RXFP1

Summary

RXFP1 (relaxin family peptide receptor 1, HGNC:19718) is a protein-coding gene on chromosome 4q32.1, encoding Relaxin receptor 1 (Q9HBX9). Receptor for relaxins.

This gene encodes a member of the leucine-rich repeat-containing subgroup of the G protein-coupled 7-transmembrane receptor superfamily. The encoded protein plays a critical role in sperm motility, pregnancy and parturition as a receptor for the protein hormone relaxin. Decreased expression of this gene may play a role in endometriosis. Alternatively spliced transcript variants encoding multiple isoforms have been observed for this gene.

Source: NCBI Gene 59350 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 105 total
• Druggable target: yes — 11 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_021634

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:19718
Approved symbol	RXFP1
Name	relaxin family peptide receptor 1
Location	4q32.1
Locus type	gene with protein product
Status	Approved
Aliases	RXFPR1
Ensembl gene	ENSG00000171509
Ensembl biotype	protein_coding
OMIM	606654
Entrez	59350

Gene structure

Transcript identifiers

Ensembl transcripts: 16 — 12 protein_coding, 2 nonsense_mediated_decay, 2 protein_coding_CDS_not_defined

ENST00000307765, ENST00000342048, ENST00000343542, ENST00000423548, ENST00000448688, ENST00000460056, ENST00000470033, ENST00000471616, ENST00000472969, ENST00000484785, ENST00000613319, ENST00000879781, ENST00000879782, ENST00000879783, ENST00000952070, ENST00000952071

RefSeq mRNA: 8 — MANE Select: NM_021634 NM_001253727, NM_001253728, NM_001253729, NM_001253730, NM_001253732, NM_001253733, NM_001363776, NM_021634

CCDS: CCDS43276, CCDS58929, CCDS58930, CCDS75204, CCDS75205, CCDS75206, CCDS87277

Canonical transcript exons

ENST00000307765 — 18 exons

Exon	Start	End
ENSE00003459909	158617131	158617205
ENSE00003475717	158644909	158645138
ENSE00003495346	158521882	158522025
ENSE00003532276	158633405	158633476
ENSE00003538610	158612130	158612201
ENSE00003549080	158639260	158639331
ENSE00003571126	158638008	158638079
ENSE00003580955	158651757	158653372
ENSE00003591286	158646791	158647201
ENSE00003592228	158626820	158626891
ENSE00003593539	158593401	158593499
ENSE00003611000	158648499	158648717
ENSE00003645431	158628638	158628709
ENSE00003649710	158607972	158608043
ENSE00003661929	158612291	158612362
ENSE00003669750	158572698	158572835
ENSE00003721877	158599326	158599431
ENSE00003741216	158605068	158605139

Expression profiles

Bgee: expression breadth ubiquitous, 147 present calls, max score 95.84.

FANTOM5 (CAGE): breadth broad, TPM avg 1.5252 / max 289.4609, expressed in 212 samples.

FANTOM5 promoters (8 alternative TSS)

Promoter ID	TPM avg	Samples expressed
50294	0.8464	162
50295	0.3663	100
50293	0.1045	45
50292	0.0906	26
203399	0.0598	17
50289	0.0304	10
50288	0.0187	5
50290	0.0084	4

Top tissues by expression

240 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
decidua	UBERON:0002450	95.84	gold quality
endothelial cell	CL:0000115	94.98	gold quality
endometrium	UBERON:0001295	90.08	gold quality
Brodmann (1909) area 46	UBERON:0006483	88.35	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	83.71	gold quality
prefrontal cortex	UBERON:0000451	82.11	gold quality
Brodmann (1909) area 9	UBERON:0013540	81.30	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	81.10	gold quality
superior frontal gyrus	UBERON:0002661	79.91	gold quality
frontal cortex	UBERON:0001870	79.42	gold quality
Brodmann (1909) area 23	UBERON:0013554	78.87	gold quality
neocortex	UBERON:0001950	77.43	gold quality
anterior cingulate cortex	UBERON:0009835	76.68	gold quality
uterus	UBERON:0000995	76.59	gold quality
postcentral gyrus	UBERON:0002581	76.18	gold quality
right frontal lobe	UBERON:0002810	75.30	gold quality
parietal lobe	UBERON:0001872	75.29	gold quality
cerebral cortex	UBERON:0000956	74.00	gold quality
stromal cell of endometrium	CL:0002255	73.92	gold quality
right lung	UBERON:0002167	71.72	gold quality
left adrenal gland cortex	UBERON:0035825	71.61	gold quality
left adrenal gland	UBERON:0001234	71.57	gold quality
right adrenal gland cortex	UBERON:0035827	71.56	gold quality
right adrenal gland	UBERON:0001233	71.20	gold quality
adrenal cortex	UBERON:0001235	71.09	gold quality
primary visual cortex	UBERON:0002436	70.44	gold quality
adrenal gland	UBERON:0002369	70.04	gold quality
entorhinal cortex	UBERON:0002728	69.12	gold quality
upper lobe of left lung	UBERON:0008952	68.74	gold quality
lung	UBERON:0002048	68.46	gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 4.

Experiment	Marker?	Max mean expression
E-HCAD-30	yes	297.30
E-HCAD-35	yes	59.38
E-MTAB-6678	yes	9.78
E-ANND-3	yes	6.59

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

115 targeting RXFP1, 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-5011-5P	100.00	83.46	5820
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-126-5P	100.00	72.71	3180
HSA-MIR-6748-5P	100.00	65.81	1057
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-6758-5P	100.00	66.21	1470
HSA-MIR-6856-5P	100.00	65.47	1298
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-3667-3P	99.99	67.17	1636
HSA-MIR-34A-5P	99.99	71.21	1784
HSA-MIR-449A	99.99	71.05	1776
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-34C-5P	99.97	70.45	1577
HSA-MIR-449B-5P	99.97	70.26	1580
HSA-MIR-4267	99.96	66.53	2368
HSA-MIR-1468-3P	99.96	72.74	3797
HSA-MIR-302E	99.96	70.74	2669
HSA-MIR-1250-3P	99.96	70.04	4038
HSA-MIR-23A-3P	99.95	74.24	3163
HSA-MIR-23B-3P	99.95	74.24	3163
HSA-MIR-23C	99.95	73.92	3192
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-450B-5P	99.92	71.48	3175
HSA-MIR-205-3P	99.92	69.92	3165
HSA-MIR-589-3P	99.91	69.62	2088
HSA-MIR-10527-5P	99.91	72.28	3754
HSA-MIR-6809-3P	99.91	71.45	3814

Literature-anchored findings (GeneRIF, showing 40)

• capable of mediating the action of relaxin through an adenosine 3’,5’-monophosphate (cAMP)-dependent pathway (PMID:11809971)
• Gene expression pattern and protein localization of LGR7 receptor in human endometrium throughout the menstrual cycle. (PMID:14742692)
• Binding to and gene expression of the LGR7 relaxin receptor changes markedly with the phases of the menstrual cycle, suggesting a specific role for the hormone in the physiology of the human uterus. (PMID:15240635)
• Substitution of the relaxin-3 A-chain with the A-chain from insulin-like peptide 5 results in a chimeric peptide that selectively activates GPCR135 and GPCR142 over LGR7. (PMID:15465925)
• mouse and rat LGR7 share 85.2 and 85.7% identity with human LGR7 (PMID:15566402)
• Data describe the conformation of the relaxin-binding site of the leucine-rich G-protein-coupled receptor 7. (PMID:15695505)
• Relaxin receptor (LGR7) increases the transcription of IGFBP-1 and prolactin in decidual and endometrial stromal cells through the promoter region containing multiple CCAAT/enhancer-binding proteins (C/EBP) binding sites. (PMID:15722441)
• human LGR7 LDL-A module NMR studies; demonstration that calicum is required for the module to form a stable and correctly folded structure (PMID:15956684)
• increase in LGR7 expression and H2 relaxin binding in the secretory phase of the menstrual cycle suggests a specific role for relaxin after ovulation in the human uterus (PMID:15956698)
• Amino acid sequence analysis of the LGR7 C-terminal tail and intracellular loops revealed multiple putative phosphorylation sites, suggesting that signal switching from Gs to Gi may occur after receptor phosphorylation (PMID:15956719)
• LGR7.10 splice variant is expressed at the cell surface, LGR7.2 is predominantly retained within cells and LGR7.1 is partially secreted. None stimulates cAMP production. (PMID:16051677)
• Relaxin stimulates leukocyte adhesion and migration through a relaxin receptor LGR7-dependent mechanism (PMID:16303766)
• The essential role of the LDLa module in LGR7 and LGR8 function is reported. (PMID:16963451)
• Specific residues in the N-terminal region of the RXFP1 receptor low density lipoprotein receptor class A (LDLa) module play a key role in receptor activation. (PMID:17148455)
• The LDL-A module of LGR7 influences receptor maturation, cell surface expression, and relaxin-activated signal transduction. (PMID:17158203)
• The dominant-negative effects of the LGR7 splice variants expressed in the chorion and decidua could be functionally significant in the peripartal period. (PMID:18079195)
• analysis of truncated human relaxin-2 and -3 (H2 and H3) relaxin peptides and their binding and cAMP activities on RXFP1, RXFP2, and RXFP3 (PMID:18434306)
• N-glycosylation at Asn-303 of RXFP1 was required for optimal intracellular cAMP signaling (PMID:18533687)
• RXFP1 is a constitutive dimer with negative cooperativity in ligand binding, and dimerization occurs through the 7TM domain, and that the ectodomain has a stabilizing effect on this interaction. (PMID:18723073)
• Decrease in the expression of relaxin receptor in the placenta is related with the occurrence and development of preeclampsia. (PMID:18843967)
• The autocrine/paracrine actions of relaxin in the decidua are under additional controls at the level of expression of its receptor on the surface of its target cells. (PMID:19116340)
• The apparent lack of classical regulation for RXFP1 and RXFP2 provides the molecular basis for the prolonged signaling and physiological actions of relaxin and related peptides (PMID:19279230)
• Point mutations of conserved residues or complete deletion of the LDL-A module resulted in loss of the cAMP response to relaxin (PMID:19416160)
• Ligand-mediated activation of RXFP1 and RXFP2 is a complex process involving various domains of the receptors (PMID:19416161)
• Relaxin binds to RXFP2 with high affinity, although INSL3 has a very poor affinity for RXFP1 (PMID:19416162)
• Data tested the hypothesis that relaxin plays a role in endometriosis by comparing the expression of relaxin mRNA and its LGR7 (RXFP1) receptor mRNA in normal human endometrium to those in samples from patients with endometriosis. (PMID:19416175)
• The data suggest that luteal LGR7 mRNA expression may be regulated by relaxin and/or LH and that the corpus luteum is a target organ for relaxin. (PMID:19416177)
• Data show the expression of the relaxin receptor RXFP1 on the acrosome of human spermatozoa. (PMID:19416186)
• Data show that connective tissues as diverse as ligaments and basal lamina keratinocytes express RXFP1. These data lend support to our contention that relaxin affects ligament integrity and wound healing. (PMID:19416214)
• The expression of RXFP1, evaluated by quantitative reverse transcription-PCR, was downregulated in uterine fibroid tissues. (PMID:19416222)
• Data showm an accelerated progression of prostate cancer in TRAMP males with transgenic relaxin overexpression and a longer survival of TRAMP, RXFP1-deficient males. (PMID:19416223)
• These results suggest that relaxin activates PPARgamma activity and increases the overall response in the presence of PPARgamma agonists, and that this activation is dependent on the presence of RXFP1. (PMID:19712722)
• Endometrial expression of relaxin and relaxin receptor in endometriosis. (PMID:20655530)
• Uncovered is a pre-assembled, constitutively active G-protein-coupled receptor signalosome, that couples the relaxin receptor, relaxin family peptide receptor 1 (RXFP1), to cAMP following receptor stimulation with sub-picomolar concentrations of peptide. (PMID:20664520)
• LGR7 is constitutively expressed in human endometrium, and an increased LGR7 immunostaining is demonstrated in the secretory phase, confirming the involvement of relaxin in the physiology of endometrium and suggesting its role in implantation. (PMID:21324453)
• [review] The relaxin receptor RXFP1 localizes in the acrosomal region of sperm. (PMID:22180889)
• relaxin-2 and its receptors RXFP1 and RXFP2 are expressed in GSV and their expression is significantly decreased in varicose GSV (PMID:22737225)
• These results provide new mechanistic insights into the binding and activation events of RXFP1 and RXFP2 by their native hormone ligands. (PMID:22973049)
• Identification of key residues essential for the structural fold and receptor selectivity within the A-chain of human gene-2 (H2) relaxin (PMID:23024363)
• The decreased cellular expression of relaxin-2 receptor RXFP1 in scleroderma skin might represent a pro-fibrotic factor and contribute to the substantial inefficacy of relaxin treatment in systemic sclerosis, as reported in the literature. (PMID:23043266)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	rxfp1	ENSDARG00000090071
mus_musculus	Rxfp1	ENSMUSG00000034009
rattus_norvegicus	Rxfp1	ENSRNOG00000024120

Paralogs (22): IGFALS (ENSG00000099769), TLR8 (ENSG00000101916), LRRC17 (ENSG00000128606), RXFP2 (ENSG00000133105), CD180 (ENSG00000134061), TLR4 (ENSG00000136869), TLR2 (ENSG00000137462), LRRC32 (ENSG00000137507), LRRC3 (ENSG00000160233), LRRC53 (ENSG00000162621), TLR3 (ENSG00000164342), VASN (ENSG00000168140), NRROS (ENSG00000174004), TLR10 (ENSG00000174123), TLR1 (ENSG00000174125), TLR6 (ENSG00000174130), LRRC3B (ENSG00000179796), TSKU (ENSG00000182704), TLR5 (ENSG00000187554), TLR7 (ENSG00000196664), LRIT2 (ENSG00000204033), LRRC3C (ENSG00000204913)

Protein

Protein identifiers

Relaxin receptor 1 — Q9HBX9 (reviewed: Q9HBX9)

Alternative names: Leucine-rich repeat-containing G-protein coupled receptor 7, Relaxin family peptide receptor 1

All UniProt accessions (6): Q9HBX9, A0A087WWV0, A0A0A0MT52, B4DGP2, E9PCA3, E9PIF0

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for relaxins. The activity of this receptor is mediated by G proteins leading to stimulation of adenylate cyclase and an increase of cAMP. Binding of the ligand may also activate a tyrosine kinase pathway that inhibits the activity of a phosphodiesterase that degrades cAMP.

Subunit / interactions. Interacts with C1QTNF8.

Subcellular location. Cell membrane.

Tissue specificity. Expressed in the brain, kidney, testis, placenta, uterus, ovary, adrenal, prostate, skin and heart. Not detected in spleen.

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

Isoforms (5)

UniProt ID	Names	Canonical?
Q9HBX9-1	1	yes
Q9HBX9-2	2, LGR7.10
Q9HBX9-3	3, LGR7.1
Q9HBX9-4	4, LGR7.2
Q9HBX9-5	5

RefSeq proteins (8): NP_001240656, NP_001240657, NP_001240658, NP_001240659, NP_001240661, NP_001240662, NP_001350705, NP_067647* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR001611	Leu-rich_rpt	Repeat
IPR002172	LDrepeatLR_classA_rpt	Repeat
IPR003591	Leu-rich_rpt_typical-subtyp	Repeat
IPR008112	Relaxin_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain
IPR023415	LDLR_class-A_CS	Conserved_site
IPR032675	LRR_dom_sf	Homologous_superfamily
IPR036055	LDL_receptor-like_sf	Homologous_superfamily

Pfam: PF00001, PF00057, PF13855

UniProt features (73 total): helix 13, repeat 9, topological domain 8, transmembrane region 7, binding site 6, glycosylation site 6, splice variant 6, strand 5, disulfide bond 4, turn 4, domain 2, chain 1, mutagenesis site 1, sequence conflict 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
7TMW	ELECTRON MICROSCOPY	3.2
2JM4	SOLUTION NMR
2M7P	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9HBX9-F1	81.08	0.48

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

Functional residue map

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

Ligand- & substrate-binding residues (6): 45; 48; 50; 52; 58; 59

Disulfide bonds (4): 27–40, 34–53, 47–62, 485–563

Glycosylation sites (6): 36, 127, 264, 272, 325, 368

Mutagenesis-validated functional residues (1):

Position	Phenotype
637	leads to constitutive increase of basal camp.

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

ID	Pathway
R-HSA-418555	G alpha (s) signalling events
R-HSA-444821	Relaxin receptors
R-HSA-162582	Signal Transduction
R-HSA-372790	Signaling by GPCR
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-375276	Peptide ligand-binding receptors
R-HSA-388396	GPCR downstream signalling
R-HSA-500792	GPCR ligand binding

MSigDB gene sets: 104 (showing top): GSE45365_NK_CELL_VS_CD8A_DC_MCMV_INFECTION_DN, GOBP_MAMMARY_GLAND_MORPHOGENESIS, chr4q32, GOBP_GLAND_MORPHOGENESIS, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_HORMONE_MEDIATED_SIGNALING_PATHWAY, GOBP_ANIMAL_ORGAN_MORPHOGENESIS, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, SCHAEFFER_PROSTATE_DEVELOPMENT_48HR_DN, GOBP_PARTURITION, GOBP_MAMMARY_GLAND_DEVELOPMENT, GOBP_RESPONSE_TO_HORMONE, GOBP_MULTI_MULTICELLULAR_ORGANISM_PROCESS

GO Biological Process (10): adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), parturition (GO:0007567), hormone-mediated signaling pathway (GO:0009755), extracellular matrix organization (GO:0030198), myofibroblast differentiation (GO:0036446), lung connective tissue development (GO:0060427), nipple morphogenesis (GO:0060658), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-modulating G protein-coupled receptor signaling pathway (GO:0007188)

GO Molecular Function (5): G protein-coupled receptor activity (GO:0004930), G protein-coupled peptide receptor activity (GO:0008528), hormone binding (GO:0042562), metal ion binding (GO:0046872), protein binding (GO:0005515)

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

Reactome top-level categories

Rollup of top-6 pathways:

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

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
signal transduction	2
G protein-coupled receptor activity	2
G protein-coupled receptor signaling pathway	2
binding	2
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase activator activity	1
multi-organism reproductive process	1
multi-multicellular organism process	1
cellular response to hormone stimulus	1
extracellular structure organization	1
external encapsulating structure organization	1
cell differentiation	1
lung development	1
connective tissue development	1
anatomical structure morphogenesis	1
mammary gland morphogenesis	1
nipple development	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
adenylate cyclase activity	1
transmembrane signaling receptor activity	1
peptide receptor activity	1
cation binding	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1662 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
RXFP1	RLN2	P04090	998
RXFP1	INSL3	P51460	994
RXFP1	RLN3	Q8WXF3	993
RXFP1	RLN1	P04808	990
RXFP1	RXFP3	Q9NSD7	897
RXFP1	RXFP4	Q8TDU9	863
RXFP1	C1QTNF8	P60827	855
RXFP1	INSL5	Q9Y5Q6	815
RXFP1	INS	P01308	710
RXFP1	ARRB2	P32121	706
RXFP1	AKAP5	P24588	704
RXFP1	INSL6	Q9Y581	625
RXFP1	INSL4	Q14641	582
RXFP1	AGT	P01019	559
RXFP1	AGTR1	P30556	542

IntAct

15 interactions, top by confidence:

A	B	Type	Score
RLN	RXFP1	psi-mi:“MI:0915”(physical association)	0.440
RLN	RXFP1	psi-mi:“MI:0914”(association)	0.440
RXFP1	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
RXFP1	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
RXFP1	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	RXFP1	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	RXFP1	psi-mi:“MI:0915”(physical association)	0.400
AKAP5	RXFP1	psi-mi:“MI:0915”(physical association)	0.400
RXFP1	AKAP5	psi-mi:“MI:0915”(physical association)	0.400
RXFP1	UPK3BL1	psi-mi:“MI:0914”(association)	0.350
PDE4D	PRKACA	psi-mi:“MI:0914”(association)	0.350
Adcy2	PRKACA	psi-mi:“MI:0914”(association)	0.350
RXFP1	PRKACA	psi-mi:“MI:0914”(association)	0.350

BioGRID (87): RXFP1 (Biochemical Activity), C1QTNF8 (Affinity Capture-Western), RXFP1 (Affinity Capture-MS), RXFP1 (Synthetic Lethality), RXFP1 (Affinity Capture-MS), BTN2A2 (Affinity Capture-MS), PCDHGC3 (Affinity Capture-MS), ATP13A2 (Affinity Capture-MS), SYNGR2 (Affinity Capture-MS), ATP2B4 (Affinity Capture-MS), KCNT2 (Affinity Capture-MS), LRRC8D (Affinity Capture-MS), PIGN (Affinity Capture-MS), PIGQ (Affinity Capture-MS), ABHD3 (Affinity Capture-MS)

ESM2 similar proteins: A6QLU6, A8WCC4, B8JK39, F1MLX5, J3S6Y1, O94955, P07224, P07225, P13612, P51810, P57097, P59822, P70259, P98118, Q12866, Q13797, Q14246, Q28520, Q2TBA3, Q3TDN0, Q3URE9, Q5M900, Q5R5V8, Q5Y4N8, Q60805, Q61549, Q61730, Q63621, Q6F3F9, Q6NRQ1, Q6QNK2, Q6R6I6, Q6R6I7, Q7L985, Q7TT36, Q7Z443, Q80T32, Q86SQ4, Q8IWK6, Q8NFZ0

Diamond homologs: O02721, P14763, P16235, P16473, P16582, P20395, P21463, P22888, P23945, P24014, P30730, P32212, P35376, P35378, P35379, P35409, P46023, P47750, P47799, P49059, P56495, P79763, Q27987, Q28005, Q28585, Q5GJ04, Q5R5V8, Q5XM32, Q6QMG1, Q6R6I6, Q6R6I7, Q6R6L8, Q6YNB6, Q7ZTV5, Q8R428, Q8SPP9, Q8WXD0, Q90674, Q91ZZ5, Q95179

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
RLN2	up-regulates	RXFP1	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	95
Likely benign	3
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

3390 predictions. Top by Δscore:

Variant	Effect	Δscore
4:158572696:A:AG	acceptor_gain	1.0000
4:158572697:G:GG	acceptor_gain	1.0000
4:158593497:GTT:G	donor_gain	1.0000
4:158593500:G:GG	donor_gain	1.0000
4:158599265:A:AG	acceptor_gain	1.0000
4:158599266:T:G	acceptor_gain	1.0000
4:158599281:T:TA	acceptor_gain	1.0000
4:158599427:GCAAT:G	donor_gain	1.0000
4:158605137:GCT:G	donor_gain	1.0000
4:158605140:G:GG	donor_gain	1.0000
4:158612199:GCT:G	donor_gain	1.0000
4:158617130:GA:G	acceptor_gain	1.0000
4:158617202:GGCT:G	donor_gain	1.0000
4:158617203:GCT:G	donor_gain	1.0000
4:158617203:GCTG:G	donor_gain	1.0000
4:158617206:G:GG	donor_gain	1.0000
4:158628632:TTTCA:T	acceptor_loss	1.0000
4:158628633:TTCA:T	acceptor_loss	1.0000
4:158628634:TCA:T	acceptor_loss	1.0000
4:158628636:A:AG	acceptor_gain	1.0000
4:158628636:A:AT	acceptor_loss	1.0000
4:158628636:AGAGT:A	acceptor_gain	1.0000
4:158628637:G:GG	acceptor_gain	1.0000
4:158628637:GA:G	acceptor_gain	1.0000
4:158628637:GAGT:G	acceptor_gain	1.0000
4:158628637:GAGTG:G	acceptor_gain	1.0000
4:158628705:GAATT:G	donor_gain	1.0000
4:158628707:ATT:A	donor_gain	1.0000
4:158628707:ATTGT:A	donor_loss	1.0000
4:158628708:TT:T	donor_gain	1.0000

AlphaMissense

5013 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
4:158638079:T:C	L348P	0.997
4:158644958:T:A	C389S	0.997
4:158644959:G:A	C389Y	0.997
4:158644959:G:C	C389S	0.997
4:158572787:T:A	C47S	0.996
4:158572788:G:C	C47S	0.996
4:158644958:T:C	C389R	0.996
4:158572805:T:A	C53S	0.995
4:158572806:G:C	C53S	0.995
4:158644931:T:A	C380S	0.995
4:158644932:G:A	C380Y	0.995
4:158644932:G:C	C380S	0.995
4:158644960:T:G	C389W	0.995
4:158612201:T:C	L203P	0.994
4:158644933:T:G	C380W	0.994
4:158647132:T:C	C563R	0.994
4:158572748:T:A	C34S	0.993
4:158572749:G:C	C34S	0.993
4:158638075:T:C	S347P	0.993
4:158644932:G:T	C380F	0.993
4:158644950:T:A	V386D	0.993
4:158644959:G:T	C389F	0.993
4:158647134:C:G	C563W	0.993
4:158572805:T:C	C53R	0.992
4:158638070:T:A	L345H	0.992
4:158644931:T:C	C380R	0.992
4:158645030:T:A	W413R	0.992
4:158645030:T:C	W413R	0.992
4:158646898:T:A	C485S	0.992
4:158646899:G:C	C485S	0.992

dbSNP variants (sampled 300 via entrez): RS1000001207 (4:158537443 G>A,T), RS10000021 (4:158520305 G>T), RS1000069684 (4:158526931 T>A,C), RS1000076956 (4:158575838 G>A), RS1000080262 (4:158620343 T>C), RS1000084942 (4:158596281 G>T), RS1000098069 (4:158643386 A>C,T), RS1000114711 (4:158559513 T>C), RS10001153 (4:158613869 G>C), RS1000121478 (4:158527240 C>T), RS1000135368 (4:158640427 C>G), RS1000156810 (4:158588033 C>T), RS1000189720 (4:158633274 A>G), RS1000215903 (4:158650807 T>A), RS1000253205 (4:158520453 G>A)

Disease associations

OMIM: gene MIM:606654 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST001320_11	Acute lymphoblastic leukemia (childhood)	1.000000e-06
GCST008161_101	Waist circumference adjusted for body mass index	5.000000e-07

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0007789	BMI-adjusted waist circumference

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1293316 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

11 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 227,688 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1200938	METHYSERGIDE MALEATE	4	4
CHEMBL1201153	ISOETHARINE MESYLATE	4	854
CHEMBL1256958	EPINEPHRINE BITARTRATE	4	2,257
CHEMBL1619	CLADRIBINE	4	91,402
CHEMBL1711	ISOPROTERENOL HYDROCHLORIDE	4	3,608
CHEMBL628	PENTOXIFYLLINE	4	26,061
CHEMBL880	FAMCICLOVIR	4	25,925
CHEMBL956	SUPROFEN	4	32,428
CHEMBL1454946	FLUBENDAZOLE	2	4,397
CHEMBL311948	LOMIFYLLINE	2	153
CHEMBL52606	COLFORSIN	2	40,599

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Relaxin family peptide receptors

Most potent curated ligand interactions (22 total), top 22:

Ligand	Action	Affinity	Parameter
relaxin	Full agonist	10.37	pEC50
LY3540378	Agonist	10.09	pKd
R2R01	Agonist	10.0	pEC50
[33P]relaxin (human)	Full agonist	9.7	pKd
SA10SC-RLX	Agonist	9.7	pEC50
relaxin	Full agonist	9.4	pKd
europium-labelled relaxin	Agonist	9.3	pKd
A(4-24)(F23A)H2	Full agonist	9.17	pKi
relaxin	Full agonist	9.1	pKd
TamRLX	Agonist	9.06	pEC50
relaxin-1	Full agonist	8.8	pEC50
SE301	Agonist	8.24	pEC50
relaxin-3	Full agonist	8.0	pKi
compound 54	Full agonist	7.92	pEC50
pexerelgon	Agonist	7.8	pEC50
B-R13HR H2 relaxin	Antagonist	7.4	pKi
relaxin	Full agonist	7.3	pKd
ML290	Biased agonist	7.03	pEC50
A(4-24)(B7-24)H2	Full agonist	6.99	pKd
B-R13/17K H2 relaxin	Antagonist	6.29	pKi
INSL3	Full agonist	5.7	pKi
(B7-33)H2	Full agonist	5.5	pKi

ChEMBL bioactivities

673 potent at pChembl≥5 of 5384 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.80	EC50	0.016	nM	CHEMBL5194101
10.70	EC50	0.01995	nM	CHEMBL5194101
10.60	EC50	0.02512	nM	CHEMBL5194101
10.50	EC50	0.03162	nM	CHEMBL5194101
10.49	EC50	0.03236	nM	CHEMBL4754949
10.48	EC50	0.033	nM	CHEMBL5559571
10.37	EC50	0.043	nM	CHEMBL3716980
10.22	EC50	0.06	nM	CHEMBL6159987
10.00	EC50	0.1	nM	CHEMBL4745611
9.70	EC50	0.2	nM	CHEMBL4795810
9.70	EC50	0.2	nM	CHEMBL6162720
9.70	EC50	0.2	nM	CHEMBL6164332
9.68	EC50	0.21	nM	CHEMBL6145550
9.57	EC50	0.27	nM	CHEMBL6150575
9.52	EC50	0.3	nM	CHEMBL6143479
9.50	EC50	0.3162	nM	CHEMBL5559571
9.50	EC50	0.3162	nM	CHEMBL5194101
9.47	EC50	0.34	nM	CHEMBL6166757
9.42	EC50	0.38	nM	CHEMBL6134421
9.40	EC50	0.4	nM	CHEMBL4786789
9.40	EC50	0.3981	nM	CHEMBL5194101
9.38	EC50	0.42	nM	CHEMBL4754949
9.37	EC50	0.43	nM	CHEMBL6151544
9.28	EC50	0.53	nM	CHEMBL6132831
9.22	EC50	0.6	nM	CHEMBL4799907
9.22	EC50	0.6	nM	CHEMBL6170452
9.21	EC50	0.61	nM	CHEMBL6149007
9.00	EC50	1	nM	CHEMBL4797641
9.00	EC50	1	nM	CHEMBL4764326
9.00	EC50	1	nM	CHEMBL6146086
8.96	Ki	1.096	nM	CHEMBL4754949
8.89	EC50	1.28	nM	CHEMBL6151587
8.87	EC50	1.35	nM	CHEMBL6170690
8.82	EC50	1.514	nM	CHEMBL5194101
8.80	EC50	1.6	nM	CHEMBL6142439
8.78	EC50	1.66	nM	CHEMBL5559571
8.70	EC50	1.995	nM	CHEMBL5179696
8.70	EC50	2	nM	CHEMBL6190291
8.60	EC50	2.512	nM	CHEMBL5194101
8.50	EC50	3.162	nM	CHEMBL5564912
8.50	EC50	3.162	nM	CHEMBL5194101
8.49	EC50	3.2	nM	CHEMBL4752287
8.44	EC50	3.6	nM	CHEMBL4793799
8.40	EC50	3.981	nM	CHEMBL5532235
8.22	EC50	6	nM	CHEMBL6190291
8.21	EC50	6.2	nM	CHEMBL6147636
8.20	EC50	6.31	nM	CHEMBL5559754
8.20	EC50	6.31	nM	CHEMBL5558885
8.20	EC50	6.31	nM	CHEMBL5559173
8.18	EC50	6.607	nM	CHEMBL5564478

PubChem BioAssay actives

212 with measured affinity, of 562 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
(1R,6R,12S,15S,18S,21S,24S,27S,30S,33S,36S,39S,42R,50S,53S,56S,59S,62S,65S,68S,71S,74R,80S,83S,88R)-88-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]-6-[[(2S)-2-[[(2S)-6-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-68-(4-aminobutyl)-30-(3-amino-3-oxopropyl)-50-benzyl-33,39-bis[(2S)-butan-2-yl]-12,24,53,65-tetrakis(3-carbamimidamidopropyl)-15-(2-carboxyethyl)-42-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]carbamoyl]-71-[(1R)-1-hydroxyethyl]-62-(hydroxymethyl)-83-(1H-imidazol-5-ylmethyl)-27,36,56-trimethyl-18,59-bis(2-methylpropyl)-7,10,13,16,19,22,25,28,31,34,37,40,49,52,55,58,61,64,67,70,73,76,79,82,85,87-hexacosaoxo-21,80-di(propan-2-yl)-3,4,44,45,90,93-hexathia-8,11,14,17,20,23,26,29,32,35,38,41,48,51,54,57,60,63,66,69,72,75,78,81,84,86-hexacosazabicyclo[72.11.9]tetranonacontane-47-carboxylic acid	1731608: Agonist activity at human RXFP1 expressed in human HEK-293T cells co-transfected with pCRE beta-galactosidase reporter plasmid assessed as inhibition of IBMX-induced cAMP accumulation incubated for 30 mins by HTRF assay	ec50	<0.0001	uM
4-[2-fluoro-4-methoxy-5-[[(1S,2R,3S,4R)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	2082529: Agonist activity at human RXFP1 expressed in HEK293 cells assessed as modulation of relaxin H2 stimulated cAMP production by measuring relaxin H2 EC50 after 15 mins by BRET sensor assay	ec50	<0.0001	uM
4-[2-fluoro-4-methoxy-5-[[(1S,2R,3S,4R)-3-[[3-(trifluoromethylsulfonyl)phenyl]carbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	1886984: Modulation of human RXFP1 stably expressed in T-REx-CHO-K1 cells assessed as stimulation of cAMP production measured after 45 mins by d2-dye labelled cAMP based HTRF assay	ec50	<0.0001	uM
4-[2-fluoro-5-[[(1R,2R,3S,4S)-3-[[4-fluoro-3-(pentafluoro-lambda6-sulfanyl)phenyl]carbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]-4-methoxyphenoxy]-1-methylcyclohexane-1-carboxylic acid	1886984: Modulation of human RXFP1 stably expressed in T-REx-CHO-K1 cells assessed as stimulation of cAMP production measured after 45 mins by d2-dye labelled cAMP based HTRF assay	ec50	<0.0001	uM
4-[2-fluoro-4-methoxy-5-[[(1R,2R,3S,4S)-3-[[3-(trifluoromethylsulfonyl)phenyl]carbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-(hydroxymethyl)cyclohexane-1-carboxylic acid	1886984: Modulation of human RXFP1 stably expressed in T-REx-CHO-K1 cells assessed as stimulation of cAMP production measured after 45 mins by d2-dye labelled cAMP based HTRF assay	ec50	<0.0001	uM
4-[2-fluoro-4-methoxy-5-[[(1R,2R,3S,4S)-3-[[3-(trifluoromethylsulfonyl)phenyl]carbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	1886984: Modulation of human RXFP1 stably expressed in T-REx-CHO-K1 cells assessed as stimulation of cAMP production measured after 45 mins by d2-dye labelled cAMP based HTRF assay	ec50	<0.0001	uM
4-[2-fluoro-5-[[(1S,2R,3S,4R)-3-[[4-fluoro-3-(pentafluoro-lambda6-sulfanyl)phenyl]carbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]-4-methoxyphenoxy]-1-methylcyclohexane-1-carboxylic acid	1886984: Modulation of human RXFP1 stably expressed in T-REx-CHO-K1 cells assessed as stimulation of cAMP production measured after 45 mins by d2-dye labelled cAMP based HTRF assay	ec50	<0.0001	uM
4-[2-fluoro-5-[[(1S,2R)-2-[[4-fluoro-3-(pentafluoro-lambda6-sulfanyl)phenyl]carbamoyl]cyclobutyl]carbamoyl]-4-methoxyphenoxy]-1-methylcyclohexane-1-carboxylic acid	1886984: Modulation of human RXFP1 stably expressed in T-REx-CHO-K1 cells assessed as stimulation of cAMP production measured after 45 mins by d2-dye labelled cAMP based HTRF assay	ec50	<0.0001	uM
2-[(2-propan-2-yloxybenzoyl)amino]-N-[3-(trifluoromethylsulfonyl)phenyl]benzamide	2082529: Agonist activity at human RXFP1 expressed in HEK293 cells assessed as modulation of relaxin H2 stimulated cAMP production by measuring relaxin H2 EC50 after 15 mins by BRET sensor assay	ec50	<0.0001	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[2-[2-[[2-[2-[2-[[2-[2-[2-[[(2S)-7-acetamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-7-acetamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-3-[[(2S)-3-[[(2S,3S)-2-[[(2S)-7-acetamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-6-aminohexanoyl]amino]heptanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-4-methylsulfanylbutanoyl]amino]hexanoyl]amino]-6-aminohexanoyl]amino]heptanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-2-methylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-6-aminohexanoyl]amino]-6-aminohexanoyl]amino]heptanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]amino]-6-aminohexanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-5-oxotricosanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0001	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-7-acetamido-1-[[(2S,3S)-1-[[(2S)-3-[[(2S)-3-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-7-acetamido-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-7-acetamido-1-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(4S)-1-amino-1,5-dioxodocosan-4-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-oxoheptan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxoheptan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-2-methyl-3-oxopropyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxoheptan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0002	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[2-[3-[2-[2-[3-[[2-[2-[3-[2-[2-[3-[[2-[2-[3-[2-[2-[3-[[(2S)-7-acetamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-7-acetamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-3-[[(2S)-3-[[(2S,3S)-2-[[(2S)-7-acetamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-6-aminohexanoyl]amino]heptanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-4-methylsulfanylbutanoyl]amino]hexanoyl]amino]-6-aminohexanoyl]amino]heptanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-2-methylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-6-aminohexanoyl]amino]-6-aminohexanoyl]amino]heptanoyl]amino]propoxy]ethoxy]ethoxy]propylamino]-2-oxoethoxy]acetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-2-oxoethoxy]acetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-2-oxoethoxy]acetyl]amino]-6-aminohexanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-5-oxotricosanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0004	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-7-acetamido-1-[[(2S,3S)-1-[[(2S)-3-[[(2S)-3-[[(2S)-1-[[(2S)-7-acetamido-1-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(4S)-1-amino-1,5-dioxotricosan-4-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethylamino]-1-oxoheptan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-2-methyl-3-oxopropyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxoheptan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0006	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-7-acetamido-1-[[(2S,3S)-1-[[(2S)-3-[[(2S)-3-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-7-acetamido-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-7-acetamido-1-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(4S)-1-amino-1,5-dioxohenicosan-4-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-oxoheptan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxoheptan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-2-methyl-3-oxopropyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxoheptan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0010	uM
(4S)-4-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[[(2S)-3-[[(2S)-3-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-6-amino-1-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(4S)-1-amino-1,5-dioxodocosan-4-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethylamino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-2-methyl-3-oxopropyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0010	uM
(4S)-4-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[[(2S)-3-[[(2S)-3-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-6-amino-1-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(4S)-1-amino-1,5-dioxoicosan-4-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethylamino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-2-methyl-3-oxopropyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0032	uM
4-[2-fluoro-5-[[(1R,2S)-2-[[4-fluoro-3-(pentafluoro-lambda6-sulfanyl)phenyl]carbamoyl]cyclopentyl]carbamoyl]-4-methoxyphenoxy]-1-methylcyclohexane-1-carboxylic acid	2082387: Agonist activity at human RXFP1 expressed in T-Rex-CHO-K1 cells assessed as stimulation of cAMP production incubated for 45 mins by HTRF assay	ec50	0.0032	uM
(4S)-4-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[[(2S)-3-[[(2S)-3-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-6-amino-1-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(4S)-1-amino-1,5-dioxohenicosan-4-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethylamino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-2-methyl-3-oxopropyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0036	uM
4-[4-(difluoromethoxy)-2-fluoro-5-[[(1S,2R,3S,4R)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0040	uM
4-[2-fluoro-4-(fluoromethoxy)-5-[[(1S,2R,3S,4R)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0063	uM
4-[2-cyano-4-methoxy-5-[[(1S,2R,3S,4R)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0063	uM
4-[2-chloro-4-methoxy-5-[[(1R,2R,3S,4S)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0063	uM
4-[2-fluoro-4-methoxy-5-[[(1S,2R,3S,4R)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-(trifluoromethyl)cyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0066	uM
4-[2-chloro-4-methoxy-5-[[(1S,2R,3S,4R)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0079	uM
(4S)-4-[[(2S)-3-[[(2S)-3-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-5-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0120	uM
4-[2-fluoro-4-methoxy-5-[[(1S,2R,3S,4R)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-(hydroxymethyl)cyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0126	uM
(4S)-4-[[(2S)-3-[[(2S)-3-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-5-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0140	uM
(4S)-4-[[(2S)-3-[[(2S)-3-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0140	uM
4-[2-fluoro-5-[[(1R,2R,3S,4S)-3-[[4-fluoro-3-(trifluoromethyl)phenyl]carbamoyl]-2-bicyclo[2.2.1]hept-5-enyl]carbamoyl]-4-methoxyphenoxy]cyclohexane-1-carboxylic acid	2082387: Agonist activity at human RXFP1 expressed in T-Rex-CHO-K1 cells assessed as stimulation of cAMP production incubated for 45 mins by HTRF assay	ec50	0.0158	uM
4-[2-fluoro-5-[[(1R,2R,3S,4S)-3-[[4-fluoro-3-(trifluoromethylsulfonyl)phenyl]carbamoyl]-2-bicyclo[2.2.1]hept-5-enyl]carbamoyl]-4-methoxyphenoxy]cyclohexane-1-carboxylic acid	2082387: Agonist activity at human RXFP1 expressed in T-Rex-CHO-K1 cells assessed as stimulation of cAMP production incubated for 45 mins by HTRF assay	ec50	0.0158	uM
4-[2-cyano-4-fluoro-5-[[(2R,3S)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0158	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[3-[[3-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-4-methylsulfanylbutanoyl]amino]-3-hydroxypropanoyl]amino]-6-aminohexanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-2-methylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-6-aminohexanoyl]amino]-6-aminohexanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0170	uM
(4S)-4-[[(2S)-3-[[(2S)-3-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0170	uM
(4S)-4-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[[(2S)-3-[[(2S)-3-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(4S)-1-amino-1,5-dioxohenicosan-4-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-2-methyl-3-oxopropyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0176	uM
(4S)-4-acetamido-5-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[[(2S)-3-[[(2S)-3-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-2-methyl-3-oxopropyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0178	uM
(4S)-4-[[(2S)-3-[[(2S)-3-[[(2S,3S)-2-[[(2S)-7-acetamido-2-[[(2S)-3-[[(2S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-6-aminohexanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]heptanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-5-[[2-[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-7-acetamido-1-amino-1-oxoheptan-2-yl]amino]-5-amino-1-oxopentan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]oxy-2-oxoethyl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0180	uM
(4S)-4-[[(2S)-3-[[(2S)-3-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0195	uM
(4S)-4-[[(2S)-3-[[(2S)-3-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-5-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0230	uM
4-[2-cyano-5-[[(1S,2R,3S,4R)-3-(2,2-dimethylpropylcarbamoyl)-2-bicyclo[2.2.1]heptanyl]carbamoyl]-4-methoxyphenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0251	uM
4-[2-cyano-5-[[(1S,2R,3S,4R)-3-[(3-fluoro-1-bicyclo[1.1.1]pentanyl)carbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]-4-methoxyphenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0251	uM
4-[2-(difluoromethyl)-4-methoxy-5-[[(1S,2R,3S,4R)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0251	uM
4-[2-fluoro-4-methoxy-5-[[(1R,2S,4S)-4-methoxy-2-[[3-(trifluoromethylsulfonyl)phenyl]carbamoyl]cyclopentyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	2082387: Agonist activity at human RXFP1 expressed in T-Rex-CHO-K1 cells assessed as stimulation of cAMP production incubated for 45 mins by HTRF assay	ec50	0.0251	uM
(1R,2S,3R,4S)-3-[[4-fluoro-2-methoxy-5-[4-methyl-4-(2H-tetrazol-5-yl)cyclohexyl]oxybenzoyl]amino]-N-[(1-methylcyclobutyl)methyl]bicyclo[2.2.1]heptane-2-carboxamide	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0316	uM
4-[5-[[(1S,2R,3S,4R)-3-[[(2R)-3,3-dimethylbutan-2-yl]carbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]-2-fluoro-4-methoxyphenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0316	uM
4-[2-fluoro-4-methoxy-5-[[(1S,2R,3S,4R)-3-[(3,3,3-trifluoro-2,2-dimethylpropyl)carbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0316	uM
4-[4-methoxy-5-[[(1S,2R,3S,4R)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]-2-(trifluoromethyl)phenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0316	uM
(4S)-5-[[2-[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-3-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-7-acetamido-1-amino-1-oxoheptan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]oxy-2-oxoethyl]amino]-4-[[(2S)-3-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0320	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-3-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-2-methylpropanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-4-methylsulfanylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-6-aminohexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-6-aminohexanoyl]amino]-6-aminohexanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0320	uM
(4S)-4-acetamido-5-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[[(2S)-3-[[(2S)-3-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-methyl-3-oxopropyl]amino]-2-methyl-3-oxopropyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	1731590: Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay	ec50	0.0370	uM
4-[5-[[(1S,2R,3S,4R)-3-(2,2-dimethylpropylcarbamoyl)-2-bicyclo[2.2.1]heptanyl]carbamoyl]-2-fluoro-4-methoxyphenoxy]-1-methylcyclohexane-1-carboxylic acid	2082450: Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP level measured after 2 hrs by HTRF cAMP assay	ec50	0.0398	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	decreases expression, increases methylation	2
sulforaphane	decreases expression	1
sodium arsenite	decreases expression	1
terbutylazine	decreases reaction, decreases expression, affects binding	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression, decreases expression	1
propazine	affects binding, decreases reaction, decreases expression	1
Grape Seed Proanthocyanidins	affects cotreatment, increases expression	1
Zoledronic Acid	increases expression	1
Atrazine	affects binding, decreases reaction, decreases expression	1
Catechin	affects cotreatment, increases expression	1
Estradiol	decreases expression, affects cotreatment	1
Lipopolysaccharides	increases expression, affects response to substance	1
Oxygen	increases expression	1
Progesterone	affects cotreatment, decreases expression	1
Simazine	affects binding, decreases reaction, decreases expression	1
Okadaic Acid	decreases expression	1

ChEMBL screening assays

82 unique, capped per target: 75 functional, 7 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1613930	Functional	PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1. (Class of assay: confirmatory)	PubChem BioAssay data set
CHEMBL2034746	Binding	Displacement of europium-labelled H2 relaxin from RXFP1 expressed in HEK-293T cells	Minimization of human relaxin-3 leading to high-affinity analogues with increased selectivity for relaxin-family peptide 3 receptor (RXFP3) over RXFP1. — J Med Chem

Cellosaurus cell lines

1 cell lines: 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_KV76	cAMP Hunter CHO-K1 RXFP1 Gs	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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