RXFP4
gene geneOn this page
Also known as GPCR142RXFPR4
Summary
RXFP4 (relaxin family peptide/INSL5 receptor 4, HGNC:14666) is a protein-coding gene on chromosome 1q22, encoding Relaxin-3 receptor 2 (Q8TDU9). High affinity receptor for INSL5.
GPR100 is a member of the rhodopsin family of G protein-coupled receptors (GPRs) (Fredriksson et al., 2003 [PubMed 14623098]).
Source: NCBI Gene 339403 — RefSeq curated summary.
At a glance
- GWAS associations: 19
- Clinical variants (ClinVar): 75 total
- Druggable target: yes
- MANE Select transcript:
NM_181885
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:14666 |
| Approved symbol | RXFP4 |
| Name | relaxin family peptide/INSL5 receptor 4 |
| Location | 1q22 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | GPCR142, RXFPR4 |
| Ensembl gene | ENSG00000173080 |
| Ensembl biotype | protein_coding |
| OMIM | 609043 |
| Entrez | 339403 |
Gene structure
Transcript identifiers
Ensembl transcripts: 1 — 1 protein_coding
ENST00000368318
RefSeq mRNA: 1 — MANE Select: NM_181885
NM_181885
CCDS: CCDS1124
Canonical transcript exons
ENST00000368318 — 1 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001446861 | 155941638 | 155943087 |
Expression profiles
Bgee: expression breadth broad, 43 present calls, max score 74.99.
Top tissues by expression
92 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| mucosa of transverse colon | UBERON:0004991 | 74.99 | gold quality |
| sural nerve | UBERON:0015488 | 72.18 | gold quality |
| rectum | UBERON:0001052 | 65.22 | gold quality |
| granulocyte | CL:0000094 | 65.01 | gold quality |
| duodenum | UBERON:0002114 | 63.94 | gold quality |
| bone marrow cell | CL:0002092 | 62.19 | gold quality |
| monocyte | CL:0000576 | 61.96 | gold quality |
| leukocyte | CL:0000738 | 61.61 | gold quality |
| transverse colon | UBERON:0001157 | 61.47 | gold quality |
| bone marrow | UBERON:0002371 | 56.78 | gold quality |
| small intestine | UBERON:0002108 | 54.09 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 53.94 | gold quality |
| colonic epithelium | UBERON:0000397 | 52.06 | gold quality |
| intestine | UBERON:0000160 | 51.35 | gold quality |
| colon | UBERON:0001155 | 50.35 | gold quality |
| blood | UBERON:0000178 | 46.26 | silver quality |
| vermiform appendix | UBERON:0001154 | 45.95 | gold quality |
| mucosa of stomach | UBERON:0001199 | 44.02 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 42.22 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 41.39 | silver quality |
| cerebellum | UBERON:0002037 | 41.23 | gold quality |
| cerebellar cortex | UBERON:0002129 | 41.09 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 41.09 | gold quality |
| left uterine tube | UBERON:0001303 | 40.87 | gold quality |
| right coronary artery | UBERON:0001625 | 40.49 | silver quality |
| apex of heart | UBERON:0002098 | 38.34 | silver quality |
| cortex of kidney | UBERON:0001225 | 37.16 | silver quality |
| gall bladder | UBERON:0002110 | 36.95 | silver quality |
| thoracic aorta | UBERON:0001515 | 36.74 | silver quality |
| primary visual cortex | UBERON:0002436 | 36.61 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 0.86 |
Regulation
Is transcription factor: no
Literature-anchored findings (GeneRIF, showing 14)
- relaxin-3/INSL7 is a ligand for GPCR142 [GPCR142] (PMID:14522967)
- 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. (PMID:15465925)
- INSL5 is an endogenous ligand for GPCR142 (PMID:15525639)
- the N-terminus and EL2 domains of RXFP3 and RXFP4 are involved in ligand binding while TM2, 3, and 5 are critical for receptor activation. (PMID:18582868)
- Mutant relaxin-3 shows a significant decrease in receptor-activation potency towards RXFP4. (PMID:24802387)
- electrostatic interactions between INSL5 and RXFP4 (PMID:25043977)
- The C-terminus of the B-chain of human INSL5 is critical for cognate RXFP4 receptor activity. (PMID:26661035)
- The role of these four INSL5 determinants in distinguishing RXFP4 from RXFP3. (PMID:27404393)
- Relaxin-3 is a high-efficacy agonist at RXFP4 with a comparable signal transduction profile to INSL5. (PMID:27888281)
- analysis of the interaction mechanism of INSL5 with its receptor RXFP4 (PMID:28274616)
- The results confirmed the presence of RXFP4 in human spermatozoa, which localized in the neck and midpiece of sperm. (PMID:28986276)
- present work shed new light on the interaction mechanism of RXFP3 and RXFP4 with agonists and antagonists, and also provided a novel approach for interaction studies of some plasma membrane receptors with their ligands. (PMID:30684458)
- Expression of the relaxin family peptide 4 receptor by enterochromaffin cells of the mouse large intestine. (PMID:35596811)
- Ligand recognition mechanism of the human relaxin family peptide receptor 4 (RXFP4). (PMID:36717591)
Cross-species orthologs
2 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Rxfp4 | ENSMUSG00000049741 |
| caenorhabditis_elegans | WBGENE00015559 |
Paralogs (7): BDKRB1 (ENSG00000100739), APLNR (ENSG00000134817), AGTR1 (ENSG00000144891), GPR15 (ENSG00000154165), BDKRB2 (ENSG00000168398), GPR25 (ENSG00000170128), AGTR2 (ENSG00000180772)
Protein
Protein identifiers
Relaxin-3 receptor 2 — Q8TDU9 (reviewed: Q8TDU9)
Alternative names: G-protein coupled receptor 100, G-protein coupled receptor GPCR142, Insulin-like peptide INSL5 receptor, Relaxin family peptide receptor 4
All UniProt accessions (1): Q8TDU9
UniProt curated annotations — full annotation on UniProt →
Function. High affinity receptor for INSL5. Also acts as a receptor for RLN3/relaxin-3, as well as bradykinin and kallidin. Binding of the ligand inhibit cAMP accumulation.
Subcellular location. Cell membrane.
Tissue specificity. Expressed in a broader range of tissues including brain, kidney, testis, thymus, placenta, prostate, salivary gland, thyroid and colon.
Similarity. Belongs to the G-protein coupled receptor 1 family.
RefSeq proteins (1): NP_871001* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000248 | ATII_rcpt | Family |
| IPR000276 | GPCR_Rhodpsn | Family |
| IPR017452 | GPCR_Rhodpsn_7TM | Domain |
| IPR050119 | CCR1-9-like | Family |
Pfam: PF00001
UniProt features (37 total): helix 13, topological domain 8, transmembrane region 7, glycosylation site 2, strand 2, turn 2, chain 1, disulfide bond 1, sequence variant 1
Structure
Experimental structures (PDB)
4 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 7YK7 | ELECTRON MICROSCOPY | 2.75 |
| 9KFK | ELECTRON MICROSCOPY | 2.95 |
| 7YK6 | ELECTRON MICROSCOPY | 3.03 |
| 7YJ4 | ELECTRON MICROSCOPY | 3.19 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q8TDU9-F1 | 81.63 | 0.51 |
Antibody-complex structures (SAbDab): 4 — 7YJ4, 7YK6, 7YK7, 9KFK
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Disulfide bonds (1): 114–191
Glycosylation sites (2): 5, 17
Function
Pathways and Gene Ontology
Reactome pathways
2 pathways
| ID | Pathway |
|---|---|
| R-HSA-418594 | G alpha (i) signalling events |
| R-HSA-444821 | Relaxin receptors |
MSigDB gene sets: 39 (showing top):
GOBP_BEHAVIOR, GOBP_POSITIVE_REGULATION_OF_BEHAVIOR, TGACCTY_ERR1_Q2, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_REGULATION_OF_BEHAVIOR, GOBP_REGULATION_OF_FEEDING_BEHAVIOR, chr1q22, GOMF_PEPTIDE_RECEPTOR_ACTIVITY, RGAGGAARY_PU1_Q6, GOBP_POSITIVE_REGULATION_OF_MULTICELLULAR_ORGANISMAL_PROCESS, GOBP_FEEDING_BEHAVIOR, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GSE13762_CTRL_VS_125_VITAMIND_DAY12_DC_DN, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY
GO Biological Process (4): neuropeptide signaling pathway (GO:0007218), positive regulation of feeding behavior (GO:2000253), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186)
GO Molecular Function (3): galanin receptor activity (GO:0004966), G protein-coupled receptor activity (GO:0004930), 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 |
|---|---|
| GPCR downstream signalling | 1 |
| Peptide ligand-binding receptors | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| G protein-coupled receptor signaling pathway | 2 |
| feeding behavior | 1 |
| positive regulation of behavior | 1 |
| regulation of feeding behavior | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| G protein-coupled receptor activity | 1 |
| signal transduction | 1 |
| neuropeptide receptor activity | 1 |
| transmembrane signaling receptor activity | 1 |
| binding | 1 |
| membrane | 1 |
| cell periphery | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
434 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| RXFP4 | RLN3 | Q8WXF3 | 993 |
| RXFP4 | INSL5 | Q9Y5Q6 | 953 |
| RXFP4 | RXFP1 | Q9HBX9 | 863 |
| RXFP4 | RLN2 | P04090 | 834 |
| RXFP4 | RLN1 | P04808 | 821 |
| RXFP4 | RXFP2 | Q8WXD0 | 817 |
| RXFP4 | INSL3 | P51460 | 744 |
| RXFP4 | RHO | P08100 | 697 |
| RXFP4 | INSL6 | Q9Y581 | 639 |
| RXFP4 | INSL4 | Q14641 | 599 |
| RXFP4 | SYCN | Q0VAF6 | 523 |
| RXFP4 | KNG1 | P01042 | 498 |
| RXFP4 | ACP4 | Q9BZG2 | 458 |
| RXFP4 | GPR142 | Q7Z601 | 456 |
| RXFP4 | KLK8 | O60259 | 456 |
IntAct
22 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| GJA8 | RXFP4 | psi-mi:“MI:0915”(physical association) | 0.560 |
| RXFP4 | SC5D | psi-mi:“MI:0914”(association) | 0.530 |
| RLN3 | RXFP4 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RXFP4 | RLN3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| GAPDH | RXFP4 | psi-mi:“MI:0915”(physical association) | 0.370 |
| TTI1 | RXFP4 | psi-mi:“MI:0915”(physical association) | 0.370 |
| MAGED1 | RXFP4 | psi-mi:“MI:0915”(physical association) | 0.370 |
| QDPR | RXFP4 | psi-mi:“MI:0915”(physical association) | 0.370 |
| TTC4 | RXFP4 | psi-mi:“MI:0915”(physical association) | 0.370 |
| TSPAN3 | RXFP4 | psi-mi:“MI:0915”(physical association) | 0.370 |
| ACTR10 | RXFP4 | psi-mi:“MI:0915”(physical association) | 0.370 |
| RXFP4 | GJA8 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (13): RMND1 (Affinity Capture-MS), SC5D (Affinity Capture-MS), RLN3 (Reconstituted Complex), RXFP4 (Two-hybrid), GAPDH (Two-hybrid), TTI1 (Two-hybrid), MAGED1 (Two-hybrid), QDPR (Two-hybrid), TTC4 (Two-hybrid), TSPAN3 (Two-hybrid), ACTR10 (Two-hybrid), RMND1 (Affinity Capture-MS), SC5D (Affinity Capture-MS)
ESM2 similar proteins: A0A6I8PUB9, O00155, O00270, O14842, O14843, O15529, O43603, O46685, O60755, O88626, O88634, O88853, O88854, O88855, P0C5I1, P46092, P46093, P50132, Q149R9, Q15722, Q15743, Q1JQB3, Q3T181, Q3UFD7, Q3ZC80, Q4KLH9, Q6XKD3, Q76JU8, Q76JU9, Q76JV1, Q86VZ1, Q8BUD0, Q8BYC4, Q8HYC3, Q8K3T4, Q8TDS5, Q8TDU9, Q920E0, Q924U0, Q96G91
Diamond homologs: A0T2N3, F1MV99, O00155, O08707, O08858, O09027, O18982, O35210, O35811, O54689, O77590, O88410, O88634, O97571, O97663, O97666, P0C5I1, P21109, P25024, P25025, P25095, P25104, P29089, P29754, P29755, P30555, P30556, P30937, P30938, P31391, P32248, P32302, P32303, P32745, P33396, P34976, P34997, P35343, P35344, P35346
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
75 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 70 |
| Likely benign | 5 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
183 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 1:155942112:C:G | donor_gain | 0.9800 |
| 1:155942134:T:TA | donor_gain | 0.9800 |
| 1:155942135:G:GA | donor_gain | 0.9800 |
| 1:155942159:C:T | donor_gain | 0.9500 |
| 1:155942226:ACG:A | donor_gain | 0.9500 |
| 1:155942138:G:GA | donor_gain | 0.8200 |
| 1:155942109:GCGC:G | donor_gain | 0.7800 |
| 1:155942202:GT:G | donor_gain | 0.7300 |
| 1:155941898:ACTG:A | donor_gain | 0.7200 |
| 1:155942136:G:GG | donor_gain | 0.6900 |
| 1:155942227:C:G | donor_gain | 0.6600 |
| 1:155942221:T:A | donor_gain | 0.6400 |
| 1:155942111:GC:G | donor_gain | 0.6300 |
| 1:155942199:G:GT | donor_gain | 0.6100 |
| 1:155942224:TG:T | donor_gain | 0.6100 |
| 1:155942225:GAC:G | donor_gain | 0.6100 |
| 1:155942112:C:CG | donor_gain | 0.5900 |
| 1:155942201:A:AG | donor_gain | 0.5900 |
| 1:155941895:GGTAC:G | donor_gain | 0.5800 |
| 1:155941896:GTAC:G | donor_gain | 0.5700 |
| 1:155941897:TACT:T | donor_gain | 0.5700 |
| 1:155942260:AG:A | donor_gain | 0.5300 |
| 1:155942261:GG:G | donor_gain | 0.5300 |
| 1:155942265:T:A | donor_gain | 0.4900 |
| 1:155942484:T:A | acceptor_gain | 0.4900 |
| 1:155942038:G:GT | donor_gain | 0.4800 |
| 1:155942281:G:GA | acceptor_gain | 0.4800 |
| 1:155941834:T:TA | donor_gain | 0.4700 |
| 1:155942437:T:TA | donor_gain | 0.4600 |
| 1:155941779:C:G | donor_gain | 0.4300 |
AlphaMissense
2368 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 1:155942292:T:C | F195L | 0.955 |
| 1:155942294:C:A | F195L | 0.955 |
| 1:155942294:C:G | F195L | 0.955 |
| 1:155942115:A:C | S136R | 0.934 |
| 1:155942117:C:A | S136R | 0.934 |
| 1:155942117:C:G | S136R | 0.934 |
| 1:155942346:T:C | F213L | 0.930 |
| 1:155942348:C:A | F213L | 0.930 |
| 1:155942348:C:G | F213L | 0.930 |
| 1:155942030:G:C | W107C | 0.908 |
| 1:155942030:G:T | W107C | 0.908 |
| 1:155942091:A:C | S128R | 0.908 |
| 1:155942093:C:A | S128R | 0.908 |
| 1:155942093:C:G | S128R | 0.908 |
| 1:155942244:T:C | F179L | 0.905 |
| 1:155942246:C:A | F179L | 0.905 |
| 1:155942246:C:G | F179L | 0.905 |
| 1:155942293:T:G | F195C | 0.905 |
| 1:155942472:T:C | F255L | 0.901 |
| 1:155942474:C:A | F255L | 0.901 |
| 1:155942474:C:G | F255L | 0.901 |
| 1:155942034:T:C | F109L | 0.896 |
| 1:155942036:C:A | F109L | 0.896 |
| 1:155942036:C:G | F109L | 0.896 |
| 1:155942613:A:C | S302R | 0.882 |
| 1:155942615:C:A | S302R | 0.882 |
| 1:155942615:C:G | S302R | 0.882 |
| 1:155941944:T:C | F79L | 0.876 |
| 1:155941946:C:A | F79L | 0.876 |
| 1:155941946:C:G | F79L | 0.876 |
dbSNP variants (sampled 300 via entrez): RS1000470577 (1:155940078 A>G), RS1001300618 (1:155941509 A>G), RS1001755193 (1:155941447 C>T), RS1002102979 (1:155940894 G>T), RS1004078269 (1:155943130 G>A), RS1005036062 (1:155942317 C>A,G,T), RS1006130046 (1:155940699 G>A), RS1008272911 (1:155941781 G>A,C), RS1010451239 (1:155940579 T>A), RS1010503657 (1:155940853 G>A), RS1011249439 (1:155939933 C>T), RS1012688259 (1:155943068 A>G), RS1013332669 (1:155941551 C>G,T), RS1015058361 (1:155942338 T>G), RS1015274681 (1:155943159 G>C)
Disease associations
OMIM: gene MIM:609043 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
19 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST004131_70 | Inflammatory bowel disease | 6.000000e-08 |
| GCST004132_44 | Crohn’s disease | 2.000000e-07 |
| GCST007294_124 | Body fat distribution (trunk fat ratio) | 8.000000e-35 |
| GCST007294_3 | Body fat distribution (trunk fat ratio) | 6.000000e-21 |
| GCST007294_50 | Body fat distribution (trunk fat ratio) | 1.000000e-15 |
| GCST007295_17 | Body fat distribution (leg fat ratio) | 3.000000e-13 |
| GCST007295_37 | Body fat distribution (leg fat ratio) | 7.000000e-17 |
| GCST007295_72 | Body fat distribution (leg fat ratio) | 1.000000e-28 |
| GCST010696_19 | Cortical thickness (min-P) | 2.000000e-10 |
| GCST010697_10 | Cortical surface area (min-P) | 3.000000e-10 |
| GCST010698_59 | Subcortical volume (min-P) | 9.000000e-10 |
| GCST010699_20 | Brain morphology (min-P) | 7.000000e-10 |
| GCST010700_5 | Cortical thickness (MOSTest) | 8.000000e-17 |
| GCST010701_66 | Cortical surface area (MOSTest) | 1.000000e-09 |
| GCST010702_43 | Subcortical volume (MOSTest) | 3.000000e-10 |
| GCST010703_253 | Brain morphology (MOSTest) | 4.000000e-14 |
| GCST012226_579 | Waist circumference adjusted for body mass index | 5.000000e-08 |
| GCST90020024_608 | A body shape index | 1.000000e-08 |
| GCST90020029_1229 | Waist circumference adjusted for body mass index | 2.000000e-09 |
EFO canonical traits (4, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004341 | body fat distribution |
| EFO:0004346 | neuroimaging measurement |
| EFO:0004840 | cortical thickness |
| EFO:0007789 | BMI-adjusted waist circumference |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL1628473 (SINGLE PROTEIN), CHEMBL4523612 (PROTEIN FAMILY)
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 (31 total), top 25:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| R3/I5 | Agonist | 10.5 | pIC50 |
| [125I]relaxin-3 (human) | Full agonist | 9.7 | pKd |
| relaxin-3 | Full agonist | 9.7 | pEC50 |
| INSL5 | Full agonist | 9.4 | pEC50 |
| A13:B7-24-GG | Agonist | 8.93 | pEC50 |
| [125I]relaxin-3-B/INSL5 A chimera | Agonist | 8.9 | pKd |
| compound 4 [PMID: 30824200] | Agonist | 8.8 | pEC50 |
| R3(BΔ23-27)R/I5 chimeric peptide | Antagonist | 8.64 | pIC50 |
| [125I]INSL5 (human) | Full agonist | 8.6 | pKd |
| compound 10d [PMID: 34855388] | Agonist | 8.57 | pEC50 |
| INSL5-A13nRbW | Antagonist | 8.37 | pKi |
| ΔR3/I5 | Agonist | 8.3 | pKi |
| europium-labelled relaxin-3-B/INSL5 A chimera | Agonist | 8.3 | pKd |
| europium-labelled mouse INSL5 | Agonist | 8.3 | pKd |
| europium-labelled INSL5 | 8.3 | pKd | |
| analogue 13: B7-24 | Agonist | 8.1 | pIC50 |
| INSL5 | Full agonist | 7.7 | pEC50 |
| hINSL5: A8-21 (T15K) | Agonist | 7.53 | pKi |
| INSL5 analogue 13 | Agonist | 7.5 | pKi |
| hINSL5: A8-21 (T9R) | Full agonist | 7.5 | pKi |
| INSL5-A13NR | Antagonist | 7.4 | pIC50 |
| compound 7a [PMID: 33730669] | Agonist | 7.3 | pEC50 |
| minimised relaxin-3 analogue 2 | Full agonist | 7.1 | pKi |
| relaxin-3 (B chain) | Partial agonist | 7.0 | pEC50 |
| DC591053 | Agonist | 6.95 | pKi |
ChEMBL bioactivities
125 potent at pChembl≥5 of 127 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.46 | EC50 | 0.3467 | nM | CHEMBL4760798 |
| 9.46 | EC50 | 0.35 | nM | CHEMBL4760798 |
| 9.29 | EC50 | 0.5129 | nM | CHEMBL4798311 |
| 9.29 | EC50 | 0.51 | nM | CHEMBL4798311 |
| 9.10 | EC50 | 0.8 | nM | CHEMBL4522365 |
| 9.05 | EC50 | 0.9 | nM | CHEMBL5094669 |
| 8.96 | EC50 | 1.1 | nM | CHEMBL5084331 |
| 8.93 | EC50 | 1.175 | nM | CHEMBL6148631 |
| 8.93 | EC50 | 1.17 | nM | CHEMBL6148631 |
| 8.88 | Ki | 1.318 | nM | CHEMBL6148111 |
| 8.88 | Ki | 1.32 | nM | CHEMBL6148111 |
| 8.80 | Ki | 1.585 | nM | CHEMBL4798311 |
| 8.80 | Ki | 1.58 | nM | CHEMBL4798311 |
| 8.78 | EC50 | 1.66 | nM | CHEMBL6132956 |
| 8.74 | EC50 | 1.8 | nM | CHEMBL5081158 |
| 8.70 | EC50 | 2 | nM | CHEMBL4522365 |
| 8.64 | Ki | 2.291 | nM | CHEMBL6148631 |
| 8.64 | Ki | 2.29 | nM | CHEMBL6148631 |
| 8.57 | EC50 | 2.7 | nM | CHEMBL5089949 |
| 8.56 | EC50 | 2.754 | nM | CHEMBL4779813 |
| 8.56 | EC50 | 2.75 | nM | CHEMBL4779813 |
| 8.51 | Ki | 3.09 | nM | CHEMBL6103355 |
| 8.47 | EC50 | 3.4 | nM | CHEMBL5072593 |
| 8.46 | IC50 | 3.467 | nM | CHEMBL2030702 |
| 8.46 | Ki | 3.467 | nM | CHEMBL6148405 |
| 8.46 | Ki | 3.47 | nM | CHEMBL6148405 |
| 8.40 | EC50 | 4 | nM | CHEMBL4470544 |
| 8.40 | EC50 | 4 | nM | CHEMBL5083969 |
| 8.34 | EC50 | 4.571 | nM | CHEMBL4752265 |
| 8.34 | EC50 | 4.57 | nM | CHEMBL4752265 |
| 8.33 | Ki | 4.677 | nM | CHEMBL6132956 |
| 8.33 | Ki | 4.68 | nM | CHEMBL6132956 |
| 8.26 | Ki | 5.495 | nM | CHEMBL4760798 |
| 8.26 | Ki | 5.5 | nM | CHEMBL4760798 |
| 8.16 | EC50 | 6.918 | nM | CHEMBL4761849 |
| 8.15 | EC50 | 7.079 | nM | CHEMBL4781389 |
| 8.11 | Ki | 7.762 | nM | CHEMBL6103273 |
| 8.11 | Ki | 7.76 | nM | CHEMBL6103273 |
| 8.11 | EC50 | 7.762 | nM | CHEMBL6148324 |
| 8.11 | EC50 | 7.76 | nM | CHEMBL6148324 |
| 8.10 | IC50 | 7.943 | nM | CHEMBL2030701 |
| 8.10 | EC50 | 7.943 | nM | CHEMBL4747872 |
| 8.10 | EC50 | 7.943 | nM | CHEMBL6103273 |
| 8.10 | EC50 | 7.94 | nM | CHEMBL6103273 |
| 8.08 | EC50 | 8.318 | nM | CHEMBL4754473 |
| 8.08 | EC50 | 8.318 | nM | CHEMBL6149303 |
| 8.08 | EC50 | 8.32 | nM | CHEMBL6149303 |
| 8.06 | Ki | 8.71 | nM | CHEMBL6149303 |
| 8.04 | EC50 | 9.12 | nM | CHEMBL6148111 |
| 8.04 | EC50 | 9.12 | nM | CHEMBL6103355 |
PubChem BioAssay actives
84 with measured affinity, of 125 total; 43 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,47R,50S,53S,56S,59S,62S,65S,68S,71S,74R,80S,83S,88R)-88-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-65-(4-aminobutyl)-21,33,39-tris[(2S)-butan-2-yl]-6-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-carboxy-2-[[(2S)-2,6-diaminohexanoyl]amino]butanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-42-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-24,83-bis(3-carbamimidamidopropyl)-15,62,80-tris(2-carboxyethyl)-27,53-bis[(1R)-1-hydroxyethyl]-56,71-bis(hydroxymethyl)-18,36-bis[(4-hydroxyphenyl)methyl]-12,50,59-tris(2-methylpropyl)-68-(2-methylsulfanylethyl)-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-30-propan-2-yl-3,4,44,45,90,91-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[72.11.7]dononacontane-47-carboxylic acid | 1711582: Agonist activity at human RXFP4 expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production by pCRE beta-galactosidase reporter assay | ec50 | 0.0003 | uM |
| (1R,6R,12S,15S,18S,21S,24S,27S,30S,33S,36R,39S,42R,47R,50S,53S,56S,59S,62S,65S,68S,71S,74R,80S,83S,88R)-6-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-88-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-65-(4-aminobutyl)-33,39-bis[(2S)-butan-2-yl]-42-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-24,83-bis(3-carbamimidamidopropyl)-62,80-bis(2-carboxyethyl)-15-(carboxymethyl)-27,53-bis[(1R)-1-hydroxyethyl]-56,71-bis(hydroxymethyl)-18,36-bis[(4-hydroxyphenyl)methyl]-12,50,59-tris(2-methylpropyl)-68-(2-methylsulfanylethyl)-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-21,30-di(propan-2-yl)-3,4,44,45,90,91-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[72.11.7]dononacontane-47-carboxylic acid | 1711582: Agonist activity at human RXFP4 expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production by pCRE beta-galactosidase reporter assay | ec50 | 0.0005 | uM |
| 2-[2-(4-chlorophenyl)ethyl]-1-[(E)-(7-ethyl-5-hydroxy-1H-indol-3-yl)methylideneamino]guanidine | 1811604: Agonist activity at human RXFP4 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay | ec50 | 0.0008 | uM |
| 1-[(E)-(5-cyano-7-ethyl-1H-indol-3-yl)methylideneamino]-2-(2-pyridin-3-ylethyl)guanidine | 1811604: Agonist activity at human RXFP4 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay | ec50 | 0.0009 | uM |
| 1-[(E)-(7-ethyl-5-methoxy-1H-indol-3-yl)methylideneamino]-2-(2-pyridin-3-ylethyl)guanidine | 1811604: Agonist activity at human RXFP4 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay | ec50 | 0.0011 | uM |
| 2-[2-(4-cyanophenyl)ethyl]-1-[(E)-(7-ethyl-5-methoxy-1H-indol-3-yl)methylideneamino]guanidine | 1811604: Agonist activity at human RXFP4 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay | ec50 | 0.0018 | uM |
| (1R,6R,12S,15S,18S,21S,24S,27S,30S,33S,36S,39S,42S,47S,50R,53R,56R,59R,62R,65R,68R,71R,74S,80S,83S,88R)-6-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-88-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-3-carboxy-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-33,39-bis[(2S)-butan-2-yl]-42-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-24-(3-carbamimidamidopropyl)-15,62,80-tris(carboxymethyl)-27,83-bis[(1R)-1-hydroxyethyl]-65-[(1S)-1-hydroxyethyl]-56,71-bis(hydroxymethyl)-18,36-bis[(4-hydroxyphenyl)methyl]-53-methyl-12,50,59-tris(2-methylpropyl)-68-(2-methylsulfanylethyl)-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-21,30-di(propan-2-yl)-3,4,44,45,90,91-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[72.11.7]dononacontane-47-carboxylic acid | 1711582: Agonist activity at human RXFP4 expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production by pCRE beta-galactosidase reporter assay | ec50 | 0.0027 | uM |
| methyl 4-[2-[[amino-[(2E)-2-[(5-cyano-7-methyl-1H-indol-3-yl)methylidene]hydrazinyl]methylidene]amino]ethyl]benzoate | 1811604: Agonist activity at human RXFP4 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay | ec50 | 0.0027 | uM |
| methyl 4-[2-[[amino-[(2E)-2-[(5-methoxy-7-methyl-1H-indol-3-yl)methylidene]hydrazinyl]methylidene]amino]ethyl]benzoate | 1811604: Agonist activity at human RXFP4 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay | ec50 | 0.0034 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43,48-diamino-25,40-bis(4-aminobutyl)-60,78-dibenzyl-16,63,75-tris[(2S)-butan-2-yl]-84-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]carbamoyl]-54,66-bis(3-carbamimidamidopropyl)-19,57-bis(2-carboxyethyl)-81-[(1R)-1-hydroxyethyl]-10,13,22,28-tetrakis(hydroxymethyl)-37-(1H-indol-3-ylmethyl)-31,69-dimethyl-7-(2-methylpropyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-72-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 661333: Agonist activity at RXFP4 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs by beta galactosidase reporter gene assay | ic50 | 0.0035 | uM |
| 2-[2-(3,4-dichlorophenyl)ethyl]-1-[(E)-(5-hydroxy-7-methyl-1H-indol-3-yl)methylideneamino]guanidine | 1603006: Agonist activity at human RXFP4 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assay | ec50 | 0.0040 | uM |
| 1-[(E)-(7-ethyl-5-methoxy-1H-indol-3-yl)methylideneamino]-2-[2-(4-fluorophenyl)ethyl]guanidine | 1811604: Agonist activity at human RXFP4 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay | ec50 | 0.0040 | uM |
| (1R,6R,12S,15S,18S,21S,24S,27S,30S,33S,36S,39S,42R,47R,50S,53S,56S,59S,62S,65S,68S,71S,74R,80S,83S,88R)-88-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-3-carboxy-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-21,33,39-tris[(2S)-butan-2-yl]-6-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-carboxy-2-[[(2S)-2,6-diaminohexanoyl]amino]butanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-42-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-24-(3-carbamimidamidopropyl)-15,80-bis(2-carboxyethyl)-62-(carboxymethyl)-27,65,83-tris[(1R)-1-hydroxyethyl]-56,71-bis(hydroxymethyl)-18,36-bis[(4-hydroxyphenyl)methyl]-53-methyl-12,50,59-tris(2-methylpropyl)-68-(2-methylsulfanylethyl)-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-30-propan-2-yl-3,4,44,45,90,91-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[72.11.7]dononacontane-47-carboxylic acid | 1711582: Agonist activity at human RXFP4 expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production by pCRE beta-galactosidase reporter assay | ec50 | 0.0046 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,51S,54S,57S,60S,63S,66S,69S,72S,75S,81R)-43-amino-25,40-bis(4-aminobutyl)-54,69-dibenzyl-16,57,66-tris[(2S)-butan-2-yl]-81-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]pentanoyl]amino]propanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-3-methylbutanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-48-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]carbamoyl]-63,75-bis(3-carbamimidamidopropyl)-19,72-bis(2-carboxyethyl)-51-[(1R)-1-hydroxyethyl]-10,13,22,28-tetrakis(hydroxymethyl)-37-(1H-indol-3-ylmethyl)-31-methyl-7-(2-methylpropyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,50,53,56,59,62,65,68,71,74,77,80-tetracosaoxo-60-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,49,52,55,58,61,64,67,70,73,76,79-tetracosazacyclodooctacontane-4-carboxylic acid | 1726175: Agonist activity at RXFP4 (unknown origin) stably expressed in CHO cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay | ec50 | 0.0069 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,51S,54S,57S,60S,63S,66S,69S,72S,75S,81R)-81-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-amino-3-oxopropoxy]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-43-amino-25,40-bis(4-aminobutyl)-54,69-dibenzyl-16,57,66-tris[(2S)-butan-2-yl]-48-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]carbamoyl]-63,75-bis(3-carbamimidamidopropyl)-19,72-bis(2-carboxyethyl)-51-[(1R)-1-hydroxyethyl]-10,13,22,28-tetrakis(hydroxymethyl)-37-(1H-indol-3-ylmethyl)-31-methyl-7-(2-methylpropyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,50,53,56,59,62,65,68,71,74,77,80-tetracosaoxo-60-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,49,52,55,58,61,64,67,70,73,76,79-tetracosazacyclodooctacontane-4-carboxylic acid | 1726175: Agonist activity at RXFP4 (unknown origin) stably expressed in CHO cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay | ec50 | 0.0071 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43-amino-22-(4-aminobutyl)-63,75,81-tris[(2S)-butan-2-yl]-48-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-carboxy-2-[[(2S)-2,6-diaminohexanoyl]amino]butanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-84-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-66-(3-carbamimidamidopropyl)-57-(2-carboxyethyl)-19,37-bis(carboxymethyl)-40,69-bis[(1R)-1-hydroxyethyl]-13,28-bis(hydroxymethyl)-60,78-bis[(4-hydroxyphenyl)methyl]-10,31-dimethyl-7,16,54-tris(2-methylpropyl)-25-(2-methylsulfanylethyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-72-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 1678659: Agonist activity at human RXFP4 transfected in CHO-K1 cells co-transfected with pCRE-beta-galactosidase reporter plasmid assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay | ec50 | 0.0079 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43-amino-25,40-bis(4-aminobutyl)-48-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-60,78-dibenzyl-16,63,75-tris[(2S)-butan-2-yl]-84-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]carbamoyl]-54,66-bis(3-carbamimidamidopropyl)-19,57-bis(2-carboxyethyl)-81-[(1R)-1-hydroxyethyl]-10,13,22,28-tetrakis(hydroxymethyl)-37-(1H-indol-3-ylmethyl)-31,69-dimethyl-7-(2-methylpropyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-72-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 661333: Agonist activity at RXFP4 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs by beta galactosidase reporter gene assay | ic50 | 0.0079 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43,48-diamino-22-(4-aminobutyl)-63,75,81-tris[(2S)-butan-2-yl]-84-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-66-(3-carbamimidamidopropyl)-57-(2-carboxyethyl)-19,37-bis(carboxymethyl)-40,69-bis[(1R)-1-hydroxyethyl]-13,28-bis(hydroxymethyl)-60,78-bis[(4-hydroxyphenyl)methyl]-10,31-dimethyl-7,16,54-tris(2-methylpropyl)-25-(2-methylsulfanylethyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-72-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 1678659: Agonist activity at human RXFP4 transfected in CHO-K1 cells co-transfected with pCRE-beta-galactosidase reporter plasmid assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay | ec50 | 0.0083 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43-amino-22-(4-aminobutyl)-48-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-63,75,81-tris[(2S)-butan-2-yl]-84-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-66-(3-carbamimidamidopropyl)-57-(2-carboxyethyl)-19,37-bis(carboxymethyl)-40,69-bis[(1R)-1-hydroxyethyl]-13,28-bis(hydroxymethyl)-60,78-bis[(4-hydroxyphenyl)methyl]-10,31-dimethyl-7,16,54-tris(2-methylpropyl)-25-(2-methylsulfanylethyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-72-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 1678659: Agonist activity at human RXFP4 transfected in CHO-K1 cells co-transfected with pCRE-beta-galactosidase reporter plasmid assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay | ec50 | 0.0110 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43-amino-22-(4-aminobutyl)-48-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-63,75,81-tris[(2S)-butan-2-yl]-84-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-66-(3-carbamimidamidopropyl)-57-(2-carboxyethyl)-19,37-bis(carboxymethyl)-40,69-bis[(1R)-1-hydroxyethyl]-13,28-bis(hydroxymethyl)-60,78-bis[(4-hydroxyphenyl)methyl]-10,31-dimethyl-7,16,54-tris(2-methylpropyl)-25-(2-methylsulfanylethyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-72-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 1678659: Agonist activity at human RXFP4 transfected in CHO-K1 cells co-transfected with pCRE-beta-galactosidase reporter plasmid assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay | ec50 | 0.0141 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43-amino-48-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-25,40-bis(4-aminobutyl)-60,78-dibenzyl-16,63,75-tris[(2S)-butan-2-yl]-84-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]carbamoyl]-54,66-bis(3-carbamimidamidopropyl)-19,57-bis(2-carboxyethyl)-81-[(1R)-1-hydroxyethyl]-10,13,22,28-tetrakis(hydroxymethyl)-37-(1H-indol-3-ylmethyl)-31,69-dimethyl-7-(2-methylpropyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-72-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 661333: Agonist activity at RXFP4 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs by beta galactosidase reporter gene assay | ic50 | 0.0141 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,51S,54S,57S,60S,63S,66S,69S,72S,75S,81R)-43-amino-25,40-bis(4-aminobutyl)-81-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-54,69-dibenzyl-16,57,66-tris[(2S)-butan-2-yl]-48-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]carbamoyl]-63,75-bis(3-carbamimidamidopropyl)-19,72-bis(2-carboxyethyl)-51-[(1R)-1-hydroxyethyl]-10,13,22,28-tetrakis(hydroxymethyl)-37-(1H-indol-3-ylmethyl)-31-methyl-7-(2-methylpropyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,50,53,56,59,62,65,68,71,74,77,80-tetracosaoxo-60-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,49,52,55,58,61,64,67,70,73,76,79-tetracosazacyclodooctacontane-4-carboxylic acid | 1726175: Agonist activity at RXFP4 (unknown origin) stably expressed in CHO cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay | ec50 | 0.0144 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43-amino-22-(4-aminobutyl)-63,75,81-tris[(2S)-butan-2-yl]-48-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-carboxy-2-[[(2S)-2,6-diaminohexanoyl]amino]butanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-84-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-40,66-bis(3-carbamimidamidopropyl)-19,37,57-tris(2-carboxyethyl)-10,69-bis[(1R)-1-hydroxyethyl]-13,28-bis(hydroxymethyl)-60,78-bis[(4-hydroxyphenyl)methyl]-31-methyl-7,16,54-tris(2-methylpropyl)-25-(2-methylsulfanylethyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-72-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 1711582: Agonist activity at human RXFP4 expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production by pCRE beta-galactosidase reporter assay | ec50 | 0.0151 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43-amino-48-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-22-(4-aminobutyl)-75,81-bis[(2S)-butan-2-yl]-84-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-40,66-bis(3-carbamimidamidopropyl)-19,37-bis(2-carboxyethyl)-57-(carboxymethyl)-10,69-bis[(1R)-1-hydroxyethyl]-13,28-bis(hydroxymethyl)-60,78-bis[(4-hydroxyphenyl)methyl]-31-methyl-7,16,54-tris(2-methylpropyl)-25-(2-methylsulfanylethyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-63,72-di(propan-2-yl)-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 1711581: Displacement of europium-labeled Eu(A)-mINSL5 from human RXFP4 expressed in CHO-K1 cells | ki | 0.0186 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,51S,54S,57S,60S,63S,66S,69S,72S,75S,81R)-43-amino-25,40-bis(4-aminobutyl)-54,69-dibenzyl-16,57,66-tris[(2S)-butan-2-yl]-81-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-1-carbamoyloxy-3-(1H-indol-3-yl)propan-2-yl]amino]pentanoyl]amino]propanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-3-methylbutanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-48-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]carbamoyl]-63,75-bis(3-carbamimidamidopropyl)-19,72-bis(2-carboxyethyl)-51-[(1R)-1-hydroxyethyl]-10,13,22,28-tetrakis(hydroxymethyl)-37-(1H-indol-3-ylmethyl)-31-methyl-7-(2-methylpropyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,50,53,56,59,62,65,68,71,74,77,80-tetracosaoxo-60-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,49,52,55,58,61,64,67,70,73,76,79-tetracosazacyclodooctacontane-4-carboxylic acid | 1726175: Agonist activity at RXFP4 (unknown origin) stably expressed in CHO cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay | ec50 | 0.0195 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43-amino-22-(4-aminobutyl)-63,75,81-tris[(2S)-butan-2-yl]-48-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-carboxy-2-[[(2S)-2,6-diaminohexanoyl]amino]butanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-84-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-40,66-bis(3-carbamimidamidopropyl)-57-(2-carboxyethyl)-19,37-bis(carboxymethyl)-69-[(1R)-1-hydroxyethyl]-13,28-bis(hydroxymethyl)-60,78-bis[(4-hydroxyphenyl)methyl]-10,31-dimethyl-7,16,54-tris(2-methylpropyl)-25-(2-methylsulfanylethyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-72-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 1711581: Displacement of europium-labeled Eu(A)-mINSL5 from human RXFP4 expressed in CHO-K1 cells | ki | 0.0234 | uM |
| 2-[2-(3,4-dichlorophenyl)ethyl]-1-[(E)-(5-methoxy-7-methyl-1H-indol-3-yl)methylideneamino]guanidine | 1603006: Agonist activity at human RXFP4 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assay | ec50 | 0.0580 | uM |
| 2-[2-(4-chlorophenyl)ethyl]-1-[(E)-(5-methoxy-7-methyl-1H-indol-3-yl)methylideneamino]guanidine | 1603006: Agonist activity at human RXFP4 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assay | ec50 | 0.1000 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43-amino-63,75,81-tris[(2S)-butan-2-yl]-48-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-carboxy-2-[[(2S)-2,6-diaminohexanoyl]amino]butanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-84-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-66-(3-carbamimidamidopropyl)-57-(2-carboxyethyl)-19,37-bis(carboxymethyl)-22,40,69-tris[(1R)-1-hydroxyethyl]-13,28-bis(hydroxymethyl)-60,78-bis[(4-hydroxyphenyl)methyl]-10,31-dimethyl-7,16,54-tris(2-methylpropyl)-25-(2-methylsulfanylethyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-72-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 1711582: Agonist activity at human RXFP4 expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production by pCRE beta-galactosidase reporter assay | ec50 | 0.1000 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,5S,8S,11S,15E,20S)-20-[[(2S)-2-[[2-[[(2S)-2-acetamido-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-2-benzyl-5-[(2S)-butan-2-yl]-8-(3-carbamimidamidopropyl)-11,20-dimethyl-3,6,9,21-tetraoxo-1,4,7,10-tetrazacyclohenicos-15-ene-11-carbonyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid | 1632041: Agonist activity at human RXFP4 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay | ec50 | 0.1122 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,5S,8S,11S,15E,20S)-20-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-2-benzyl-5-[(2S)-butan-2-yl]-8-(3-carbamimidamidopropyl)-11,20-dimethyl-3,6,9,21-tetraoxo-1,4,7,10-tetrazacyclohenicos-15-ene-11-carbonyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid | 1632041: Agonist activity at human RXFP4 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay | ec50 | 0.1202 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,5S,8S,11S,15E,20S)-20-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-2-benzyl-5-[(2S)-butan-2-yl]-8-(3-carbamimidamidopropyl)-11,20-dimethyl-3,6,9,21-tetraoxo-1,4,7,10-tetrazacyclohenicos-15-ene-11-carbonyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid | 1632041: Agonist activity at human RXFP4 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay | ec50 | 0.1230 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,5S,8S,11S,15E,20S)-20-[[(2S)-2-[[2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-2-benzyl-5-[(2S)-butan-2-yl]-8-(3-carbamimidamidopropyl)-11,20-dimethyl-3,6,9,21-tetraoxo-1,4,7,10-tetrazacyclohenicos-15-ene-11-carbonyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid | 1632041: Agonist activity at human RXFP4 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay | ec50 | 0.1905 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,5S,8S,11S,15E,20S)-20-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-2-benzyl-5-[(2S)-butan-2-yl]-8-(3-carbamimidamidopropyl)-11,20-dimethyl-3,6,9,21-tetraoxo-1,4,7,10-tetrazacyclohenicos-15-ene-11-carbonyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid | 1632040: Displacement of Eu-INSL5 from human RXFP4 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay | ki | 0.2754 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,51S,54S,57S,60S,63S,66S,69S,72S,75S,81R)-43-amino-25,40-bis(4-aminobutyl)-54,69-dibenzyl-16,57,66-tris[(2S)-butan-2-yl]-81-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-1-hydroxy-3-(1H-indol-3-yl)propan-2-yl]amino]pentanoyl]amino]propanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-3-methylbutanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-48-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]carbamoyl]-63,75-bis(3-carbamimidamidopropyl)-19,72-bis(2-carboxyethyl)-51-[(1R)-1-hydroxyethyl]-10,13,22,28-tetrakis(hydroxymethyl)-37-(1H-indol-3-ylmethyl)-31-methyl-7-(2-methylpropyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,50,53,56,59,62,65,68,71,74,77,80-tetracosaoxo-60-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,49,52,55,58,61,64,67,70,73,76,79-tetracosazacyclodooctacontane-4-carboxylic acid | 1726175: Agonist activity at RXFP4 (unknown origin) stably expressed in CHO cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay | ec50 | 0.2818 | uM |
| (4S)-4-[[(2S)-2-[[2-[[(2S)-2-acetamido-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-5-[[(2S)-1-[[(3S,6S,9S,12S,16Z,21S)-21-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]-9-(3-carbamimidamidopropyl)-6,12,21-trimethyl-2,5,8,11-tetraoxo-3-propan-2-yl-1,4,7,10-tetrazacyclohenicos-16-en-12-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-oxopentanoic acid | 1632041: Agonist activity at human RXFP4 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay | ec50 | 0.5012 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,5S,8S,11S,20S)-20-[[(2S)-2-[[2-[[(2S)-2-acetamido-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-2-benzyl-5-[(2S)-butan-2-yl]-8-(3-carbamimidamidopropyl)-3,6,9,17,21-pentaoxo-1,4,7,10,16-pentazacyclohenicosane-11-carbonyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid | 1632041: Agonist activity at human RXFP4 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay | ec50 | 0.5370 | uM |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,37S,40S,43R,48R,54S,57S,60S,63S,66S,69S,72S,75S,78S,81S,84R)-43-amino-63,75,81-tris[(2S)-butan-2-yl]-48-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-carboxy-2-[[(2S)-2,6-diaminohexanoyl]amino]butanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-84-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-40,66-bis(3-carbamimidamidopropyl)-57-(2-carboxyethyl)-19,37-bis(carboxymethyl)-22,69-bis[(1R)-1-hydroxyethyl]-13,28-bis(hydroxymethyl)-60,78-bis[(4-hydroxyphenyl)methyl]-10,31-dimethyl-7,16,54-tris(2-methylpropyl)-25-(2-methylsulfanylethyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,49,52,55,58,61,64,67,70,73,76,79,82-pentacosaoxo-72-propan-2-yl-1,2,45,46-tetrathia-5,8,11,14,17,20,23,26,29,32,35,38,41,50,53,56,59,62,65,68,71,74,77,80,83-pentacosazacyclopentaoctacontane-4-carboxylic acid | 1711582: Agonist activity at human RXFP4 expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production by pCRE beta-galactosidase reporter assay | ec50 | 0.6026 | uM |
| (4S)-4-[[(2S)-2-[[2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]propanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-3-sulfanylpropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-5-[[(2S)-1-[[(2S,3S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2R)-1-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-oxopentanoic acid | 1632041: Agonist activity at human RXFP4 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay | ec50 | 1.6982 | uM |
| (4S)-4-[[(2S)-2-[[2-[[(2S)-2-acetamido-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-5-[[(2S)-1-[[(2S,3S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-oxopentanoic acid | 1632041: Agonist activity at human RXFP4 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay | ec50 | 2.6915 | uM |
| (4S)-4-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-5-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(3S,6S,9S,12S,16Z,21S)-3-benzyl-6-[(2S)-butan-2-yl]-21-[[(2S)-1-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]-12,21-dimethyl-2,5,8,11-tetraoxo-9-propan-2-yl-1,4,7,10-tetrazacyclohenicos-16-en-12-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-oxopentanoic acid | 1632041: Agonist activity at human RXFP4 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay | ec50 | 2.7542 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(5S,8S,11S,14S,17S)-17-[[(2S)-2-[[2-[[(2S)-2-acetamido-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-14-benzyl-11-[(2S)-butan-2-yl]-8-(3-carbamimidamidopropyl)-7,10,13,16-tetraoxo-1,2-dithia-6,9,12,15-tetrazacyclononadecane-5-carbonyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid | 1632041: Agonist activity at human RXFP4 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay | ec50 | 3.7153 | uM |
| (4S)-4-[[(2S)-2-[[2-[[(2S)-2-acetamido-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-5-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[2-[[2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-oxopentanoic acid | 1632041: Agonist activity at human RXFP4 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay | ec50 | 5.8884 | uM |
CTD chemical–gene interactions
11 total (human), top 11 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| sotorasib | affects cotreatment, decreases expression | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | decreases expression | 1 |
| jinfukang | affects cotreatment, decreases expression | 1 |
| trametinib | affects cotreatment, decreases expression | 1 |
| NVP-BKM120 | affects cotreatment, decreases expression | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Benzo(a)pyrene | affects methylation | 1 |
| Cisplatin | decreases expression, affects cotreatment | 1 |
| Diethylhexyl Phthalate | decreases expression | 1 |
| Plant Extracts | affects cotreatment, decreases expression | 1 |
| Valproic Acid | increases methylation | 1 |
ChEMBL screening assays
32 unique, capped per target: 20 functional, 12 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL2034649 | Functional | Agonist activity at RXFP4 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs by beta galactosidase reporter gene assay | 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 |
| CHEMBL2034744 | Binding | Displacement of europium-labelled mouse INSL-5 from RXFP4 expressed in CHO-K1 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
2 cell lines: 2 spontaneously immortalized cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_KV79 | cAMP Hunter CHO-K1 RXFP4 Gi | Spontaneously immortalized cell line | Female |
| CVCL_KZ07 | PathHunter CHO-K1 RXFP4 beta-arrestin | Spontaneously immortalized cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.