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 — RefSeq curated summary.

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 64 total
• Druggable target: yes
• MANE Select transcript: NM_198179

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: 5 — 3 protein_coding, 1 nonsense_mediated_decay, 1 retained_intron

ENST00000334383, ENST00000394427, ENST00000507331, ENST00000512235, ENST00000970622

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.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
53799	0.0640	27

Top tissues by expression

121 total, 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

Single-cell (SCXA)

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

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

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

32 targeting QRFPR, 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-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

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

7 orthologs

Organism	Symbol	Gene ID
danio_rerio	qrfpra	ENSDARG00000039349
danio_rerio	QRFPR	ENSDARG00000101969
mus_musculus	Qrfprl	ENSMUSG00000029917
mus_musculus	Qrfpr	ENSMUSG00000058400
rattus_norvegicus	Qrfprl	ENSRNOG00000006782
rattus_norvegicus	Qrfpr	ENSRNOG00000014414
drosophila_melanogaster	SIFaR	FBGN0038880

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)

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): F2Z3L3, J3KNR3, Q96P65

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 (40 total): helix 15, 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.

PDB	Method	Resolution (Å)
8WZ2	ELECTRON MICROSCOPY	2.73
8ZH8	ELECTRON MICROSCOPY	3.19

Predicted structure (AlphaFold)

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

Antibody-complex structures (SAbDab): 2 — 8WZ2, 8ZH8

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): 19

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-389397	Orexin and neuropeptides FF and QRFP bind to their respective receptors
R-HSA-416476	G alpha (q) signalling events

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

Rollup of top-2 pathways:

Category	Pathways
Peptide ligand-binding receptors	1
GPCR downstream signalling	1

GO top-level categories

Rollup of top GO terms by namespace:

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

Protein interactions and networks

STRING

620 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
QRFPR	QRFP	P83859	999
QRFPR	GNAQ	P50148	801
QRFPR	GAL	P22466	757
QRFPR	NPFF	O15130	597
QRFPR	KISS1	Q15726	579
QRFPR	PRLH	P81277	507
QRFPR	NPVF	Q9HCQ7	506
QRFPR	HCRT	O43612	439
QRFPR	PRLHR	P49683	422
QRFPR	PHTF1	Q9UMS5	417
QRFPR	IGFLR1	Q9H665	405
QRFPR	NPY	P01303	381
QRFPR	TRAM1L1	Q8N609	372
QRFPR	CHIA	Q9BZP6	356
QRFPR	RPA1	P27694	355

IntAct

16 interactions, top by confidence:

A	B	Type	Score
QRFPR	NTM	psi-mi:“MI:0915”(physical association)	0.560
GJA8	QRFPR	psi-mi:“MI:0915”(physical association)	0.560
QRFPR	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
RAMP1	QRFPR	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	QRFPR	psi-mi:“MI:0915”(physical association)	0.400
QRFPR	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	QRFPR	psi-mi:“MI:0915”(physical association)	0.400
NTM	QRFPR	psi-mi:“MI:0915”(physical association)	0.000
QRFPR	GJA8	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (11): QRFPR (Two-hybrid), QRFPR (Two-hybrid), SLCO4A1 (Co-fractionation), QRFPR (Co-fractionation), QRFPR (Co-fractionation), SLC15A4 (Co-fractionation), SLC38A1 (Co-fractionation), SMCHD1 (Co-fractionation), TMED10 (Co-fractionation), TMED9 (Co-fractionation), QRFPR (Affinity Capture-MS)

ESM2 similar proteins: B0BM39, B3VSC2, D1LYT2, O14494, O42602, O42603, O62772, P08220, P0C2W5, P15431, P18505, P19019, P21548, P27681, P28472, P28473, P34998, P35347, P35353, P47866, P47870, P50571, P60588, P63079, P63080, P63137, P63138, P83858, P83861, Q06AA5, Q13324, Q15303, Q4L208, Q4R8V4, Q5ZJ75, Q60748, Q61527, Q6DCQ3, Q76LL8, Q8BJU2

Diamond homologs: A5A4K9, A5A4L1, C3ZQF9, F1MV99, G4WMX4, O02835, O02836, O08725, O42179, O43614, O54799, O62729, O62809, O70342, O77408, P0DQD5, P11617, P20288, P22270, P24053, P24628, P25929, P25931, P28336, P29274, P30731, P30938, P30975, P32251, P35346, P35371, P41143, P47211, P47751, P49146, P49219, P49285, P49288, P49683, P50391

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

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

Top pathogenic / likely-pathogenic (0)

SpliceAI

1228 predictions. Top by Δscore:

Variant	Effect	Δscore
4:121330424:A:AC	donor_gain	1.0000
4:121330425:C:CT	donor_gain	1.0000
4:121330425:CTGT:C	donor_gain	1.0000
4:121336795:A:C	donor_gain	1.0000
4:121337744:CA:C	donor_gain	1.0000
4:121340491:T:TA	donor_gain	1.0000
4:121380306:AC:A	donor_gain	1.0000
4:121380306:ACC:A	donor_gain	1.0000
4:121380306:ACCC:A	donor_gain	1.0000
4:121380306:ACCCC:A	donor_gain	1.0000
4:121380307:CC:C	donor_gain	1.0000
4:121380307:CCC:C	donor_gain	1.0000
4:121380307:CCCC:C	donor_gain	1.0000
4:121380307:CCCCC:C	donor_gain	1.0000
4:121330425:CT:C	donor_gain	0.9900
4:121330522:TCCTA:T	acceptor_loss	0.9900
4:121330523:CCTAA:C	acceptor_loss	0.9900
4:121330524:CTAAA:C	acceptor_loss	0.9900
4:121330525:T:C	acceptor_loss	0.9900
4:121330531:C:T	acceptor_gain	0.9900
4:121332913:A:AC	donor_gain	0.9900
4:121332914:C:CC	donor_gain	0.9900
4:121332915:TG:T	donor_gain	0.9900
4:121333060:C:CT	acceptor_gain	0.9900
4:121337755:T:TA	donor_gain	0.9900
4:121337775:T:A	donor_gain	0.9900
4:121340455:G:C	donor_gain	0.9900
4:121340591:CATCT:C	acceptor_gain	0.9900
4:121340608:CAC:C	acceptor_gain	0.9900
4:121340612:T:A	acceptor_loss	0.9900

AlphaMissense

2856 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
4:121333003:C:A	W205C	0.993
4:121333003:C:G	W205C	0.993
4:121336860:A:G	W170R	0.992
4:121336860:A:T	W170R	0.992
4:121330475:A:C	F282L	0.990
4:121330475:A:T	F282L	0.990
4:121330477:A:G	F282L	0.990
4:121333005:A:G	W205R	0.988
4:121333005:A:T	W205R	0.988
4:121340598:C:T	C118Y	0.988
4:121380378:A:C	S90R	0.988
4:121380378:A:T	S90R	0.988
4:121380380:T:G	S90R	0.988
4:121340598:C:G	C118S	0.986
4:121340599:A:T	C118S	0.986
4:121330465:A:G	W286R	0.983
4:121330465:A:T	W286R	0.983
4:121340532:G:T	A140D	0.983
4:121340597:G:C	C118W	0.981
4:121329648:C:T	G321E	0.980
4:121340599:A:G	C118R	0.980
4:121336850:G:T	A173E	0.978
4:121330468:A:G	C285R	0.976
4:121340522:C:A	R143S	0.976
4:121340522:C:G	R143S	0.976
4:121340539:A:G	C138R	0.976
4:121380373:A:G	L92P	0.976
4:121329618:A:T	V331D	0.975
4:121332941:G:C	P226R	0.975
4:121380315:C:A	W111C	0.975

dbSNP variants (sampled 300 via entrez): RS1000001113 (4:121340664 T>G), RS1000033658 (4:121340855 C>T), RS1000093056 (4:121357317 C>T), RS1000111907 (4:121374152 G>A), RS1000125285 (4:121332798 G>A), RS1000137551 (4:121360212 C>T), RS1000142998 (4:121374400 C>A,T), RS1000257160 (4:121356565 G>A,T), RS1000285984 (4:121377325 A>G), RS1000289755 (4:121356900 G>A), RS1000311305 (4:121329211 TGTC>T), RS1000330296 (4:121362313 A>T), RS1000414657 (4:121363331 TAATA>T,TAATAAATA), RS1000448421 (4:121344796 T>A), RS1000469395 (4:121361714 A>G)

Disease associations

OMIM: gene MIM:606925 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST002876_11	Type 1 diabetes and autoimmune thyroid diseases	4.000000e-10
GCST009391_94	Metabolite levels	2.000000e-06
GCST012053_11	Weight	5.000000e-08

EFO canonical traits (2, from GWAS)

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 (VIP=true, CPIC=false)

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)

8 measured of 9 human assays (9 total across all organisms); most potent 8 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
P550	KI	6 nM
P518	KI	7 nM
P517	KI	235 nM
P52	KI	245 nM
P513	KI	258 nM
CHEMBL1802377	EC50	588 nM
P552	KI	607 nM
P51	KI	1500 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	affects cotreatment, increases expression	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)

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