GPR174
geneOn this page
Also known as FKSG79LPS3
Summary
GPR174 (G protein-coupled receptor 174, HGNC:30245) is a protein-coding gene on chromosome Xq21.1, encoding Probable G-protein coupled receptor 174 (Q9BXC1). G-protein-coupled receptor of lysophosphatidylserine (LysoPS) that plays different roles in immune response.
This gene encodes a protein belonging to the G protein-coupled receptor superfamily. These proteins are characterized by the presence of seven alpha-helical transmembrane domains, and they activate or interact with various endogenous or exogenous ligands, including neurotransmitters, hormones, and odorant and taste substances. This family member is classified as an orphan receptor because the cognate ligand has not been identified.
Source: NCBI Gene 84636 — RefSeq curated summary.
At a glance
- GWAS associations: 1
- Clinical variants (ClinVar): 39 total
- Druggable target: yes
- MANE Select transcript:
NM_032553
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:30245 |
| Approved symbol | GPR174 |
| Name | G protein-coupled receptor 174 |
| Location | Xq21.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | FKSG79, LPS3 |
| Ensembl gene | ENSG00000147138 |
| Ensembl biotype | protein_coding |
| OMIM | 300903 |
| Entrez | 84636 |
Gene structure
Transcript identifiers
Ensembl transcripts: 2 — 2 protein_coding
ENST00000645147, ENST00000871945
RefSeq mRNA: 1 — MANE Select: NM_032553
NM_032553
CCDS: CCDS14443
Canonical transcript exons
ENST00000645147 — 3 exons
| Exon | Start | End |
|---|---|---|
| ENSE00003826852 | 79144688 | 79145217 |
| ENSE00003827115 | 79156822 | 79156918 |
| ENSE00003827781 | 79170452 | 79175318 |
Expression profiles
Bgee: expression breadth ubiquitous, 133 present calls, max score 88.24.
FANTOM5 (CAGE): breadth broad, TPM avg 10.4909 / max 563.0730, expressed in 286 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 196794 | 10.3964 | 286 |
| 196795 | 0.0945 | 54 |
Top tissues by expression
236 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| thymus | UBERON:0002370 | 88.24 | gold quality |
| ileal mucosa | UBERON:0000331 | 83.30 | gold quality |
| lymph node | UBERON:0000029 | 83.15 | gold quality |
| granulocyte | CL:0000094 | 82.07 | gold quality |
| vermiform appendix | UBERON:0001154 | 77.67 | gold quality |
| epithelium of nasopharynx | UBERON:0001951 | 75.85 | gold quality |
| colonic epithelium | UBERON:0000397 | 75.16 | gold quality |
| spleen | UBERON:0002106 | 73.98 | gold quality |
| superficial temporal artery | UBERON:0001614 | 71.70 | silver quality |
| blood | UBERON:0000178 | 71.39 | gold quality |
| caecum | UBERON:0001153 | 70.67 | gold quality |
| bone marrow cell | CL:0002092 | 70.10 | silver quality |
| tonsil | UBERON:0002372 | 69.74 | gold quality |
| jejunal mucosa | UBERON:0000399 | 68.92 | gold quality |
| bone marrow | UBERON:0002371 | 68.45 | gold quality |
| leukocyte | CL:0000738 | 67.09 | gold quality |
| rectum | UBERON:0001052 | 66.11 | gold quality |
| monocyte | CL:0000576 | 65.36 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 64.76 | gold quality |
| tibialis anterior | UBERON:0001385 | 64.05 | silver quality |
| small intestine Peyer’s patch | UBERON:0003454 | 63.19 | gold quality |
| duodenum | UBERON:0002114 | 63.13 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 63.04 | gold quality |
| gall bladder | UBERON:0002110 | 62.99 | gold quality |
| small intestine | UBERON:0002108 | 62.71 | gold quality |
| pancreatic ductal cell | CL:0002079 | 61.87 | silver quality |
| mucosa of transverse colon | UBERON:0004991 | 61.16 | gold quality |
| palpebral conjunctiva | UBERON:0001812 | 61.07 | gold quality |
| colonic mucosa | UBERON:0000317 | 60.66 | gold quality |
| jejunum | UBERON:0002115 | 59.01 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 5.06 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
21 targeting GPR174, 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-3185 | 99.99 | 68.12 | 1959 |
| HSA-MIR-450B-5P | 99.92 | 71.48 | 3175 |
| HSA-MIR-320A-3P | 99.77 | 69.73 | 2107 |
| HSA-MIR-320B | 99.77 | 69.73 | 2107 |
| HSA-MIR-320C | 99.77 | 69.73 | 2107 |
| HSA-MIR-320D | 99.77 | 69.73 | 2107 |
| HSA-MIR-4429 | 99.77 | 69.62 | 2111 |
| HSA-MIR-4802-3P | 99.72 | 70.13 | 1273 |
| HSA-MIR-4519 | 99.48 | 66.10 | 859 |
| HSA-MIR-19A-5P | 99.36 | 66.93 | 1675 |
| HSA-MIR-19B-1-5P | 99.36 | 67.07 | 1669 |
| HSA-MIR-19B-2-5P | 99.36 | 67.07 | 1669 |
| HSA-MIR-505-3P | 99.19 | 69.71 | 896 |
| HSA-MIR-11399 | 98.71 | 65.69 | 869 |
| HSA-MIR-4274 | 98.59 | 66.10 | 630 |
| HSA-MIR-4468 | 98.01 | 66.85 | 1187 |
| HSA-MIR-146B-3P | 97.83 | 65.29 | 782 |
| HSA-MIR-6893-3P | 97.79 | 64.91 | 1238 |
| HSA-MIR-2278 | 97.30 | 66.19 | 1130 |
| HSA-MIR-370-3P | 97.09 | 64.92 | 1221 |
| HSA-MIR-503-3P | 92.89 | 66.09 | 537 |
Literature-anchored findings (GeneRIF, showing 10)
- These results suggested that GPR174 was a putative LysoPS receptor conjugating with Galpha(s), and its expression induced morphological changes in CHO cells by constitutively activating adenylyl cycles accompanied with cell conjunctions and delay of proliferation. (PMID:23178570)
- The finding of an X-linked risk locus for Graves’ disease expands our understanding of the role of the X chromosome in disease susceptibility. (PMID:23667180)
- this study provides the first replication in a Caucasian population of the association between Graves’ disease and the GPR174 rs3827440 single nucleotide polymorphism originally reported among Chinese. (PMID:24289805)
- We have demonstrated a significant association of this X chromosome-encoded immunoreceptor with autoimmune Addison’s disease for the first time. (PMID:25295623)
- Alteration of gene expression profiling including GPR174 and GNG2 is associated with vasovagal syncope. (PMID:25367286)
- Studied association of and RNASET2, GPR174, and PTPN22 gene polymorphisms and liver damage(LD) due to Graves’ disease (GD) hyperthyroidism. Found GPR174 rs3827440, PTPN22 rs3789604, and RNASET2 rs9355610 were significantly associated with altered GD-derived LD risk. (PMID:28568286)
- GPR174 and ITM2A Gene Polymorphisms rs3827440 and rs5912838 on the X chromosome in Korean Children with Autoimmune Thyroid Disease. (PMID:32727090)
- GPR174 mRNA Acts as a Novel Prognostic Biomarker for Patients With Sepsis via Regulating the Inflammatory Response. (PMID:35173706)
- Gpr174 Knockout Alleviates DSS-Induced Colitis via Regulating the Immune Function of Dendritic Cells. (PMID:35669778)
- Structural basis for ligand recognition and signaling of the lysophosphatidylserine receptors GPR34 and GPR174. (PMID:38048360)
Cross-species orthologs
2 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Gpr174 | ENSMUSG00000073008 |
| rattus_norvegicus | Gpr174 | ENSRNOG00000032970 |
Paralogs (7): GPR146 (ENSG00000164849), GPR183 (ENSG00000169508), GPR151 (ENSG00000173250), RXFP3 (ENSG00000182631), GPR132 (ENSG00000183484), GPR141 (ENSG00000187037), P2RY11 (ENSG00000244165)
Protein
Protein identifiers
Probable G-protein coupled receptor 174 — Q9BXC1 (reviewed: Q9BXC1)
All UniProt accessions (1): Q9BXC1
UniProt curated annotations — full annotation on UniProt →
Function. G-protein-coupled receptor of lysophosphatidylserine (LysoPS) that plays different roles in immune response. Plays a negative role in regulatory T-cell accumulation and homeostasis. Under inflammatory conditions where LysoPS production increases, contributes to the down-regulation of regulatory T-cell activity to favor effector response. Mediates the suppression of IL-2 production in activated T-lymphocytes leading to inhibition of growth, proliferation and differentiation of T-cells. Mechanistically, acts via G(s)-containing heterotrimeric G proteins to trigger elevated cyclic AMP levels and protein kinase A/PKA activity, which may in turn act to antagonize proximal TCR signaling. Plays an important role in the initial period of sepsis through the regulation of macrophage polarization and pro- and anti-inflammatory cytokine secretions. Upon testosterone treatment, acts as a receptor for CCL21 and subsequently triggers through G(q)-alpha and G(12)/G(13) proteins a calcium flux leading to chemotactic effects on activated B-cells. Signals via GNA13 and PKA to promote CD86 up-regulation by follicular B-cells.
Subunit / interactions. Interacts with GNA13. Interacts with CCL21.
Subcellular location. Cell membrane.
Similarity. Belongs to the G-protein coupled receptor 1 family.
RefSeq proteins (1): NP_115942* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000276 | GPCR_Rhodpsn | Family |
| IPR017452 | GPCR_Rhodpsn_7TM | Domain |
| IPR047836 | GPR174_7tmA | Domain |
Pfam: PF00001
UniProt features (41 total): helix 12, topological domain 8, transmembrane region 7, mutagenesis site 4, strand 4, glycosylation site 2, chain 1, disulfide bond 1, sequence variant 1, turn 1
Structure
Experimental structures (PDB)
5 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 9XXT | ELECTRON MICROSCOPY | 2 |
| 7XV3 | ELECTRON MICROSCOPY | 2.76 |
| 8KH5 | ELECTRON MICROSCOPY | 2.83 |
| 8IZB | ELECTRON MICROSCOPY | 3.06 |
| 20YC | ELECTRON MICROSCOPY | 3.4 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9BXC1-F1 | 84.18 | 0.53 |
Antibody-complex structures (SAbDab): 3 — 7XV3, 8IZB, 8KH5
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): 91–168
Glycosylation sites (2): 4, 164
Mutagenesis-validated functional residues (4):
| Position | Phenotype |
|---|---|
| 22 | substantially reduced receptor activity. |
| 75 | substantially reduced receptor activity. |
| 98 | substantially reduced receptor activity. |
| 156 | substantially reduced receptor activity. |
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 104 (showing top):
FREAC2_01, BENPORATH_ES_WITH_H3K27ME3, GOBP_T_CELL_HOMEOSTASIS, GOBP_LYMPHOCYTE_HOMEOSTASIS, FOXO1_01, CAGCTG_AP4_Q5, GOBP_NEGATIVE_REGULATION_OF_MULTICELLULAR_ORGANISMAL_PROCESS, GOBP_CYTOKINE_PRODUCTION, TGANTCA_AP1_C, GOBP_MULTICELLULAR_ORGANISMAL_LEVEL_HOMEOSTASIS, GOBP_NEGATIVE_REGULATION_OF_CYTOKINE_PRODUCTION, FOXO4_02, GOBP_LEUKOCYTE_HOMEOSTASIS, GOBP_NEGATIVE_REGULATION_OF_INTERLEUKIN_2_PRODUCTION, GOBP_HOMEOSTATIC_PROCESS
GO Biological Process (5): G protein-coupled receptor signaling pathway (GO:0007186), negative regulation of interleukin-2 production (GO:0032703), T cell homeostasis (GO:0043029), signal transduction (GO:0007165), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189)
GO Molecular Function (2): G protein-coupled receptor activity (GO:0004930), bioactive lipid receptor activity (GO:0045125)
GO Cellular Component (3): plasma membrane (GO:0005886), centriolar satellite (GO:0034451), membrane (GO:0016020)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| G protein-coupled receptor activity | 2 |
| cellular anatomical structure | 2 |
| signal transduction | 1 |
| negative regulation of cytokine production | 1 |
| interleukin-2 production | 1 |
| regulation of interleukin-2 production | 1 |
| lymphocyte homeostasis | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | 1 |
| adenylate cyclase activator activity | 1 |
| transmembrane signaling receptor activity | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| membrane | 1 |
| cell periphery | 1 |
| centrosome | 1 |
Protein interactions and networks
STRING
754 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| GPR174 | PLA1A | Q53H76 | 511 |
| GPR174 | LPAR2 | Q9HBW0 | 463 |
| GPR174 | CCL21 | O00585 | 461 |
| GPR174 | ARHGAP15 | Q53QZ3 | 438 |
| GPR174 | ABHD12 | Q8N2K0 | 437 |
| GPR174 | POU2AF1 | Q16633 | 429 |
| GPR174 | CR2 | P20023 | 426 |
| GPR174 | BTLA | Q7Z6A9 | 423 |
| GPR174 | ITM2A | O43736 | 418 |
| GPR174 | ABHD16A | O95870 | 418 |
| GPR174 | CD69 | Q07108 | 415 |
| GPR174 | GPR22 | Q99680 | 411 |
| GPR174 | TMEM89 | A2RUT3 | 399 |
| GPR174 | CD22 | P20273 | 382 |
| GPR174 | ARMCX5 | Q6P1M9 | 372 |
IntAct
7 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| RAMP1 | GPR174 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP2 | GPR174 | psi-mi:“MI:0915”(physical association) | 0.400 |
| GPR174 | RAMP2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| GPR174 | RAMP3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP3 | GPR174 | psi-mi:“MI:0915”(physical association) | 0.400 |
| GPR174 | psi-mi:“MI:0915”(physical association) | 0.000 |
ESM2 similar proteins: A1A5S3, A5PLE7, B0UXR0, B5X337, F5HDK1, F5HF62, F8VQN3, O00421, O18982, O97663, P09703, P32249, P35351, P35374, P46002, P49685, P50052, P51676, P56412, P69332, P69333, Q01035, Q0II78, Q0VDU3, Q14330, Q1RMI1, Q28929, Q3T0E9, Q3U507, Q4R613, Q6IYF9, Q75ZH0, Q83207, Q89609, Q8BZR0, Q8IYL9, Q8K1Z6, Q95N03, Q96P67, Q98146
Diamond homologs: A5PLE7, B0UXR0, B5X337, D4A7K7, F1MV99, O08858, O35210, O35811, O77590, O88634, P11613, P21556, P25025, P25095, P25104, P25106, P26824, P29089, P29754, P29755, P30555, P30556, P30937, P30938, P31391, P32249, P32250, P32300, P33396, P33535, P34976, P35346, P35366, P35372, P35373, P35383, P41143, P41231, P41232, P42866
SIGNOR signaling
4 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| GPR174 | “up-regulates activity” | GNAS | binding |
| GPR174 | “up-regulates activity” | GNAL | binding |
| GPR174 | “up-regulates activity” | GNA13 | binding |
| “lysophosphatidylserine 14:0(1-)” | “up-regulates activity” | GPR174 | “chemical activation” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
39 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 28 |
| Likely benign | 6 |
| Benign | 5 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
311 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| X:79171648:A:G | donor_gain | 0.7100 |
| X:79171718:G:T | donor_gain | 0.6100 |
| X:79171714:CAGGG:C | donor_gain | 0.5900 |
| X:79171716:GGG:G | donor_gain | 0.5800 |
| X:79171717:GGG:G | donor_gain | 0.5800 |
| X:79171227:CTG:C | acceptor_gain | 0.5700 |
| X:79171712:TGCAG:T | donor_gain | 0.5700 |
| X:79171713:GCAGG:G | donor_gain | 0.5700 |
| X:79171852:GTCT:G | acceptor_gain | 0.5700 |
| X:79171574:C:T | donor_gain | 0.5600 |
| X:79171621:C:G | acceptor_gain | 0.5600 |
| X:79171851:A:AG | acceptor_gain | 0.5600 |
| X:79171852:G:GG | acceptor_gain | 0.5600 |
| X:79171228:TG:T | acceptor_gain | 0.5100 |
| X:79171753:GTTTT:G | acceptor_gain | 0.5100 |
| X:79171225:CACTG:C | acceptor_gain | 0.5000 |
| X:79171226:ACTGA:A | acceptor_gain | 0.5000 |
| X:79171229:G:GC | acceptor_gain | 0.5000 |
| X:79171620:ACCT:A | acceptor_gain | 0.5000 |
| X:79171752:A:AG | acceptor_gain | 0.5000 |
| X:79171753:G:GG | acceptor_gain | 0.5000 |
| X:79171896:AAT:A | acceptor_gain | 0.5000 |
| X:79171834:T:TA | acceptor_gain | 0.4900 |
| X:79171960:CCTTT:C | donor_gain | 0.4900 |
| X:79171686:A:T | donor_gain | 0.4800 |
| X:79171807:GAAGG:G | donor_gain | 0.4800 |
| X:79171851:AGTCT:A | acceptor_gain | 0.4800 |
| X:79171852:GTCTG:G | acceptor_gain | 0.4800 |
| X:79171961:CTTTG:C | donor_loss | 0.4800 |
| X:79171964:TGT:T | donor_loss | 0.4800 |
AlphaMissense
2198 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| X:79171259:G:C | W84C | 0.999 |
| X:79171259:G:T | W84C | 0.999 |
| X:79171431:T:A | W142R | 0.999 |
| X:79171431:T:C | W142R | 0.999 |
| X:79171201:A:C | D65A | 0.998 |
| X:79171202:C:A | D65E | 0.998 |
| X:79171202:C:G | D65E | 0.998 |
| X:79171734:T:C | F243L | 0.998 |
| X:79171736:T:A | F243L | 0.998 |
| X:79171736:T:G | F243L | 0.998 |
| X:79171104:G:C | G33R | 0.997 |
| X:79171105:G:A | G33D | 0.997 |
| X:79171118:T:A | N37K | 0.997 |
| X:79171118:T:G | N37K | 0.997 |
| X:79171200:G:C | D65H | 0.997 |
| X:79171201:A:G | D65G | 0.997 |
| X:79171201:A:T | D65V | 0.997 |
| X:79171257:T:A | W84R | 0.997 |
| X:79171257:T:C | W84R | 0.997 |
| X:79171344:A:C | S113R | 0.997 |
| X:79171346:T:A | S113R | 0.997 |
| X:79171346:T:G | S113R | 0.997 |
| X:79171752:A:C | S249R | 0.997 |
| X:79171754:T:A | S249R | 0.997 |
| X:79171754:T:G | S249R | 0.997 |
| X:79171851:A:C | S282R | 0.997 |
| X:79171853:T:A | S282R | 0.997 |
| X:79171853:T:G | S282R | 0.997 |
| X:79171320:A:C | S105R | 0.996 |
| X:79171322:C:A | S105R | 0.996 |
dbSNP variants (sampled 300 via entrez): RS1000143245 (X:79164442 T>A), RS1000597444 (X:79149167 A>T), RS1000603080 (X:79158015 T>C), RS1000924977 (X:79174269 T>G), RS1000942238 (X:79145413 G>A), RS1000949253 (X:79157732 G>A), RS1001267173 (X:79145526 G>C,T), RS1001275188 (X:79154245 G>A,T), RS1001539190 (X:79162363 G>A,C), RS1001546385 (X:79166107 T>C), RS1001592507 (X:79145823 G>A,T), RS1001595903 (X:79170243 T>G), RS1001690134 (X:79149594 G>A,C), RS1002023202 (X:79169923 T>C), RS1002032046 (X:79147068 G>T)
Disease associations
OMIM: gene MIM:300903 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
1 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001984_4 | Graves’ disease | 2.000000e-33 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL3562167 (SINGLE PROTEIN)
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: gpcr — Class A Orphans with emerging pharmacology
Most potent curated ligand interactions (1 total), top 1:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| lysophosphatidylserine | Full agonist | 7.1 | pEC50 |
ChEMBL bioactivities
136 potent at pChembl≥5 of 138 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 7.75 | EC50 | 18 | nM | CHEMBL3577172 |
| 7.74 | EC50 | 18.2 | nM | CHEMBL3577172 |
| 7.70 | IC50 | 20 | nM | CHEMBL4851095 |
| 7.60 | EC50 | 25 | nM | CHEMBL3577175 |
| 7.60 | EC50 | 25.12 | nM | CHEMBL3577175 |
| 7.51 | EC50 | 31 | nM | CHEMBL3577265 |
| 7.51 | EC50 | 30.9 | nM | CHEMBL3577265 |
| 7.48 | EC50 | 33 | nM | CHEMBL3577174 |
| 7.48 | EC50 | 33.11 | nM | CHEMBL3577174 |
| 7.40 | EC50 | 40 | nM | CHEMBL3577263 |
| 7.40 | EC50 | 39.81 | nM | CHEMBL3577263 |
| 7.36 | EC50 | 44 | nM | CHEMBL3577171 |
| 7.36 | EC50 | 43.65 | nM | CHEMBL3577171 |
| 7.20 | EC50 | 63 | nM | CHEMBL3577156 |
| 7.20 | EC50 | 63.1 | nM | CHEMBL3577156 |
| 7.12 | EC50 | 76 | nM | CHEMBL3577173 |
| 7.12 | EC50 | 75.86 | nM | CHEMBL3577173 |
| 7.09 | EC50 | 82 | nM | CHEMBL3577168 |
| 7.09 | EC50 | 81.28 | nM | CHEMBL3577168 |
| 7.07 | EC50 | 86 | nM | CHEMBL3577176 |
| 7.07 | EC50 | 85.11 | nM | CHEMBL3577176 |
| 7.00 | IC50 | 100 | nM | CHEMBL4863268 |
| 7.00 | IC50 | 100 | nM | CHEMBL4868780 |
| 6.82 | IC50 | 150 | nM | CHEMBL4864992 |
| 6.70 | EC50 | 200 | nM | CHEMBL4851095 |
| 6.54 | EC50 | 290 | nM | CHEMBL3577144 |
| 6.54 | EC50 | 288.4 | nM | CHEMBL3577144 |
| 6.52 | EC50 | 300 | nM | CHEMBL4855006 |
| 6.52 | EC50 | 300 | nM | CHEMBL4867113 |
| 6.52 | EC50 | 300 | nM | CHEMBL4863268 |
| 6.52 | EC50 | 300 | nM | CHEMBL4850132 |
| 6.40 | EC50 | 400 | nM | CHEMBL4867113 |
| 6.40 | EC50 | 400 | nM | CHEMBL4853607 |
| 6.40 | EC50 | 400 | nM | CHEMBL4847967 |
| 6.40 | EC50 | 400 | nM | CHEMBL4855006 |
| 6.40 | EC50 | 400 | nM | CHEMBL4864992 |
| 6.31 | EC50 | 490 | nM | CHEMBL3577169 |
| 6.31 | EC50 | 489.8 | nM | CHEMBL3577169 |
| 6.30 | EC50 | 500 | nM | CHEMBL4854909 |
| 6.30 | EC50 | 500 | nM | CHEMBL4878165 |
| 6.30 | EC50 | 500 | nM | CHEMBL4860146 |
| 6.30 | EC50 | 500 | nM | CHEMBL4852656 |
| 6.30 | EC50 | 500 | nM | CHEMBL4868780 |
| 6.30 | EC50 | 500 | nM | CHEMBL4859150 |
| 6.30 | EC50 | 500 | nM | CHEMBL4854655 |
| 6.30 | EC50 | 500 | nM | CHEMBL4851095 |
| 6.29 | EC50 | 510 | nM | CHEMBL3577170 |
| 6.29 | EC50 | 512.9 | nM | CHEMBL3577170 |
| 6.28 | EC50 | 520 | nM | CHEMBL1742484 |
| 6.28 | EC50 | 524.8 | nM | CHEMBL1742484 |
PubChem BioAssay actives
54 with measured affinity, of 80 total; 27 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 |
|---|---|---|---|---|
| (2S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[3-(3-undecoxyphenyl)propanoyloxy]propoxy]phosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.0180 | uM |
| (2S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[3-(3-pentadecoxyphenyl)propanoyloxy]propoxy]phosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.0250 | uM |
| (2S,3S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[3-(3-undecoxyphenyl)propanoylamino]propoxy]phosphoryl]oxybutanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.0309 | uM |
| (2S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[3-(2-pentadecoxyphenyl)propanoyloxy]propoxy]phosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.0330 | uM |
| (2S,3S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[3-(3-undecoxyphenyl)propanoyloxy]propoxy]phosphoryl]oxybutanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.0398 | uM |
| (2S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[3-(2-undecoxyphenyl)propanoyloxy]propoxy]phosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.0437 | uM |
| (2S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[[(Z)-octadec-9-enoyl]amino]propoxy]phosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.0630 | uM |
| (2S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[3-(4-undecoxyphenyl)propanoyloxy]propoxy]phosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.0759 | uM |
| (2S)-2-amino-3-[[(2R)-3-[3-(3-heptoxyphenyl)propanoyloxy]-2-hydroxypropoxy]-hydroxyphosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.0813 | uM |
| (2S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[3-(4-pentadecoxyphenyl)propanoyloxy]propoxy]phosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.0851 | uM |
| (2S)-2-amino-3-[[(2R)-3-[(Z)-hexadec-9-enoyl]oxy-2-hydroxypropoxy]-hydroxyphosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.2884 | uM |
| (2S)-2-amino-3-[[(2R)-3-[3-(4-heptoxyphenyl)propanoyloxy]-2-hydroxypropoxy]-hydroxyphosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.4898 | uM |
| (2S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[3-(2-nonoxyphenyl)propanoyloxy]propoxy]phosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.5100 | uM |
| (2S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[(Z)-octadec-9-enoyl]oxypropoxy]phosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.5200 | uM |
| (2S)-2-amino-3-[[(2R)-3-hexadecanoyloxy-2-hydroxypropoxy]-hydroxyphosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.5370 | uM |
| (2S,3S)-2-amino-3-[[(2R)-3-[(Z)-hexadec-9-enoyl]oxy-2-hydroxypropoxy]-hydroxyphosphoryl]oxybutanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.5800 | uM |
| (2S,3S)-2-amino-3-[[(2R)-3-[3-(3-heptoxyphenyl)propanoyloxy]-2-hydroxypropoxy]-hydroxyphosphoryl]oxybutanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.7200 | uM |
| (2S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-tetradecanoyloxypropoxy]phosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.7700 | uM |
| (2S,3S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-[(Z)-octadec-9-enoyl]oxypropoxy]phosphoryl]oxybutanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.8300 | uM |
| (2S)-2-amino-3-[[(2R)-2-fluoro-3-[3-(2-undecoxyphenyl)propanoyloxy]propoxy]-hydroxyphosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 0.8900 | uM |
| (2S,3S)-2-amino-3-[[(2R)-3-hexadecanoyloxy-2-hydroxypropoxy]-hydroxyphosphoryl]oxybutanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 1.0471 | uM |
| [(2R)-3-[[(2S)-2-amino-3-methoxy-3-oxopropoxy]-hydroxyphosphoryl]oxy-2-hydroxypropyl] (Z)-octadec-9-enoate | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 1.0965 | uM |
| (2S)-2-amino-3-[[(2R)-3-[3-(2-heptoxyphenyl)propanoyloxy]-2-hydroxypropoxy]-hydroxyphosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 1.3490 | uM |
| (2S,3S)-2-amino-3-[hydroxy-[(2R)-2-hydroxy-3-tetradecanoyloxypropoxy]phosphoryl]oxybutanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 1.5488 | uM |
| (2S)-2-amino-3-[[(2R)-3-dodecanoyloxy-2-hydroxypropoxy]-hydroxyphosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 1.7783 | uM |
| (2S)-2-amino-3-[hydroxy-[(2S)-2-hydroxy-3-[(Z)-octadec-9-enoyl]oxypropoxy]phosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 1.9000 | uM |
| (2S)-2-amino-3-[[(2R)-2-fluoro-3-[(Z)-octadec-9-enoyl]oxypropoxy]-hydroxyphosphoryl]oxypropanoic acid | 1226969: Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | ec50 | 1.9953 | uM |
CTD chemical–gene interactions
10 total (human), top 10 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Benzo(a)pyrene | decreases expression, decreases methylation | 2 |
| triphenyl phosphate | affects expression | 1 |
| quercitrin | increases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| (+)-JQ1 compound | decreases expression | 1 |
| Arsenic Trioxide | decreases expression | 1 |
| Air Pollutants | increases abundance, increases expression | 1 |
| Diethylhexyl Phthalate | decreases expression | 1 |
| Methyl Methanesulfonate | decreases expression | 1 |
| Particulate Matter | increases expression, increases abundance | 1 |
ChEMBL screening assays
39 unique, capped per target: 35 functional, 4 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL3579721 | Binding | Agonist activity at GPR174 (unknown origin) transfected in HEK293FT cells after 1 hr by TGFalpha shedding assay | Structure-activity relationships of lysophosphatidylserine analogs as agonists of G-protein-coupled receptors GPR34, P2Y10, and GPR174. — J Med Chem |
| CHEMBL4807192 | Functional | Inverse agonist activity at human GPR174 expressed in cells assessed as inhibition of CRE-luc reporter activity by measuring decrease in Gs-protein signalling activity relative to control | Inhibitors of GPR174 and Uses Thereof |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): Graves disease