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 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 70 total
• Druggable target: yes — 5 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001161417

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: 7 — 6 protein_coding, 1 protein_coding_CDS_not_defined

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

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.

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

293 total, 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

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

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

71 targeting GPR17, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

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

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

3 orthologs

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

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)

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): Q13304, C9JWY5, 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 (38 total): helix 12, 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.

PDB	Method	Resolution (Å)
7Y89	ELECTRON MICROSCOPY	3.02

Predicted structure (AlphaFold)

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

Antibody-complex structures (SAbDab): 1 — 7Y89

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): 132–209

Glycosylation sites (3): 42, 204, 282

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-391906	Leukotriene receptors
R-HSA-416476	G alpha (q) signalling events
R-HSA-417957	P2Y receptors
R-HSA-418594	G alpha (i) signalling events

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 (5): negative regulation of inflammatory response to antigenic stimulus (GO:0002862), 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

Rollup of top-3 pathways:

Category	Pathways
GPCR downstream signalling	2
Eicosanoid ligand-binding receptors	1
Nucleotide-like (purinergic) receptors	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	2
inflammatory response to antigenic stimulus	1
regulation of inflammatory response to antigenic stimulus	1
negative regulation of inflammatory response	1
negative regulation of immune response	1
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

868 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GPR17	ITGA4	P13612	701
GPR17	GPR176	Q14439	619
GPR17	LTC4S	Q16873	576
GPR17	P0DN79	P0DN79	571
GPR17	OLIG2	Q13516	555
GPR17	OLIG1	Q8TAK6	555
GPR17	ITGAL	P20701	545
GPR17	P2RY12	Q9H244	511
GPR17	SOX10	P56693	493
GPR17	MYRF	Q9Y2G1	491
GPR17	OXGR1	Q96P68	487
GPR17	SELL	P14151	475
GPR17	CNP	P09543	474
GPR17	BCAS1	O75363	465
GPR17	GPR37	O15354	456

IntAct

6 interactions, top by confidence:

A	B	Type	Score
GPR17	IPO8	psi-mi:“MI:0914”(association)	0.530
PDZK1	GPR17	psi-mi:“MI:0407”(direct interaction)	0.440
GPR17	GPR37	psi-mi:“MI:0915”(physical association)	0.370
GPR17	TMEM120B	psi-mi:“MI:0914”(association)	0.350
GPR17	C1QTNF9B	psi-mi:“MI:0914”(association)	0.350

BioGRID (280): ADRBK1 (Affinity Capture-Luminescence), GPR17 (Two-hybrid), FAM126A (Affinity Capture-MS), MUL1 (Affinity Capture-MS), ATP2A2 (Affinity Capture-MS), MFSD5 (Affinity Capture-MS), HOOK2 (Affinity Capture-MS), ATP12A (Affinity Capture-MS), ATM (Affinity Capture-MS), C19orf25 (Affinity Capture-MS), SLC38A9 (Affinity Capture-MS), XYLT2 (Affinity Capture-MS), CCDC132 (Affinity Capture-MS), TONSL (Affinity Capture-MS), USO1 (Affinity Capture-MS)

ESM2 similar proteins: A7YY44, B0UXR0, B5X337, E7FEL0, O00254, O08675, O14843, O15529, O15552, O46685, P25116, P26824, P30558, P34996, P46093, P47749, P47900, P48042, P49650, P49651, P49652, P50132, P55085, P55086, P56488, P59902, Q00991, Q09QM4, Q13304, Q15743, Q1JQB3, Q2HJA4, Q3UFD7, Q4KLH9, Q58D85, Q63645, Q76EI6, Q86VZ1, Q8BFQ3, Q8BLG2

Diamond homologs: A0A4W3GG95, A0A6I8PUB9, B2GV46, B5X337, D4A7K7, E7FEL0, E9QJ73, F8VQN3, O00270, O08726, O08858, O14842, O14843, O15529, O42179, O43603, O46685, O60755, O77408, O88410, O88626, O88634, O88853, P21109, P23944, P25024, P25025, P35344, P35383, P35414, P41231, P41232, P46092, P46093, P49652, P49682, P49683, P50132, P51675, P51679

SIGNOR signaling

6 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

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	56
Likely benign	8
Benign	3

Top pathogenic / likely-pathogenic (0)

SpliceAI

1101 predictions. Top by Δscore:

Variant	Effect	Δscore
2:127654418:CCTCA:C	donor_loss	1.0000
2:127654419:CTCA:C	donor_loss	1.0000
2:127654420:TCACC:T	donor_loss	1.0000
2:127654421:CA:C	donor_loss	1.0000
2:127654540:CTCAC:C	acceptor_gain	1.0000
2:127654541:TCAC:T	acceptor_gain	1.0000
2:127654542:CAC:C	acceptor_gain	1.0000
2:127654542:CACC:C	acceptor_gain	1.0000
2:127654543:AC:A	acceptor_gain	1.0000
2:127654543:ACCTG:A	acceptor_loss	1.0000
2:127654544:CC:C	acceptor_gain	1.0000
2:127654897:C:CC	acceptor_gain	1.0000
2:127654909:C:CT	acceptor_gain	1.0000
2:127646241:AGAGG:A	donor_loss	0.9900
2:127646243:AGGTA:A	donor_loss	0.9900
2:127646244:GGTAA:G	donor_loss	0.9900
2:127646245:GTAAG:G	donor_loss	0.9900
2:127646246:T:G	donor_loss	0.9900
2:127650711:TCCA:T	acceptor_loss	0.9900
2:127650712:CCA:C	acceptor_loss	0.9900
2:127650713:CAG:C	acceptor_loss	0.9900
2:127650714:A:AG	acceptor_gain	0.9900
2:127650715:G:C	acceptor_loss	0.9900
2:127650715:G:GG	acceptor_gain	0.9900
2:127654791:T:TA	donor_gain	0.9900
2:127654792:C:A	donor_gain	0.9900
2:127654814:CTG:C	donor_gain	0.9900
2:127654815:TGT:T	donor_gain	0.9900
2:127654824:CCTTA:C	donor_loss	0.9900
2:127654825:CTTAC:C	donor_loss	0.9900

AlphaMissense

2190 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
2:127651026:G:C	W125C	0.997
2:127651026:G:T	W125C	0.997
2:127651111:A:C	S154R	0.997
2:127651113:C:A	S154R	0.997
2:127651113:C:G	S154R	0.997
2:127651201:T:A	W184R	0.995
2:127651201:T:C	W184R	0.995
2:127651276:T:A	C209S	0.995
2:127651277:G:C	C209S	0.995
2:127651046:G:A	C132Y	0.994
2:127651087:A:C	S146R	0.994
2:127651089:C:A	S146R	0.994
2:127651089:C:G	S146R	0.994
2:127651276:T:C	C209R	0.994
2:127651477:T:C	F276L	0.994
2:127651479:C:A	F276L	0.994
2:127651479:C:G	F276L	0.994
2:127651045:T:A	C132S	0.993
2:127651046:G:C	C132S	0.993
2:127651336:T:C	F229L	0.993
2:127651338:C:A	F229L	0.993
2:127651338:C:G	F229L	0.993
2:127651484:C:A	P278H	0.993
2:127651484:C:G	P278R	0.993
2:127651047:C:G	C132W	0.992
2:127651277:G:A	C209Y	0.992
2:127651278:C:G	C209W	0.992
2:127651346:C:G	P232R	0.992
2:127651045:T:C	C132R	0.990
2:127651121:G:C	R157P	0.990

dbSNP variants (sampled 300 via entrez): RS1000023950 (2:127652732 T>C), RS1000035540 (2:127647396 G>A,C), RS1000118169 (2:127652975 G>A), RS1000435329 (2:127644179 G>A), RS1000636411 (2:127646212 C>T), RS1000856810 (2:127647242 G>A), RS1001122135 (2:127651791 T>C), RS1001419979 (2:127649238 T>C), RS1001494475 (2:127649141 A>C), RS1001626774 (2:127644259 G>A), RS1002426061 (2:127648049 G>A,C), RS1002467748 (2:127645794 G>C), RS1002894079 (2:127645424 C>T), RS1002909780 (2:127647828 C>T), RS1003091814 (2:127650290 G>A)

Disease associations

OMIM: gene MIM:603071 | disease phenotypes: MIM:616827

GenCC curated gene-disease

Mondo (2): autosomal recessive limb-girdle muscular dystrophy type 2W (MONDO:0014788), primary ovarian failure (MONDO:0005387)

Orphanet (2): OBSOLETE: LIMS2-related myopathy (Orphanet:466801), NON RARE IN EUROPE: Primary ovarian failure (Orphanet:619)

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST010916_8	Proportion of activated microglia (inferior temporal cortex)	3.000000e-06

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D016649	Primary Ovarian Insufficiency	C12.050.351.500.056.630.750; C12.100.250.056.630.750; C19.391.630.750

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1075162 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

5 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 196,643 (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
CHEMBL1097279	CANGRELOR TETRASODIUM	4	108
CHEMBL21333	PRANLUKAST	4	12,755
CHEMBL6	INDOMETHACIN	4	156,366
CHEMBL787	MONTELUKAST	4	26,700
CHEMBL44793	GAVESTINEL	2	714

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

GtoPdb / IUPHAR curated pharmacology

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

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

Most potent curated ligand interactions (14 total), top 14:

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
cangrelor	Antagonist	8.92	pIC50
UDP-galactose	Agonist	8.92	pEC50
UDP	Agonist	8.8	pEC50
ASN04421891	Agonist	8.44	pEC50
LTD4	Agonist	8.36	pEC50
ATP	Agonist	7.43	pEC50
montelukast	Antagonist	7.21	pIC50

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

62 with measured affinity, of 256 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
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
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-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
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
3-(2-carboxyethyl)-6-phenoxy-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	0.2700	uM
3-(2-carboxyethyl)-4-chloro-6-(4-fluorophenyl)-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	0.4230	uM
azane;[(2R,3S,5R)-5-[6-(methylamino)purin-9-yl]-2-(phosphonooxymethyl)oxolan-3-yl] dihydrogen 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	0.5080	uM
[(2R,3S,5R)-5-(6-amino-2-chloropurin-9-yl)-2-(phosphonooxymethyl)oxolan-3-yl] dihydrogen phosphate;azane	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	0.5820	uM
4-bromo-3-(2-carboxyethyl)-6-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	0.6240	uM
3-(2-carboxyethyl)-6-phenyl-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	0.7310	uM
azane;[(2R,3S,4R,5R)-3,4-dihydroxy-5-(5-iodo-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methyl 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	0.9450	uM
trisodium;[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl] 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	1.1400	uM
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid	1137664: Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by homologous competition binding assay in presence of pranlukast	ki	1.2100	uM
3-(2-carboxy-1,1,2,2-tetratritioethyl)-4,6-dichloro-1H-indole-2-carboxylic acid	1137659: Binding affinity to human GPR17 expressed in CHO-K1 cell membranes after 60 mins by saturation curve study	kd	1.2560	uM
(3-nitrophenyl) 4-[(4-methylbenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	1.3300	uM
3-(2-carboxyethyl)-6-fluoro-4-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	1.4700	uM
(3-cyanophenyl) 4-[(3-methylbenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	1.6000	uM
3-[(E)-3-anilino-3-oxoprop-1-enyl]-4,6-dichloro-1H-indole-2-carboxylic acid	1137667: Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay	ki	1.6300	uM
(3-nitrophenyl) 4-[(3-methoxybenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	1.6500	uM
(3-nitrophenyl) 4-[(2-chlorobenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	1.6700	uM
3-(4,6-dichloro-1H-indol-3-yl)propanoic 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	1.6800	uM
(3-nitrophenyl) 4-[(3-methylbenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	1.9200	uM
(3-nitrophenyl) 3-[(3-chlorobenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	2.3200	uM
(3-nitrophenyl) 4-[(3-chlorobenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	3.0000	uM
3-(2-carboxyethyl)-7-fluoro-6-phenyl-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	3.0100	uM
(3-nitrophenyl) 3-[(4-chlorobenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	3.0600	uM
(3-nitrophenyl) 4-benzamidobenzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	3.2000	uM
(3-nitrophenyl) 4-[(3,4-dichlorobenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	3.3300	uM
(3-nitrophenyl) 4-[(4-chlorobenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	3.3700	uM
(3-nitrophenyl) 3-[(3-fluorobenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	3.6100	uM
3-(2-carboxyethyl)-6-chloro-4-(4-fluorophenyl)-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	3.6800	uM
3-(2-carboxyethyl)-6-chloro-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	3.7200	uM
(3-nitrophenyl) 4-[[3-(trifluoromethyl)benzoyl]amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	3.8800	uM
3-(2-carboxyethyl)-6-(4-fluorophenyl)-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	4.0200	uM
N-[4-oxo-2-(2H-tetrazol-5-yl)chromen-8-yl]-4-(4-phenylbutoxy)benzamide	1137667: Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay	ki	4.0600	uM
methyl 3-[[3-[(3-methylbenzoyl)amino]phenyl]carbamoylamino]benzoate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	4.0700	uM
3-(2-carboxyethyl)-4,6-diphenyl-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	4.0900	uM
3-(2-carboxyethyl)-6-(furan-2-yl)-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	4.1300	uM
(3-nitrophenyl) 4-[(3-bromobenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	4.1800	uM
(3-nitrophenyl) 4-[(3-fluorobenzoyl)amino]benzenesulfonate	1716958: Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay	ic50	4.6200	uM
6-bromo-3-(2-carboxyethyl)-7-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	4.8300	uM
6-benzyl-3-(2-carboxyethyl)-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	4.9800	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	affects cotreatment, increases expression, decreases expression	2
Esketamine	increases expression	1
bisphenol A	affects cotreatment, increases methylation	1
CGP 52608	increases reaction, affects binding	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	affects cotreatment, decreases expression	1
Plant Extracts	decreases expression, affects cotreatment	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)

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

Trial	Phase	Status	Title
NCT00417066	PHASE4	COMPLETED	Flexible GnRH Antagonist vs Flare up GnRH Agonist Protocol in Poor Responders
NCT00732693	PHASE4	COMPLETED	Evaluation of Physiologic and Standard Sex Steroid Replacement Regimens in Women With Premature Ovarian Failure
NCT00837616	PHASE4	COMPLETED	Estrogen Dosing in Turner Syndrome: Pharmacology and Metabolism
NCT01853501	PHASE4	UNKNOWN	Effects of ADSC Therapy in Women With POF
NCT02783937	PHASE4	COMPLETED	Filgrastim for Premature Ovarian Insufficiency
NCT03535480	PHASE4	UNKNOWN	Autologous Bone Marrow Stem Cell Ovarian Transplantation to Restore Ovarian Function in Premature Ovarian Failure
NCT00140998	PHASE3	COMPLETED	Estrogen Treatment (Oral vs. Patches) in Turner Syndrome
NCT00001951	PHASE2	COMPLETED	Hormone Replacement in Young Women With Premature Ovarian Failure
NCT00370019	PHASE2	WITHDRAWN	Effects of an Estrogen Replacement Therapy Skin Patch on Ovulation in Women With Premature Ovarian Failure
NCT00429494	PHASE2	COMPLETED	GnRH Analogue for Ovarian Function Preservation in Hematopoietic Stem Cell Transplantation Patients
NCT03816852	PHASE2	SUSPENDED	The Safety and Efficiency Study of Mesenchymal Stem Cell (19#iSCLife®-POI) in Premature Ovarian Insufficiency
NCT04536467	PHASE2	UNKNOWN	Prevention of Chemotherapy-Induced Ovarian Failure With Goserelin in Premenopausal Lymphoma Patients
NCT06117982	PHASE2	COMPLETED	The Impact of Granulocyte Colony Stimulating Factor on Premature Ovarian Insufficiency
NCT02912104	PHASE1	COMPLETED	A Therapeutic Trial of Human Amniotic Epithelial Cells Transplantation for Primary Ovarian Failure
NCT03178695	PHASE1	COMPLETED	Inovium Ovarian Rejuvenation Trials
NCT04815213	PHASE1	ACTIVE_NOT_RECRUITING	The Use of Expandeded Mesenchymal Stromal Cells (MSC) in Premature Ovarian Failure (POF) in Adult Humans
NCT05138367	PHASE1	COMPLETED	Effects of UCA-PSCs in Women With POF
NCT06132542	PHASE1	UNKNOWN	Autologous ADMSC Transplantation in Patients With POI
NCT05989620	Not specified	RECRUITING	Long-Term Development of Muscular Dystrophy Outcome Assessments
NCT00948857	PHASE2/PHASE3	TERMINATED	Dehydroepiandrosterone (DHEA) Treatment and Premature Ovarian Failure (POF)
NCT04031456	PHASE2/PHASE3	RECRUITING	Autologous PRP Infusion May Restore Ovarian Function and May Promote Folliculogenesis in POI Patients
NCT02043743	PHASE1/PHASE2	UNKNOWN	Autologous Stem Cells Transplantation in Patients With Idiopathic and Drug Induced Premature Ovarian Failure
NCT02062931	PHASE1/PHASE2	UNKNOWN	Autologous Mesenchymal Stem Cells Transplantation In Women With Premature Ovarian Failure
NCT02151890	PHASE1/PHASE2	COMPLETED	Pregnancy After Stem Cell Transplantation in Premature Ovarian Failure
NCT02372474	PHASE1/PHASE2	COMPLETED	It is a Real The First Baby Of Autologous Stem Cell Therapy in Premature Ovarian Failure
NCT02603744	PHASE1/PHASE2	UNKNOWN	Autologous Adipose Derived Mesenchymal Stromal Cells Transplantation in Women With Premature Ovarian Failure (POF)
NCT02644447	PHASE1/PHASE2	COMPLETED	Transplantation of HUC-MSCs With Injectable Collagen Scaffold for POF
NCT03069209	PHASE1/PHASE2	UNKNOWN	Autologous Bone Marrow-Derived Stem Cell Transplantation in Patients With Premature Ovarian Failure (POF)
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NCT05462379	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Autologous Heterotopic Fresh Ovarian Graft in Woman With LACC Eligible for Pelvic Radiotherapy Treatment.
NCT06202547	PHASE1/PHASE2	UNKNOWN	Intra-ovarian Injection of MSC-EVs in Idiopathic Premature Ovarian Failure
NCT01129947	EARLY_PHASE1	WITHDRAWN	The Use of DHEA in Women With Premature Ovarian Failure
NCT05522634	EARLY_PHASE1	UNKNOWN	A Clinical Study of Chinese Herbal Compound TJAOA101 in the Treatment of Premature Ovarian Insufficiency
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NCT00001275	Not specified	COMPLETED	Ovarian Follicle Function in Patients With Primary Ovarian Failure
NCT00001306	Not specified	COMPLETED	Steroid Therapy in Autoimmune Premature Ovarian Failure
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