPLETED	Inovium Ovarian Rejuvenation Trials
NCT04815213	Phase 1	ACTIVE_NOT_RECRUITING	The Use of Expandeded Mesenchymal Stromal Cells (MSC) in Premature Ovarian Failure (POF) in Adult Humans
NCT05138367	Phase 1	COMPLETED	Effects of UCA-PSCs in Women With POF
NCT06132542	Phase 1	UNKNOWN	Autologous ADMSC Transplantation in Patients With POI
NCT05989620	Not specified	RECRUITING	Long-Term Development of Muscular Dystrophy Outcome Assessments
NCT00948857	Phase 2/3	TERMINATED	Dehydroepiandrosterone (DHEA) Treatment and Premature Ovarian Failure (POF)
NCT04031456	Phase 2/3	RECRUITING	Autologous PRP Infusion May Restore Ovarian Function and May Promote Folliculogenesis in POI Patients
NCT02043743	Phase 1/2	UNKNOWN	Autologous Stem Cells Transplantation in Patients With Idiopathic and Drug Induced Premature Ovarian Failure
NCT02062931	Phase 1/2	UNKNOWN	Autologous Mesenchymal Stem Cells Transplantation In Women With Premature Ovarian Failure
NCT02151890	Phase 1/2	COMPLETED	Pregnancy After Stem Cell Transplantation in Premature Ovarian Failure
NCT02372474	Phase 1/2	COMPLETED	It is a Real The First Baby Of Autologous Stem Cell Therapy in Premature Ovarian Failure
NCT02603744	Phase 1/2	UNKNOWN	Autologous Adipose Derived Mesenchymal Stromal Cells Transplantation in Women With Premature Ovarian Failure (POF)
NCT02644447	Phase 1/2	COMPLETED	Transplantation of HUC-MSCs With Injectable Collagen Scaffold for POF
NCT03069209	Phase 1/2	UNKNOWN	Autologous Bone Marrow-Derived Stem Cell Transplantation in Patients With Premature Ovarian Failure (POF)
NCT03985462	Phase 1/2	WITHDRAWN	Very Small Embryonic-like Stem Cells for Ovary
NCT04009473	Phase 1/2	UNKNOWN	Stem Cell Therapy and Growth Factor Ovarian in Vitro Activation
NCT04071574	Phase 1/2	COMPLETED	Comparative Study on the Efficacy of Ovarian Stimulation Protocols on the Success Rate of ICSI in Female Infertility
NCT04922398	Phase 1/2	UNKNOWN	Ovarian Injection of PRP (Platelet -Rich Plasma) Vs Normal Saline in Premature Ovarian Insufficiency
NCT05462379	Phase 1/2	ACTIVE_NOT_RECRUITING	Autologous Heterotopic Fresh Ovarian Graft in Woman With LACC Eligible for Pelvic Radiotherapy Treatment.
NCT06202547	Phase 1/2	COMPLETED	Intra-ovarian Injection of MSC-EVs in Idiopathic Premature Ovarian Failure
NCT01129947	Early Phase 1	WITHDRAWN	The Use of DHEA in Women With Premature Ovarian Failure
NCT05522634	Early Phase 1	UNKNOWN	A Clinical Study of Chinese Herbal Compound TJAOA101 in the Treatment of Premature Ovarian Insufficiency
NCT07308327	Early Phase 1	ACTIVE_NOT_RECRUITING	The Influence of Gut Microbiota on Ovarian Function: A Single-center, Randomized,Double Blind, Parallel-controlled, Exploratory Clinical Trial
NCT00001275	Not specified	COMPLETED	Ovarian Follicle Function in Patients With Primary Ovarian Failure
NCT00001306	Not specified	COMPLETED	Steroid Therapy in Autoimmune Premature Ovarian Failure
NCT00006156	Not specified	COMPLETED	Feasibility Study for Development of an Early Test for Ovarian Failure
NCT00119925	Not specified	UNKNOWN	‘SPRING’-Study: Subfertility Guidelines: Patient Related Implementation in the Netherlands Among Gynaecologists
NCT00295087	Not specified	COMPLETED	X-Chromosome Inactivation Status and Premature Ovarian Failure
NCT00417157	Not specified	COMPLETED	Modified Natural Cycle Offers a Chance of Pregnancy in Patients With Poor Response and High Basal FSH
NCT00619333	Not specified	UNKNOWN	Inactive FSH in Galactosemia
NCT00780897	Not specified	UNKNOWN	Premature Ovarian Failure (Genetic and Physiopathologic Analysis)
NCT01187524	Not specified	TERMINATED	The Natural History of Reproductive and Overall Health in Girls and Women With a Pre-Mutation in the FMR1 Gene; Creation of a Patient Registry
NCT01411644	Not specified	UNKNOWN	Pheno- & Genotyping POF (WHO III)
NCT02086318	Not specified	UNKNOWN	A New Algorithm to Predict Ovarian Age
NCT02467231	Not specified	ACTIVE_NOT_RECRUITING	Ovarian Reserve After Cancer: Longitudinal Effects
NCT02696889	Not specified	COMPLETED	Rejuvenation of Premature Ovarian Failure With Stem Cells
NCT02779374	Not specified	TERMINATED	Autologous Bone Marrow Transplantation for Premature Ovarian Insufficiency
NCT03207412	Not specified	UNKNOWN	Human Amniotic Epithelial Cells Treatment for Ovarian Insufficiency
NCT03381300	Not specified	ACTIVE_NOT_RECRUITING	Preservation of Ovarian Cortex Tissue in Girls With Turner Syndrome
NCT03412487	Not specified	UNKNOWN	Ovarian Histopathology and Laparoscopic Assessment of Premature Ovarian Failure
NCT03474120	Not specified	UNKNOWN	Prospective Genetic Study in Patients With Ovarian Insufficiency
NCT03480412	Not specified	UNKNOWN	Second Step Protocol in Poor Ovarian Responder (POR)
NCT03840824	Not specified	COMPLETED	Blood Spot Self-administered Test and Assay
NCT03861715	Not specified	UNKNOWN	Single Follicular Dexarelix for LH Suppression During Ovarian Stimulation in Oocyte Donors.
NCT03924648	Not specified	COMPLETED	Endocan Levels in Women With Premature Ovarian Insufficiency
NCT04149028	Not specified	COMPLETED	Platelet Rich Plasma Injection Into Ovary of Patients With Premature Ovarian Insufficiency

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for GPR17 across ~30M SureChEMBL compounds — explore on Sugi Predict.