QRFPR

Summary

QRFPR (pyroglutamylated RFamide peptide receptor, HGNC:15565) is a protein-coding gene on chromosome 4q27, encoding Pyroglutamylated RF-amide peptide receptor (Q96P65). Receptor for the orexigenic neuropeptide QRFP.

Enables G protein-coupled receptor activity. Involved in G protein-coupled receptor signaling pathway. Predicted to be located in non-motile cilium. Predicted to be active in plasma membrane.

Source: NCBI Gene 84109 — automated summary from GO annotations (Alliance of Genome Resources).

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 64 total
• GTEx eGene: eQTL in 24 tissues, sQTL in 0 (q < 0.05)
• Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 1.53 (unconstrained)
• MANE Select transcript: NM_198179
• Notable: 64 clinical variants but no curated precision-oncology (CIViC) evidence yet

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:15565
Approved symbol	QRFPR
Name	pyroglutamylated RFamide peptide receptor
Location	4q27
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000186867
Ensembl biotype	protein_coding
OMIM	606925
Entrez	84109

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 6 protein_coding, 1 nonsense_mediated_decay, 1 retained_intron

MANE Select: ENST00000394427

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 2, TSL 2: 2

ENST00000394427, ENST00000334383, ENST00000507331, ENST00000512235, ENST00000970622, ENST00001116200, ENST00001130429, ENST00001133274

RefSeq mRNA: 1 — MANE Select: NM_198179 NM_198179

CCDS: CCDS3719

Canonical transcript exons

ENST00000394427 — 6 exons

Exon	Start	End
ENSE00001333960	121336807	121336868
ENSE00001333965	121340452	121340610
ENSE00003488506	121328642	121329714
ENSE00003528799	121330426	121330523
ENSE00003553683	121380308	121381018
ENSE00003694338	121332821	121333056

Expression profiles

Bgee: expression breadth broad, 94 present calls, max score 83.42.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0640 / max 12.1953, expressed in 27 samples.

Highest expression (Bgee): primordial germ cell in gonad, cortex of kidney, metanephros cortex, heart left ventricle, prefrontal cortex.

Genetic regulation across tissues (GTEx eQTL / sQTL)

QRFPR is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 24 tissues and its splicing (sQTL) in 0 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 24 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Thyroid	eqtl	4.5e-52	-0.76	4:121355721:A:G
Esophagus Muscularis	eqtl	6.4e-25	+1.82	4:121316146:T:C
Testis	eqtl	3.0e-22	-0.73	4:121381268:T:A
Adrenal Gland	eqtl	3.2e-22	-0.86	4:121355721:A:G
Heart Atrial Appendage	eqtl	2.8e-17	-0.55	4:121355721:A:G
Esophagus Gastroesophageal Junction	eqtl	3.4e-16	+1.69	4:121316146:T:C
Artery Tibial	eqtl	5.0e-15	+1.24	4:121316146:T:C
Breast Mammary Tissue	eqtl	9.2e-13	+1.19	4:121316146:T:C
Heart Left Ventricle	eqtl	4.8e-12	-0.55	4:121398325:A:T
Esophagus Mucosa	eqtl	7.7e-11	+0.37	4:121376812:A:AC
Colon Sigmoid	eqtl	2.9e-09	+1.39	4:121316146:T:C
Skin Sun Exposed Lower leg	eqtl	3.0e-09	+0.90	4:121335397:C:T
Adipose Visceral Omentum	eqtl	3.5e-09	+1.15	4:121335937:A:T
Artery Coronary	eqtl	8.3e-08	+1.57	4:121316146:T:C
Brain Amygdala	eqtl	1.7e-04	+1.40	4:121443827:A:T
Brain Frontal Cortex BA9	eqtl	2.0e-04	-0.33	4:121371326:G:A
Pituitary	eqtl	2.5e-03	-0.31	4:121375652:C:T
Minor Salivary Gland	eqtl	2.7e-03	-0.54	4:121355721:A:G
Brain Spinal cord cervical c-1	eqtl	3.1e-03	-0.46	4:121355721:A:G
Artery Aorta	eqtl	3.9e-03	-0.28	4:121355721:A:G

FANTOM5 promoters

1 alternative TSS:

Promoter ID	TPM avg	Samples expressed
53799	0.0640	27

Top tissues by expression

showing 100 of 121 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	83.42	gold quality
cortex of kidney	UBERON:0001225	66.12	gold quality
metanephros cortex	UBERON:0010533	64.99	gold quality
heart left ventricle	UBERON:0002084	63.60	gold quality
prefrontal cortex	UBERON:0000451	60.89	gold quality
primary visual cortex	UBERON:0002436	60.65	gold quality
hypothalamus	UBERON:0001898	60.22	gold quality
right atrium auricular region	UBERON:0006631	59.83	gold quality
heart	UBERON:0000948	59.58	gold quality
apex of heart	UBERON:0002098	58.11	gold quality
kidney	UBERON:0002113	57.55	gold quality
superior frontal gyrus	UBERON:0002661	57.50	gold quality
bone marrow cell	CL:0002092	56.39	gold quality
adult mammalian kidney	UBERON:0000082	55.96	gold quality
frontal cortex	UBERON:0001870	53.54	gold quality
cortical plate	UBERON:0005343	52.02	silver quality
right adrenal gland	UBERON:0001233	49.08	gold quality
adrenal tissue	UBERON:0018303	48.82	gold quality
Brodmann (1909) area 9	UBERON:0013540	48.49	gold quality
cerebral cortex	UBERON:0000956	48.46	gold quality
right coronary artery	UBERON:0001625	48.07	gold quality
right lobe of thyroid gland	UBERON:0001119	47.71	gold quality
left adrenal gland cortex	UBERON:0035825	47.70	gold quality
right adrenal gland cortex	UBERON:0035827	47.62	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	47.24	gold quality
left adrenal gland	UBERON:0001234	47.10	gold quality
adrenal gland	UBERON:0002369	46.82	gold quality
left lobe of thyroid gland	UBERON:0001120	46.33	gold quality
thyroid gland	UBERON:0002046	46.30	gold quality
adenohypophysis	UBERON:0002196	46.03	gold quality
esophagus mucosa	UBERON:0002469	45.75	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	44.95	gold quality
corpus callosum	UBERON:0002336	43.58	silver quality
anterior cingulate cortex	UBERON:0009835	42.95	gold quality
brain	UBERON:0000955	42.86	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	42.61	gold quality
right frontal lobe	UBERON:0002810	42.24	gold quality
temporal lobe	UBERON:0001871	42.12	gold quality
bone marrow	UBERON:0002371	42.08	gold quality
ganglionic eminence	UBERON:0004023	42.04	gold quality
amygdala	UBERON:0001876	41.75	gold quality
pituitary gland	UBERON:0000007	41.42	gold quality
colonic epithelium	UBERON:0000397	41.27	gold quality
Ammon’s horn	UBERON:0001954	41.07	gold quality
ovary	UBERON:0000992	40.86	gold quality
endometrium	UBERON:0001295	40.54	silver quality
left ovary	UBERON:0002119	39.94	gold quality
omental fat pad	UBERON:0010414	39.90	gold quality
substantia nigra	UBERON:0002038	39.60	gold quality
mucosa of stomach	UBERON:0001199	39.36	silver quality
transverse colon	UBERON:0001157	39.18	gold quality
muscle tissue	UBERON:0002385	38.93	gold quality
esophagus	UBERON:0001043	38.83	gold quality
right ovary	UBERON:0002118	38.76	silver quality
prostate gland	UBERON:0002367	38.58	gold quality
colon	UBERON:0001155	38.28	gold quality
skeletal muscle tissue	UBERON:0001134	38.24	gold quality
fundus of stomach	UBERON:0001160	37.60	gold quality
smooth muscle tissue	UBERON:0001135	37.32	gold quality
duodenum	UBERON:0002114	37.28	gold quality
muscle layer of sigmoid colon	UBERON:0035805	37.23	gold quality
muscle of leg	UBERON:0001383	36.92	gold quality
gastrocnemius	UBERON:0001388	36.86	gold quality
intestine	UBERON:0000160	36.80	gold quality
granulocyte	CL:0000094	36.56	gold quality
ventricular zone	UBERON:0003053	36.48	gold quality
multicellular organism	UBERON:0000468	36.35	gold quality
vermiform appendix	UBERON:0001154	35.98	silver quality
mucosa of transverse colon	UBERON:0004991	35.65	gold quality
caudate nucleus	UBERON:0001873	35.59	silver quality
nucleus accumbens	UBERON:0001882	35.57	gold quality
sural nerve	UBERON:0015488	35.34	gold quality
descending thoracic aorta	UBERON:0002345	35.30	gold quality
monocyte	CL:0000576	35.25	silver quality
liver	UBERON:0002107	35.21	silver quality
lymph node	UBERON:0000029	35.14	gold quality
leukocyte	CL:0000738	35.11	silver quality
placenta	UBERON:0001987	34.64	gold quality
tibial artery	UBERON:0007610	34.37	gold quality
popliteal artery	UBERON:0002250	34.31	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	33.85	gold quality
left uterine tube	UBERON:0001303	33.72	gold quality
thoracic aorta	UBERON:0001515	33.63	silver quality
ascending aorta	UBERON:0001496	33.53	silver quality
endocervix	UBERON:0000458	33.50	silver quality
left coronary artery	UBERON:0001626	33.17	gold quality
right lung	UBERON:0002167	32.84	gold quality
small intestine	UBERON:0002108	32.72	silver quality
myometrium	UBERON:0001296	32.57	silver quality
lung	UBERON:0002048	32.47	gold quality
adipose tissue	UBERON:0001013	32.45	gold quality
stomach	UBERON:0000945	31.51	gold quality
lower esophagus	UBERON:0013473	31.20	gold quality
lower esophagus muscularis layer	UBERON:0035833	31.14	gold quality
small intestine Peyer’s patch	UBERON:0003454	31.02	silver quality
thoracic mammary gland	UBERON:0005200	30.50	gold quality
testis	UBERON:0000473	30.48	silver quality
minor salivary gland	UBERON:0001830	30.39	gold quality
saliva-secreting gland	UBERON:0001044	30.28	gold quality
putamen	UBERON:0001874	30.21	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	3.92

HPA expression

RNA tissue specificity: Tissue enhanced

60 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Frontal cortex	tissue	3.2
Postcentral gyrus	tissue	2.3
Locus coeruleus	tissue	1.5
Choroid plexus	tissue	1.1
Hippocampus	tissue	1.0	not detected
Cerebral cortex	tissue	0.9	not detected
Motor cortex	tissue	0.9
Nucleus accumbens	tissue	0.9
Insular cortex	tissue	0.9
Heart muscle	tissue	0.7	not detected
Caudate putamen	tissue	0.6
Putamen	tissue	0.5
Kidney	tissue	0.5	low
Prefrontal cortex	tissue	0.4
Basal ganglia	tissue	0.4	not detected
Hypothalamus	tissue	0.4	medium
Thyroid gland	tissue	0.4	medium
Hippocampal formation	tissue	0.4
Retrosplenial and cingulate cortex	tissue	0.4
Septum	tissue	0.4
Retrosplenial cortex	tissue	0.4
Pituitary gland	tissue	0.3
Ovary	tissue	0.3	not detected
Amygdala	tissue	0.3
Thalamus	tissue	0.3
Ventral forebrain	tissue	0.3
Temporal cortex	tissue	0.3
Stomach 1	tissue	0.2	medium
Midbrain	tissue	0.2
Medulla oblongata	tissue	0.2
Adrenal gland	tissue	0.2	low
Bone marrow	tissue	0.2	not detected
Entorhinal cortex	tissue	0.2
Skin 1	tissue	0.1	not detected
Breast	tissue	0.1	not detected
Testis	tissue	0.1	medium
Retina	tissue	0.1
Pons	tissue	0.1
Seminal vesicle	tissue	0.1	medium
Adipose tissue	tissue	0.1	not detected
Esophagus	tissue	0.1	not detected
Epididymis	tissue	0.1	medium
Substantia nigra	tissue	0.1
Spinal cord	tissue	0.1
Corpus callosum	tissue	0.1
Prostate	tissue	0.1	medium
Periaqueductal gray	tissue	0.1
Somatosensory cortex	tissue	0.1
Appendix	tissue	0.1	medium
Occipital cortex	tissue	0.1
Cervix	tissue	0.0	low
Salivary gland	tissue	0.0	low
Rectum	tissue	0.0	medium
Colon	tissue	0.0	medium
Pancreas	tissue	0.0	low
Endometrium 1	tissue	0.0	low
Placenta	tissue	0.0	medium
Small intestine	tissue	0.0	medium
Duodenum	tissue	0.0	medium
Fallopian tube	tissue	0.0	medium

Brain sub-regions (HPA Brain Atlas): detected in 187; highest nTPM — Lateral hypothalamic area (14.0), Ventromedial nucleus (7.8), Nuclei of the trapezoid body (7.7), Preoptic area (7.6), Pontine nuclei (7.0).

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

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

showing 30 of 32 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-4668-3P	100.00	68.74	2635
HSA-MIR-30A-5P	100.00	76.31	3233
HSA-MIR-30B-5P	100.00	76.29	3248
HSA-MIR-30C-5P	100.00	76.29	3248
HSA-MIR-30D-5P	100.00	76.32	3233
HSA-MIR-30E-5P	100.00	76.32	3242
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-MIR-6809-3P	99.91	71.45	3814
HSA-MIR-153-5P	99.89	73.86	6317
HSA-MIR-4659A-3P	99.80	72.62	4248
HSA-MIR-4659B-3P	99.80	72.62	4248
HSA-MIR-323A-3P	99.79	70.30	1739
HSA-MIR-7856-5P	99.75	69.99	2901
HSA-MIR-4261	99.59	70.30	3415
HSA-MIR-6716-5P	99.56	68.62	1244
HSA-MIR-147B-5P	99.45	70.62	2432
HSA-MIR-6507-5P	99.36	70.46	2524
HSA-MIR-6504-3P	99.17	69.31	2891
HSA-MIR-10399-5P	99.17	69.87	2610
HSA-MIR-7151-3P	99.04	69.72	2370
HSA-MIR-181A-2-3P	98.91	67.60	1168
HSA-MIR-374B-3P	98.63	68.24	1360
HSA-MIR-299-5P	98.56	71.14	1140
HSA-MIR-6878-5P	98.49	67.91	2142
HSA-MIR-6509-3P	98.32	67.33	1343
HSA-MIR-12120	98.05	68.44	1768
HSA-MIR-194-3P	97.36	65.96	1027
HSA-MIR-6759-3P	96.94	68.31	823

Functional genomics

gnomAD constraint: pLI 6.27e-12, LOEUF 1.53, missense Z 0.145 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000394427 — one region, missense o/e 1.02.

Literature-anchored findings (GeneRIF, showing 9)

• characterization and tissue distribution of SP9155 (GPR103) ligand (PMID:12714592)
• QRFP and GPR103A/B may regulate diverse neuroendocrine and behavioral functions and implicate this neuropeptide system in metabolic syndrome (PMID:16648250)
• Results suggest that GPR103b and QRFP work in an autocrine/paracrine manner to regulate adipogenesis. (PMID:20534693)
• Effects of systematic N-terminus deletions and benzoylations of endogenous RF-amide peptides on NPFF1R, NPFF2R, GPR10, GPR54 and GPR103. (PMID:26211894)
• The expression of both QRFP and GPR103 at the gene and protein level was higher in human prostate cancer tissue samples compared to control and benign prostatic hyperplasia samples. (PMID:30483810)
• The study represents the first to use WES in multiplex families for preeclampsia and identifies two novel genes (QRFPR and C1orf35) not previously associated with preeclampsia and find nominal association of rs34270076 with protein levels. (PMID:30633125)
• N-glycosylation of the human neuropeptide QRFP receptor (QRFPR) is essential for ligand binding and receptor activation. (PMID:33655503)
• Two naturally occurring mutations of human GPR103 define distinct G protein selection bias. (PMID:33872671)
• The variations in human orphan G protein-coupled receptor QRFPR affect PI3K-AKT-mTOR signaling. (PMID:34018631)

Cross-species orthologs

10 orthologs

Organism	Symbol	Gene ID
danio_rerio	qrfpra	ENSDARG00000039349
danio_rerio	qrfprb	ENSDARG00000101969
mus_musculus	Qrfprl	ENSMUSG00000029917
mus_musculus	Qrfpr	ENSMUSG00000058400
rattus_norvegicus	Qrfprl	ENSRNOG00000006782
rattus_norvegicus	Qrfpr	ENSRNOG00000014414
drosophila_melanogaster	AkhR	FBGN0025595
drosophila_melanogaster	CCAP-R	FBGN0039396
caenorhabditis_elegans		WBGENE00013642
caenorhabditis_elegans	gnrr-1	WBGENE00018798

Paralogs (16): NPFFR2 (ENSG00000056291), GNRHR (ENSG00000109163), CCKBR (ENSG00000110148), HCRTR1 (ENSG00000121764), AVPR2 (ENSG00000126895), GALR3 (ENSG00000128310), HCRTR2 (ENSG00000137252), NPFFR1 (ENSG00000148734), CCKAR (ENSG00000163394), AVPR1A (ENSG00000166148), GALR1 (ENSG00000166573), GPR22 (ENSG00000172209), GPR150 (ENSG00000178015), OXTR (ENSG00000180914), FFAR4 (ENSG00000186188), AVPR1B (ENSG00000198049)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:2677633) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 9 distinct phenotype terms.

Mouse phenotype (MP)	Records
decreased bone mineral density	1
abnormal trabecular bone morphology	1
abnormal vertebrae morphology	1
kyphosis	1
abnormal lumbar vertebrae morphology	1
abnormal response/metabolism to endogenous compounds	1
abnormal intervertebral disk morphology	1
abnormal vertebrae development	1
abnormal nucleus pulposus morphology	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	Q5IS62	100.0%	Diamond
Ovis aries	Q28602	99.1%	Diamond
Macaca mulatta	Q9GK74	99.0%	Diamond
Bos taurus	P79113	97.9%	Diamond
Sus scrofa	O02836	95.2%	Diamond
Cavia porcellus	Q9Z2D5	93.8%	Diamond
Gallus gallus	Q9DDN6	81.9%	Diamond
Xenopus laevis	P34992	81.6%	Diamond
Tribolium castaneum	G4WMX4	53.7%	Diamond
Branchiostoma floridae	C3ZQF9	47.8%	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
NDNF-AS1	ncRNA	105377400
NDNF	protein-coding	79625
TNIP3	protein-coding	79931
PRDM5-DT	ncRNA	105377399
PRDM5	protein-coding	11107

Protein

Protein identifiers

Pyroglutamylated RF-amide peptide receptor — Q96P65 (reviewed: Q96P65)

Alternative names: AQ27, G protein-coupled receptor 103, Orexigenic neuropeptide QRFP receptor, SP9155

All UniProt accessions (3): Q96P65, F2Z3L3, J3KNR3

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for the orexigenic neuropeptide QRFP. The activity of this receptor is mediated by G proteins that modulate adenylate cyclase activity and intracellular calcium levels.

Subcellular location. Cell membrane.

Tissue specificity. Expressed widely in the brain with high levels in the hypothalamus, trigeminal ganglia and vestibular neurons, and moderate levels in the amygdala, cortex, pituitary, hippocampus, thalamus, caudate nucleus and medulla oblongata. In peripheral tissues, expressed at high levels in the retina and at moderate levels in the heart, kidney, testis and thyroid.

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

RefSeq proteins (1): NP_937822* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000611	NPY_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (43 total): helix 18, topological domain 8, transmembrane region 7, sequence variant 3, sequence conflict 2, strand 2, chain 1, glycosylation site 1, turn 1

Structure

Experimental structures (PDB)

2 structures by resolution:

PDB	Title	Method	Resolution (Å)
8WZ2	Structure of 26RFa-pyroglutamylated RFamide peptide receptor complex	ELECTRON MICROSCOPY	2.73
8ZH8	Human GPR103 -Gq complex bound to QRFP26	ELECTRON MICROSCOPY	3.19

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q96P65-F1	78.74	0.45

Antibody-complex structures (SAbDab)

2 antibodies co-crystallized with this protein: 8WZ2, 8ZH8

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

Antibody reliability (HPA): IH approved

Functional residue map

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

Glycosylation sites (1)

Type	Positions
N-linked (glcnac…) asparagine	19

Function

Pathways and Gene Ontology

Reactome pathways

2 curated (TAS) of 8; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

8 pathways:

ID	Pathway	Evidence
R-HSA-416476	G alpha (q) signalling events	curated
R-HSA-389397	Orexin and neuropeptides FF and QRFP bind to their respective receptors	curated
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)	—
R-HSA-388396	GPCR downstream signalling	—
R-HSA-500792	GPCR ligand binding	—
R-HSA-375276	Peptide ligand-binding receptors	—
R-HSA-162582	Signal Transduction	—
R-HSA-372790	Signaling by GPCR	—

MSigDB gene sets: 54 (showing top): GSE45365_HEALTHY_VS_MCMV_INFECTION_CD8_TCELL_IFNAR_KO_UP, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, GOBP_RESPONSE_TO_HORMONE, GOMF_PEPTIDE_RECEPTOR_ACTIVITY, AACTTT_UNKNOWN, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, REACTOME_G_ALPHA_Q_SIGNALLING_EVENTS, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, MEISSNER_NPC_HCP_WITH_H3_UNMETHYLATED, MEISSNER_BRAIN_HCP_WITH_H3K4ME3_AND_H3K27ME3, MIKKELSEN_MCV6_HCP_WITH_H3K27ME3, MIKKELSEN_MEF_HCP_WITH_H3K27ME3, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY

GO Biological Process (4): G protein-coupled receptor signaling pathway (GO:0007186), cellular response to hormone stimulus (GO:0032870), signal transduction (GO:0007165), neuropeptide signaling pathway (GO:0007218)

GO Molecular Function (3): G protein-coupled receptor activity (GO:0004930), neuropeptide Y receptor activity (GO:0004983), protein binding (GO:0005515)

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

Reactome top-level categories

6 top-level categories:

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

GO top-level categories

17 GO namespaces:

Category	Terms
G protein-coupled receptor signaling pathway	2
G protein-coupled receptor activity	1
signal transduction	1
response to hormone	1
cellular response to chemical stimulus	1
cellular response to endogenous stimulus	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
transmembrane signaling receptor activity	1
neuropeptide receptor activity	1
binding	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 2 of 9 annotations. The rest are phylogenetic / computational / electronic (IEA).

2 experimentally-supported GO terms:

GO term	NS	Evidence
G protein-coupled receptor signaling pathway	BP	direct assay
G protein-coupled receptor activity	MF	direct assay

Protein interactions and networks

STRING

showing 15 of 460 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
QRFPR	QRFP	P83859	988
QRFPR	GAL	P22466	754
QRFPR	GNAQ	P50148	698
QRFPR	NPFF	O15130	598
QRFPR	NPVF	Q9HCQ7	550
QRFPR	PRLH	P81277	483
QRFPR	HCRT	O43612	423
QRFPR	GPR149	Q86SP6	387
QRFPR	CCDC137	Q6PK04	382
QRFPR	IGFLR1	Q9H665	361
QRFPR	TRAM1L1	Q8N609	361
QRFPR	MMAB	Q96EY8	361
QRFPR	PHTF1	Q9UMS5	354
QRFPR	HBM	Q6B0K9	349
QRFPR	NPY	P01303	340

IntAct

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

5 partners by confidence:

Partner	Interaction type	MIscore	Records
GJA8	physical association	0.560	3
NTM	physical association	0.560	3
RAMP1	physical association	0.400	3
RAMP2	physical association	0.400	3
RAMP3	physical association	0.400	3

BioGRID (11 interactions; top human partners by supporting records): GJA8 (Two-hybrid), IL1RAP (Co-fractionation), NSF (Co-fractionation), NTM (Two-hybrid), PTEN (Affinity Capture-MS), SLC15A4 (Co-fractionation), SLC38A1 (Co-fractionation), SLCO4A1 (Co-fractionation), SMCHD1 (Co-fractionation), TMED10 (Co-fractionation), TMED9 (Co-fractionation)

Protein complexes (CORUM) (2)

Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).

2 complexes by size:

Complex	Subunits	Members
★ HCRTR1-QRFPR complex	2	HCRTR1, QRFPR
★ HCRTR2-QRFPR complex	2	QRFPR, HCRTR2

Ligand–receptor pairs (CellPhoneDB) (1)

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

1 ligand–receptor pairs:

Partner	This gene’s role	Signaling class
QRFP	receptor

Disease & clinical

Genetic variants

Variant evidence for QRFPR: 64 ClinVar records (0 pathogenic / likely pathogenic); 3 GWAS associations.

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	58
Likely benign	0
Benign	0

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 28 predictions of 652):

Position(s)	Effect	Δscore	Sites
4:121336795	donor_gain	1.0000
4:121330524–121330525	acceptor_loss	0.9900	6
4:121330531	acceptor_gain	0.9900
4:121337775	donor_gain	0.9900
4:121340455	donor_gain	0.9900
4:121340611–121340612	acceptor_loss	0.9900	6
4:121380306–121380307	donor_loss	0.9900	4
4:121330421	donor_loss	0.9800
4:121330424–121330425	donor_loss	0.9800	6
4:121333061	acceptor_gain	0.9800

AlphaMissense

651 missense substitutions predicted likely pathogenic (of 2,856 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
D91	8	0.930	0.966
F282	8	0.918	0.990
N63	8	0.909	0.971
C118	7	0.976	0.988
W205	7	0.951	0.993
C201	7	0.949	0.970
W286	7	0.917	0.983
W111	7	0.909	0.975
F83	7	0.908	0.947
F223	7	0.904	0.965
N328	7	0.881	0.963
F289	7	0.873	0.956
R143	7	0.860	0.976
F25	7	0.857	0.961
F322	7	0.840	0.955
E142	7	0.820	0.917
D191	7	0.817	0.871
W170	7	0.807	0.992
P329	6	0.903	0.952
P226	6	0.899	0.975

HPA cancer prognostics

RNA cancer specificity: Group enriched (Kidney Renal Clear Cell Carcinoma, Kidney Renal Papillary Cell Carcinoma)

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

3 prognostic cancer types:

Cancer	Prognostic	p-value
Kidney Renal Clear Cell Carcinoma (TCGA)	favorable	1.38e-08
Kidney Renal Papillary Cell Carcinoma (TCGA)	favorable	0.000436
Kidney Renal Clear Cell Carcinoma (validation)	favorable	0.000516

Disease associations

OMIM: gene MIM:606925 | disease phenotypes:

GWAS associations

3 associations:

Study	Trait	p-value
GCST002876_11	Type 1 diabetes and autoimmune thyroid diseases	4e-10
GCST012053_11	Weight	5e-8
GCST009391_69	Metabolite levels	2e-6

EFO canonical traits (from GWAS)

2 canonical traits:

EFO ID	Trait name
EFO:0010473	cyclic adenosine monophosphate measurement
EFO:0004338	body weight

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5852 (SINGLE PROTEIN)

PharmGKB: 1 entry (CPIC guideline: no)

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — QRFP receptor

Most potent curated ligand interactions (10 total), top 10:

Ligand	Action	Affinity	Parameter
[125I]QRFP43 (human)	Full agonist	10.3	pKd
QRFP43 (43RFa)	Full agonist	8.57	pEC50
QRFP26	Full agonist	8.22	pEC50
QRFP26 (26RFa)	Full agonist	8.15	pEC50
QRFP43	Full agonist	7.64	pEC50
compound 25e [PMID: 25875054]	Antagonist	7.34	pIC50
LV-2186	Agonist	7.18	pEC50
QRFP43	Full agonist	7.15	pEC50
LV-2172	Agonist	6.79	pEC50
LV-2211	Agonist	6.49	pEC50

Binding affinities (BindingDB)

99 measured of 139 human assays (140 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
P550	EC50	4.9 nM
CHEMBL4284294	EC50	6.9 nM
P518	EC50	10 nM
CHEMBL3287810	IC50	25 nM
CHEMBL1802418	EC50	30.2 nM
CHEMBL1802419	EC50	37.5 nM
CHEMBL1802480	EC50	39 nM
CHEMBL3287814	IC50	40 nM
CHEMBL1800099	EC50	43.2 nM
CHEMBL4277648	EC50	46 nM
CHEMBL4281420	EC50	66 nM
CHEMBL1802482	EC50	67 nM
CHEMBL3287585	IC50	79 nM
CHEMBL2170403	EC50	94 nM
CHEMBL1802420	EC50	95.3 nM
CHEMBL3287811	IC50	100 nM
CHEMBL3314358	IC50	110 nM
CHEMBL3287586	IC50	126 nM
CHEMBL3287813	IC50	126 nM
CHEMBL3314354	IC50	130 nM
CHEMBL2170390	EC50	136 nM
CHEMBL1802416	EC50	138 nM
CHEMBL2170249	EC50	138 nM
CHEMBL3287584	IC50	158 nM
CHEMBL2170402	EC50	164 nM
CHEMBL1802373	EC50	166 nM
CHEMBL1802417	EC50	185 nM
CHEMBL3287833	IC50	200 nM
CHEMBL1802369	EC50	233 nM
CHEMBL1802423	EC50	233 nM
P517	KI	235 nM
CHEMBL1802421	EC50	237 nM
P52	KI	245 nM
P513	KI	258 nM
CHEMBL1802422	EC50	282 nM
CHEMBL1802476	EC50	282 nM
CHEMBL2170396	EC50	341 nM
CHEMBL1802370	EC50	355 nM
CHEMBL1802372	EC50	374 nM
CHEMBL2170401	EC50	382 nM
CHEMBL2170389	EC50	429 nM
CHEMBL1802379	EC50	455 nM
CHEMBL3314361	IC50	460 nM
CHEMBL3314359	IC50	500 nM
CHEMBL3287819	IC50	501 nM
CHEMBL3314350	IC50	570 nM
CHEMBL4277047	IC50	579 nM
CHEMBL1802377	EC50	588 nM
P552	KI	607 nM
CHEMBL3287821	IC50	631 nM

ChEMBL bioactivities

132 potent at pChembl≥5 of 137 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.90	IC50	1.26	nM	CHEMBL1802413
8.69	Ki	2.04	nM	CHEMBL1802414
8.31	EC50	4.9	nM	CHEMBL1802414
8.16	EC50	6.9	nM	CHEMBL4284294
7.99	EC50	10.2	nM	CHEMBL1802413
7.98	EC50	10.4	nM	CHEMBL1802413
7.90	IC50	12.59	nM	CHEMBL3287814
7.70	IC50	19.95	nM	CHEMBL3287810
7.70	IC50	19.95	nM	CHEMBL3287813
7.60	IC50	25.12	nM	CHEMBL3287810
7.52	EC50	30.2	nM	CHEMBL1802418
7.43	EC50	37.5	nM	CHEMBL1802419
7.41	EC50	39	nM	CHEMBL1802480
7.40	IC50	39.81	nM	CHEMBL3287814
7.40	IC50	40	nM	CHEMBL3314362
7.37	EC50	43.2	nM	CHEMBL1800099
7.34	IC50	46	nM	CHEMBL3314362
7.34	EC50	46	nM	CHEMBL4277648
7.30	IC50	50.12	nM	CHEMBL3287584
7.20	IC50	63.1	nM	CHEMBL3287811
7.18	EC50	66.4	nM	CHEMBL4281420
7.17	EC50	67	nM	CHEMBL1802482
7.16	IC50	70	nM	CHEMBL3314349
7.10	IC50	79.43	nM	CHEMBL3287585
7.03	EC50	93.6	nM	CHEMBL2170403
7.02	EC50	95.3	nM	CHEMBL1802420
7.00	IC50	100	nM	CHEMBL3287586
7.00	IC50	100	nM	CHEMBL3287811
6.96	IC50	110	nM	CHEMBL3314358
6.90	IC50	125.9	nM	CHEMBL3287586
6.90	IC50	125.9	nM	CHEMBL3287813
6.89	IC50	130	nM	CHEMBL3314354
6.87	EC50	136	nM	CHEMBL2170390
6.86	EC50	138	nM	CHEMBL2170249
6.86	EC50	138	nM	CHEMBL1802416
6.80	IC50	158.5	nM	CHEMBL3287812
6.80	IC50	158.5	nM	CHEMBL3287584
6.79	EC50	164	nM	CHEMBL2170402
6.78	EC50	166	nM	CHEMBL1802373
6.73	EC50	185	nM	CHEMBL1802417
6.70	IC50	199.5	nM	CHEMBL3287833
6.63	EC50	233	nM	CHEMBL1802423
6.63	EC50	233	nM	CHEMBL1802369
6.62	IC50	240	nM	CHEMBL3314352
6.62	EC50	237	nM	CHEMBL1802421
6.60	IC50	251.2	nM	CHEMBL3287819
6.60	IC50	251.2	nM	CHEMBL3287821
6.55	IC50	280	nM	CHEMBL3314352
6.55	EC50	282	nM	CHEMBL1802422
6.55	EC50	282	nM	CHEMBL1802476

PubChem BioAssay actives

132 with measured affinity, of 283 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
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	701390: Displacement of [125I]26RFa from human GPR103 expressed in HEK293 cells incubated for 1 h by gamma counter based method	ic50	0.0013	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	1820168: Displacement of [125I]-43RFa from human QRFP receptor expressed in CHO cells by TopCount scintillation counting method	ki	0.0020	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	1409316: Agonist activity at human QRFPR expressed in CHO cells co-expressing Galpha16 assessed as increase Ca2+ mobilization after 3 mins by Fluo-4 AM-based scanning fluorometery	ec50	0.0069	uM
4-chloro-N’-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]benzenecarboximidamide	1154925: Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay	ic50	0.0126	uM
N’-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]benzenecarboximidamide	1154925: Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay	ic50	0.0199	uM
5-bromo-N’-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]thiophene-2-carboximidamide	1154925: Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay	ic50	0.0199	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2,4-diamino-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.0302	uM
(4S)-4-amino-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.0375	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.0390	uM
(5-chloro-1-methylindol-2-yl)-[6-[(dimethylamino)methyl]-7-methyl-3,4-dihydro-1H-isoquinolin-2-yl]methanone	1180052: Displacement of [125I]QRFP43 from human GPR103 receptor expressed in HEK cells after 90 mins incubation by scintillation counting	ic50	0.0400	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-4-methyl-2-[[(2S)-pyrrolidine-2-carbonyl]amino]pentanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.0432	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-amino-3-methylbutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	1409316: Agonist activity at human QRFPR expressed in CHO cells co-expressing Galpha16 assessed as increase Ca2+ mobilization after 3 mins by Fluo-4 AM-based scanning fluorometery	ec50	0.0460	uM
N’-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]thiophene-2-carboximidamide	1154925: Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay	ic50	0.0501	uM
N’-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]-4-methylthiophene-2-carboximidamide	1154925: Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay	ic50	0.0631	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-[(N’-methylcarbamimidoyl)amino]pentanamide	1409316: Agonist activity at human QRFPR expressed in CHO cells co-expressing Galpha16 assessed as increase Ca2+ mobilization after 3 mins by Fluo-4 AM-based scanning fluorometery	ec50	0.0664	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-(benzylamino)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.0670	uM
(5-chloro-1-methylindol-2-yl)-[6-[(dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanone	1180051: Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay	ic50	0.0700	uM
(6R)-N-(5-chloro-2-methoxyphenyl)-6-(dimethylamino)-4-methoxy-5,6,7,8-tetrahydronaphthalene-1-sulfonamide	1154925: Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay	ic50	0.0794	uM
(2S)-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)-2-[[(2S)-2-[[2-[2,3-dihydroxypropyl-[[(2S)-3-phenyl-2-[(2-piperazin-1-ylacetyl)amino]propanoyl]amino]amino]acetyl]amino]-3-phenylpropanoyl]amino]pentanamide	701391: Agonist activity at human GPR103 expressed in CHO cells co-expressing Galpha16 assessed as increase in intracellular calcium level measured for 2 mins by fluorimetry	ec50	0.0936	uM
(2S)-2-amino-N-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]butanediamide	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.0953	uM
N’-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]thiophene-3-carboximidamide	1154925: Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay	ic50	0.1000	uM
(5-bromo-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[(dimethylamino)methyl]-4-methyl-3,4-dihydro-1H-isoquinolin-2-yl]methanone	1180051: Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay	ic50	0.1100	uM
[6-[(dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-(5-iodo-1-methylpyrrolo[2,3-c]pyridin-2-yl)methanone	1180051: Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay	ic50	0.1300	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[2-(2-aminoacetyl)hydrazinyl]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamide	701391: Agonist activity at human GPR103 expressed in CHO cells co-expressing Galpha16 assessed as increase in intracellular calcium level measured for 2 mins by fluorimetry	ec50	0.1360	uM
(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-N-[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]hexanamide	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.1380	uM
(2S)-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-3-hydroxy-2-[[(2S)-3-phenyl-2-[(2-piperazin-1-ylacetyl)amino]propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]pentanamide	701391: Agonist activity at human GPR103 expressed in CHO cells co-expressing Galpha16 assessed as increase in intracellular calcium level measured for 2 mins by fluorimetry	ec50	0.1380	uM
4-bromo-N’-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]thiophene-2-carboximidamide	1154925: Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay	ic50	0.1585	uM
(2S)-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)-2-[[(2S)-3-phenyl-2-[[2-[[[(2S)-3-phenyl-2-[(2-piperazin-1-ylacetyl)amino]propanoyl]amino]-propylamino]acetyl]amino]propanoyl]amino]pentanamide	701391: Agonist activity at human GPR103 expressed in CHO cells co-expressing Galpha16 assessed as increase in intracellular calcium level measured for 2 mins by fluorimetry	ec50	0.1640	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-(dibenzylamino)-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.1660	uM
(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-N-[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]hexanamide	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.1850	uM
N’-[3-(2-cyclopentylethyl)-4-methoxyphenyl]benzenecarboximidamide	1154926: Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting	ic50	0.1995	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]pentanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamide	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.2330	uM
(2S)-2,6-diamino-N-[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]hexanamide	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.2330	uM
(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-N-[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]hexanamide	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.2370	uM
(5-bromo-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[(dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanone	1180051: Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay	ic50	0.2400	uM
N’-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]pyridine-3-carboximidamide	1154925: Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay	ic50	0.2512	uM
N-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]-N’-methylthiophene-2-carboximidamide	1154925: Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay	ic50	0.2512	uM
(2S)-6-amino-N-[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]hexanamide	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.2820	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[di(piperidin-1-yl)amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.2820	uM
(2S)-2-[[(2S)-2-[[2-[[[(2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-(2,3-dihydroxypropyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamide	701391: Agonist activity at human GPR103 expressed in CHO cells co-expressing Galpha16 assessed as increase in intracellular calcium level measured for 2 mins by fluorimetry	ec50	0.3410	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]butanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamide	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.3550	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamide	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.3740	uM
(2S)-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)-2-[[(2S)-2-[[2-[2,3-dihydroxypropyl-[[(2S)-3-phenyl-2-[(2-pyrazolidin-1-ylacetyl)amino]propanoyl]amino]amino]acetyl]amino]-3-phenylpropanoyl]amino]pentanamide	701391: Agonist activity at human GPR103 expressed in CHO cells co-expressing Galpha16 assessed as increase in intracellular calcium level measured for 2 mins by fluorimetry	ec50	0.3820	uM
(2S)-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-hydrazinylacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]pentanamide	701391: Agonist activity at human GPR103 expressed in CHO cells co-expressing Galpha16 assessed as increase in intracellular calcium level measured for 2 mins by fluorimetry	ec50	0.4290	uM
(2S)-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[bis(dimethylamino)methylideneamino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanamide	606472: Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis	ec50	0.4550	uM
(5-chloro-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[1-(dimethylamino)ethyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanone	1180051: Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay	ic50	0.4600	uM
(5-chloro-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[(dimethylamino)methyl]-1-methyl-3,4-dihydro-1H-isoquinolin-2-yl]methanone	1180051: Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay	ic50	0.5000	uM
N’-[3-(cyclopentylsulfanylmethyl)-4-fluorophenyl]thiophene-2-carboximidamide	1154925: Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay	ic50	0.5012	uM
(5-chloro-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[(dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanone	1180051: Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay	ic50	0.5700	uM
(5-bromo-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[(dimethylamino)methyl]-4-methyl-1,3-dihydroisoquinolin-8a-ylium-2-yl]methanone	1409317: Antagonist activity at human QRFPR expressed in CHO cells co-expressing Galpha16 assessed as inhibition of 26RFa-induced Ca2+ mobilization preincubated for 15 mins followed by agonist addition measured after 3 mins by Fluo-4 AM-based scanning fluorometery	ic50	0.5790	uM

CTD chemical–gene interactions

27 total (human), top 27 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, increases expression, affects expression	3
Benzo(a)pyrene	increases expression, increases methylation	2
Phenylmercuric Acetate	affects cotreatment, increases expression	2
FR900359	increases phosphorylation	1
ethyl-p-hydroxybenzoate	increases expression	1
terbufos	increases methylation	1
arsenite	decreases expression	1
sodium arsenite	decreases expression	1
tobacco tar	increases expression	1
chloropicrin	increases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	increases expression, affects cotreatment	1
erucylphospho-N,N,N-trimethylpropylammonium	increases expression	1
ICG 001	increases expression	1
dorsomorphin	affects cotreatment, increases expression	1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid	increases expression	1
Temozolomide	decreases expression	1
Caffeine	increases phosphorylation	1
Fonofos	increases methylation	1
Gasoline	affects cotreatment, increases abundance, increases expression	1
Parathion	increases methylation	1
Polycyclic Aromatic Hydrocarbons	affects cotreatment, increases abundance, increases expression	1
Thiram	decreases expression	1
Triclosan	decreases expression	1
Asbestos, Crocidolite	decreases expression	1
Cadmium Chloride	decreases expression	1
Okadaic Acid	increases expression	1
Particulate Matter	affects cotreatment, increases abundance, increases expression	1

ChEMBL screening assays

26 unique, capped per target: 13 binding, 13 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1031407	Binding	Inhibition of human GPR103 at 3 uM	Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. — *J Med Chem*
CHEMBL1804403	Functional	Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization at 10’ -12 to 10’-5 M after 2 mins by fluorometric analysis	Structure-activity relationships of a series of analogues of the RFamide-related peptide 26RFa. — *J Med Chem*

Cellosaurus cell lines

2 cell lines: 2 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_H442	CHO-K1/GPR103/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KX20	PathHunter CHO-K1 GPR103 beta-arrestin	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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

Predicted chemistry — Sugi Predict

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