NMUR2
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Summary
NMUR2 (neuromedin U receptor 2, HGNC:16454) is a protein-coding gene on chromosome 5q33.1, encoding Neuromedin-U receptor 2 (Q9GZQ4). Receptor for the neuromedin-U and neuromedin-S neuropeptides.
This gene encodes a protein from the G-protein coupled receptor 1 family. This protein is a receptor for neuromedin U, which is a neuropeptide that is widely distributed in the gut and central nervous system. This receptor plays an important role in the regulation of food intake and body weight.
Source: NCBI Gene 56923 — RefSeq curated summary.
At a glance
- GWAS associations: 27
- Clinical variants (ClinVar): 63 total
- Druggable target: yes — 1 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_020167
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:16454 |
| Approved symbol | NMUR2 |
| Name | neuromedin U receptor 2 |
| Location | 5q33.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000132911 |
| Ensembl biotype | protein_coding |
| OMIM | 605108 |
| Entrez | 56923 |
Gene structure
Transcript identifiers
Ensembl transcripts: 3 — 2 protein_coding, 1 protein_coding_CDS_not_defined
ENST00000255262, ENST00000518933, ENST00000916655
RefSeq mRNA: 1 — MANE Select: NM_020167
NM_020167
CCDS: CCDS4321
Canonical transcript exons
ENST00000255262 — 4 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000767902 | 152395459 | 152395584 |
| ENSE00001021222 | 152391546 | 152392501 |
| ENSE00001021223 | 152404388 | 152405279 |
| ENSE00003468312 | 152398060 | 152398144 |
Expression profiles
Bgee: expression breadth broad, 85 present calls, max score 82.48.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.1031 / max 15.2250, expressed in 36 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 64445 | 0.0539 | 19 |
| 64446 | 0.0492 | 21 |
Top tissues by expression
226 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| tibialis anterior | UBERON:0001385 | 82.48 | silver quality |
| pancreatic ductal cell | CL:0002079 | 78.52 | silver quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 78.23 | gold quality |
| ileal mucosa | UBERON:0000331 | 78.10 | silver quality |
| oocyte | CL:0000023 | 64.98 | gold quality |
| deltoid | UBERON:0001476 | 63.25 | silver quality |
| corpus callosum | UBERON:0002336 | 62.09 | gold quality |
| upper leg skin | UBERON:0004262 | 57.64 | gold quality |
| endothelial cell | CL:0000115 | 57.01 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 56.90 | gold quality |
| myocardium | UBERON:0002349 | 56.26 | gold quality |
| C1 segment of cervical spinal cord | UBERON:0006469 | 56.23 | gold quality |
| spinal cord | UBERON:0002240 | 54.76 | gold quality |
| medial globus pallidus | UBERON:0002477 | 54.60 | silver quality |
| cardiac muscle of right atrium | UBERON:0003379 | 54.34 | gold quality |
| left ventricle myocardium | UBERON:0006566 | 54.23 | gold quality |
| kidney epithelium | UBERON:0004819 | 53.93 | gold quality |
| upper arm skin | UBERON:0004263 | 53.52 | gold quality |
| right testis | UBERON:0004534 | 52.47 | gold quality |
| quadriceps femoris | UBERON:0001377 | 52.42 | gold quality |
| right lung | UBERON:0002167 | 51.44 | gold quality |
| hypothalamus | UBERON:0001898 | 50.77 | gold quality |
| sperm | CL:0000019 | 50.74 | gold quality |
| left testis | UBERON:0004533 | 50.34 | gold quality |
| testis | UBERON:0000473 | 50.14 | gold quality |
| vastus lateralis | UBERON:0001379 | 49.88 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 48.65 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 47.96 | gold quality |
| Brodmann (1909) area 46 | UBERON:0006483 | 47.86 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 47.71 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 3.90 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
57 targeting NMUR2, 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-3064-3P | 100.00 | 70.09 | 1254 |
| HSA-MIR-4692 | 100.00 | 67.32 | 2066 |
| HSA-MIR-450A-1-3P | 100.00 | 69.33 | 1837 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-454-3P | 99.91 | 74.01 | 1925 |
| HSA-MIR-106A-5P | 99.90 | 73.94 | 2683 |
| HSA-MIR-374A-5P | 99.90 | 71.34 | 2923 |
| HSA-MIR-374B-5P | 99.90 | 69.98 | 2734 |
| HSA-MIR-130A-3P | 99.90 | 73.31 | 1861 |
| HSA-MIR-130B-3P | 99.90 | 73.27 | 1850 |
| HSA-MIR-301A-3P | 99.90 | 73.15 | 1839 |
| HSA-MIR-301B-3P | 99.90 | 73.19 | 1836 |
| HSA-MIR-3666 | 99.90 | 73.24 | 1833 |
| HSA-MIR-4295 | 99.90 | 73.11 | 1838 |
| HSA-MIR-95-5P | 99.89 | 72.17 | 3973 |
| HSA-MIR-17-5P | 99.89 | 73.83 | 2665 |
| HSA-MIR-106B-5P | 99.88 | 74.72 | 2795 |
| HSA-MIR-20A-5P | 99.88 | 74.76 | 2769 |
| HSA-MIR-20B-5P | 99.88 | 74.01 | 2621 |
| HSA-MIR-519D-3P | 99.88 | 73.97 | 2607 |
| HSA-MIR-526B-3P | 99.88 | 74.06 | 2587 |
| HSA-MIR-93-5P | 99.88 | 73.98 | 2606 |
| HSA-MIR-548AZ-5P | 99.83 | 69.94 | 3230 |
| HSA-MIR-548T-5P | 99.83 | 69.91 | 3220 |
| HSA-MIR-6817-3P | 99.79 | 68.35 | 2126 |
| HSA-MIR-34B-5P | 99.78 | 67.56 | 1175 |
| HSA-MIR-449C-5P | 99.78 | 67.63 | 1168 |
| HSA-MIR-2682-5P | 99.73 | 67.38 | 1055 |
| HSA-MIR-519A-3P | 99.67 | 71.67 | 1868 |
| HSA-MIR-519B-3P | 99.67 | 71.67 | 1868 |
Literature-anchored findings (GeneRIF, showing 6)
- A cell-based reporter gene assay has been developed and used for the screening of the human NMU2R agonist. (PMID:16781063)
- polymorphisms in the gene may be useful in identifying women at risk for osteoporosis. (PMID:25871004)
- Study identified a novel NMUR2 splice variant lacking the third exon and able to form heteromeric complexes with NMUR1 and NMUR2 without Neuromedin U (NMU). Its expression can block NMU signaling suppressing then ovarian cancer cells proliferation. (PMID:26317338)
- NMU might contribute to progression of NMUR2-positive breast cancer (PMID:28423716)
- Activation by NMU2 is longer lasting if NmS is the ligand. (PMID:29724789)
- A genome-wide association study implicates the pleiotropic effect of NMUR2 on asthma and COPD. (PMID:36543808)
Cross-species orthologs
8 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Nmur2 | ENSMUSG00000037393 |
| rattus_norvegicus | Nmur2 | ENSRNOG00000014081 |
| drosophila_melanogaster | CapaR | FBGN0037100 |
| drosophila_melanogaster | PK2-R2 | FBGN0038139 |
| drosophila_melanogaster | PK2-R1 | FBGN0038140 |
| drosophila_melanogaster | PK1-R | FBGN0038201 |
| caenorhabditis_elegans | WBGENE00016747 | |
| caenorhabditis_elegans | WBGENE00019616 |
Paralogs (15): NTSR1 (ENSG00000101188), BRS3 (ENSG00000102239), MLNR (ENSG00000102539), GHSR (ENSG00000121853), GRPR (ENSG00000126010), NMBR (ENSG00000135577), EDNRB (ENSG00000136160), EDNRA (ENSG00000151617), NTSR2 (ENSG00000169006), GPR37L1 (ENSG00000170075), GPR37 (ENSG00000170775), NMUR1 (ENSG00000171596), GPR148 (ENSG00000173302), TRHR (ENSG00000174417), GPR39 (ENSG00000183840)
Protein
Protein identifiers
Neuromedin-U receptor 2 — Q9GZQ4 (reviewed: Q9GZQ4)
Alternative names: G-protein coupled receptor FM-4, G-protein coupled receptor TGR-1
All UniProt accessions (1): Q9GZQ4
UniProt curated annotations — full annotation on UniProt →
Function. Receptor for the neuromedin-U and neuromedin-S neuropeptides.
Subcellular location. Cell membrane.
Tissue specificity. Predominantly expressed in the CNS, particularly in the medulla oblongata, pontine reticular formation, spinal cord, and thalamus. High level in testis whereas lower levels are present in a variety of peripheral tissues including the gastrointestinal tract, genitourinary tract, liver, pancreas, adrenal gland, thyroid gland, lung, trachea, spleen and thymus.
Similarity. Belongs to the G-protein coupled receptor 1 family.
RefSeq proteins (1): NP_064552* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000276 | GPCR_Rhodpsn | Family |
| IPR005390 | NeuromedU_rcpt | Family |
| IPR005392 | NeuromedU_rcpt_2 | Family |
| IPR017452 | GPCR_Rhodpsn_7TM | Domain |
| IPR045561 | NMU-R2_C | Domain |
Pfam: PF00001, PF19285
UniProt features (43 total): helix 12, topological domain 8, transmembrane region 7, sequence variant 5, strand 4, glycosylation site 3, chain 1, disulfide bond 1, sequence conflict 1, turn 1
Structure
Experimental structures (PDB)
3 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 7W55 | ELECTRON MICROSCOPY | 2.8 |
| 7W57 | ELECTRON MICROSCOPY | 3.2 |
| 7XK8 | ELECTRON MICROSCOPY | 3.3 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9GZQ4-F1 | 79.92 | 0.51 |
Antibody-complex structures (SAbDab): 2 — 7W55, 7W57
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): 119–204
Glycosylation sites (3): 9, 27, 194
Function
Pathways and Gene Ontology
Reactome pathways
3 pathways
| ID | Pathway |
|---|---|
| R-HSA-375276 | Peptide ligand-binding receptors |
| R-HSA-416476 | G alpha (q) signalling events |
| R-HSA-418594 | G alpha (i) signalling events |
MSigDB gene sets: 106 (showing top):
GOBP_BEHAVIOR, GOBP_REGULATION_OF_CALCIUM_MEDIATED_SIGNALING, GOBP_RESPONSE_TO_DIETARY_EXCESS, GOBP_REGULATION_OF_SMOOTH_MUSCLE_CONTRACTION, GOBP_INORGANIC_ANION_TRANSPORT, GOBP_MULTICELLULAR_ORGANISMAL_RESPONSE_TO_STRESS, GOBP_CELL_CELL_SIGNALING, GOBP_ORGANIC_ACID_TRANSPORT, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_POSITIVE_REGULATION_OF_CALCIUM_MEDIATED_SIGNALING, GOBP_EATING_BEHAVIOR, GOBP_REGULATION_OF_MUSCLE_CONTRACTION, GOBP_CHLORIDE_TRANSPORT, GOBP_MUSCLE_CONTRACTION, GOBP_RESPONSE_TO_PAIN
GO Biological Process (15): reduction of food intake in response to dietary excess (GO:0002023), regulation of smooth muscle contraction (GO:0006940), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), neuropeptide signaling pathway (GO:0007218), cell-cell signaling (GO:0007267), central nervous system development (GO:0007417), grooming behavior (GO:0007625), feeding behavior (GO:0007631), response to pain (GO:0048265), arachidonate secretion (GO:0050482), positive regulation of calcium-mediated signaling (GO:0050850), chloride transport (GO:0006821), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), chloride transmembrane transport (GO:1902476)
GO Molecular Function (7): neuromedin U receptor activity (GO:0001607), G protein-coupled receptor activity (GO:0004930), intracellularly calcium-gated chloride channel activity (GO:0005229), GTP binding (GO:0005525), neuropeptide receptor activity (GO:0008188), neuromedin U binding (GO:0042924), 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 | 2 |
| Class A/1 (Rhodopsin-like receptors) | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| G protein-coupled receptor signaling pathway | 3 |
| cell communication | 2 |
| signaling | 2 |
| behavior | 2 |
| neuropeptide binding | 2 |
| response to dietary excess | 1 |
| eating behavior | 1 |
| regulation of muscle contraction | 1 |
| smooth muscle contraction | 1 |
| phospholipase C activator activity | 1 |
| nervous system development | 1 |
| system development | 1 |
| multicellular organismal response to stress | 1 |
| icosanoid secretion | 1 |
| arachidonate transport | 1 |
| calcium-mediated signaling | 1 |
| regulation of calcium-mediated signaling | 1 |
| positive regulation of intracellular signal transduction | 1 |
| monoatomic anion transport | 1 |
| inorganic anion transport | 1 |
| cellular process | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| G protein-coupled receptor activity | 1 |
| signal transduction | 1 |
| chloride transport | 1 |
| monoatomic anion transmembrane transport | 1 |
| neuropeptide receptor activity | 1 |
| neuromedin U binding | 1 |
| transmembrane signaling receptor activity | 1 |
| chloride channel activity | 1 |
| ligand-gated monoatomic anion channel activity | 1 |
| intracellularly calcium-gated channel activity | 1 |
| guanyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| neuropeptide signaling pathway | 1 |
| G protein-coupled peptide receptor activity | 1 |
| binding | 1 |
| membrane | 1 |
| cell periphery | 1 |
Protein interactions and networks
STRING
830 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| NMUR2 | NMU | P48645 | 999 |
| NMUR2 | NMS | Q5H8A3 | 978 |
| NMUR2 | CHRNB4 | P30926 | 559 |
| NMUR2 | GALNT10 | Q86SR1 | 473 |
| NMUR2 | POMC | P01189 | 470 |
| NMUR2 | MPP2 | Q14168 | 462 |
| NMUR2 | NPS | P0C0P6 | 446 |
| NMUR2 | DLG2 | Q15700 | 443 |
| NMUR2 | AUTS2 | Q8WXX7 | 435 |
| NMUR2 | VPS54 | Q9P1Q0 | 419 |
| NMUR2 | PTPRD | P23468 | 415 |
| NMUR2 | CFDP1 | Q9UEE9 | 411 |
| NMUR2 | HSD17B2 | P37059 | 403 |
| NMUR2 | PPT1 | P50897 | 397 |
| NMUR2 | NMUR1 | Q9HB89 | 393 |
IntAct
24 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| NMUR2 | psi-mi:“MI:0915”(physical association) | 0.560 | |
| TCF4 | NMUR2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| NMUR2 | TRAF2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| ADAMTSL4 | NMUR2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| NMUR2 | ADAMTSL4 | psi-mi:“MI:0915”(physical association) | 0.560 |
| NMUR2 | TCF4 | psi-mi:“MI:0915”(physical association) | 0.560 |
| TRAF2 | NMUR2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| NMUR2 | NOTCH2NLA | psi-mi:“MI:0915”(physical association) | 0.490 |
| NOTCH2NLA | NMUR2 | psi-mi:“MI:0915”(physical association) | 0.490 |
| RAMP1 | NMUR2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP3 | NMUR2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| NMUR2 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| NMUR2 | RAMP2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| NMUR2 | TMEM63A | psi-mi:“MI:0914”(association) | 0.350 |
| NMUR2 | SMPD2 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (43): NMUR2 (Two-hybrid), NMUR2 (Two-hybrid), NMUR2 (Two-hybrid), KRTAP13-1 (Two-hybrid), NOTCH2NL (Two-hybrid), TAOK2 (Affinity Capture-MS), SLC6A6 (Affinity Capture-MS), SLC12A6 (Affinity Capture-MS), IGHA2 (Affinity Capture-MS), ATP2B4 (Affinity Capture-MS), TYW1 (Affinity Capture-MS), TMEM63A (Affinity Capture-MS), SLC41A3 (Affinity Capture-MS), ADCK2 (Affinity Capture-MS), ATP11C (Affinity Capture-MS)
ESM2 similar proteins: A0A2L0VBG2, A1ZAX0, B2ZHY2, O43194, O43614, O46635, O46639, O54798, O62809, O93603, O97967, P08909, P14842, P18599, P20789, P21761, P28223, P28335, P30975, P32247, P32940, P34968, P34981, P35363, P35371, P41984, P47751, P50128, P50129, P56490, P56719, P58308, Q01717, Q28596, Q4V622, Q5IS53, Q5IS66, Q5IS98, Q5R4Q6, Q5U431
Diamond homologs: A5A4K9, A5A4L1, C3ZQF9, O08725, O17239, O42179, O43193, O55040, O88319, O93603, P19020, P20789, P20905, P21917, P24628, P30989, P35367, P49683, P58826, P79291, Q09388, Q25188, Q28553, Q58CW4, Q5QD24, Q63384, Q7JQF1, Q8BZ39, Q8ITC7, Q90WY4, Q923Y8, Q92847, Q93126, Q95254, Q99P50, Q9ESQ4, Q9GZQ4, Q9HB89, Q9JJI5, Q9JJS7
SIGNOR signaling
10 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| NMS | up-regulates | NMUR2 | binding |
| NMUR2 | “up-regulates activity” | GNAI1 | binding |
| NMUR2 | “up-regulates activity” | GNAI3 | binding |
| NMUR2 | “up-regulates activity” | GNAO1 | binding |
| NMUR2 | “up-regulates activity” | GNAZ | binding |
| NMUR2 | “up-regulates activity” | GNAQ | binding |
| NMUR2 | “up-regulates activity” | GNA14 | binding |
| NMUR2 | “up-regulates activity” | GNA15 | binding |
| NMUR2 | “up-regulates activity” | GNA12 | binding |
| VXJPSOQJNUZHDN-YJFQKBDPSA-N | “up-regulates activity” | NMUR2 | “chemical activation” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
63 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 54 |
| Likely benign | 4 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
737 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 5:152398058:A:AC | donor_gain | 1.0000 |
| 5:152398059:C:CC | donor_gain | 1.0000 |
| 5:152398059:CA:C | donor_gain | 1.0000 |
| 5:152398059:CACAG:C | donor_gain | 1.0000 |
| 5:152404380:ATACT:A | donor_loss | 1.0000 |
| 5:152404381:TACT:T | donor_loss | 1.0000 |
| 5:152404382:AC:A | donor_loss | 1.0000 |
| 5:152404384:TCA:T | donor_loss | 1.0000 |
| 5:152404385:CAC:C | donor_loss | 1.0000 |
| 5:152404386:A:AC | donor_gain | 1.0000 |
| 5:152404386:A:T | donor_loss | 1.0000 |
| 5:152404386:ACT:A | donor_gain | 1.0000 |
| 5:152404387:C:CT | donor_gain | 1.0000 |
| 5:152404387:CT:C | donor_gain | 1.0000 |
| 5:152404387:CTC:C | donor_gain | 1.0000 |
| 5:152404387:CTCT:C | donor_gain | 1.0000 |
| 5:152404387:CTCTG:C | donor_gain | 1.0000 |
| 5:152395582:CAA:C | acceptor_gain | 0.9900 |
| 5:152395585:C:CC | acceptor_gain | 0.9900 |
| 5:152398141:TTAGC:T | acceptor_loss | 0.9800 |
| 5:152398142:TAG:T | acceptor_gain | 0.9800 |
| 5:152398142:TAGC:T | acceptor_loss | 0.9800 |
| 5:152398143:AGC:A | acceptor_loss | 0.9800 |
| 5:152398144:GCT:G | acceptor_loss | 0.9800 |
| 5:152398145:C:A | acceptor_loss | 0.9800 |
| 5:152398145:C:CC | acceptor_gain | 0.9800 |
| 5:152398146:T:G | acceptor_loss | 0.9800 |
| 5:152404379:GATAC:G | donor_loss | 0.9800 |
| 5:152404492:TGATG:T | donor_gain | 0.9800 |
| 5:152398051:GGCAC:G | donor_loss | 0.9700 |
AlphaMissense
2741 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 5:152404691:G:C | S141R | 0.996 |
| 5:152404691:G:T | S141R | 0.996 |
| 5:152404693:T:G | S141R | 0.996 |
| 5:152404856:G:C | S86R | 0.996 |
| 5:152404856:G:T | S86R | 0.996 |
| 5:152404858:T:G | S86R | 0.996 |
| 5:152395533:C:G | R288P | 0.993 |
| 5:152395544:G:C | F284L | 0.990 |
| 5:152395544:G:T | F284L | 0.990 |
| 5:152395546:A:G | F284L | 0.990 |
| 5:152404758:C:G | C119S | 0.990 |
| 5:152404759:A:T | C119S | 0.990 |
| 5:152404706:G:C | S136R | 0.989 |
| 5:152404706:G:T | S136R | 0.989 |
| 5:152404708:T:G | S136R | 0.989 |
| 5:152404603:A:G | W171R | 0.988 |
| 5:152404603:A:T | W171R | 0.988 |
| 5:152404759:A:G | C119R | 0.988 |
| 5:152404503:C:G | C204S | 0.987 |
| 5:152404504:A:T | C204S | 0.987 |
| 5:152404504:A:G | C204R | 0.986 |
| 5:152392482:G:C | S319R | 0.984 |
| 5:152392482:G:T | S319R | 0.984 |
| 5:152392484:T:G | S319R | 0.984 |
| 5:152404683:C:G | R144P | 0.984 |
| 5:152404778:G:C | F112L | 0.984 |
| 5:152404778:G:T | F112L | 0.984 |
| 5:152404780:A:G | F112L | 0.984 |
| 5:152395520:G:C | S292R | 0.983 |
| 5:152395520:G:T | S292R | 0.983 |
dbSNP variants (sampled 300 via entrez): RS1000565906 (5:152405805 C>T), RS1000622662 (5:152401416 T>A,C), RS1000895609 (5:152395068 A>G,T), RS1000914600 (5:152406779 GT>G), RS1001345424 (5:152395166 G>A,T), RS1001504932 (5:152405507 T>C), RS1001578682 (5:152398657 G>C,T), RS1001620970 (5:152392070 C>A), RS1001900930 (5:152393771 G>A,T), RS1001928911 (5:152400350 T>G), RS1001930097 (5:152393832 G>A,T), RS1001966684 (5:152399792 A>G), RS1002154351 (5:152406044 G>A), RS1002580312 (5:152397325 C>T), RS1002632399 (5:152397103 T>A)
Disease associations
OMIM: gene MIM:605108 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
27 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST000659_1 | Optic nerve measurement (cup area) | 8.000000e-06 |
| GCST001567_9 | Bipolar disorder and schizophrenia | 7.000000e-06 |
| GCST002136_12 | Periodontitis (PAL4Q3) | 5.000000e-06 |
| GCST002932_22 | Manganese levels | 2.000000e-07 |
| GCST003766_70 | Subjective well-being | 2.000000e-08 |
| GCST004946_41 | Schizophrenia | 4.000000e-08 |
| GCST006913_6 | Sedentary behaviour duration | 2.000000e-08 |
| GCST006919_3 | Ability to confide in someone | 4.000000e-06 |
| GCST006923_1 | Loneliness | 1.000000e-07 |
| GCST006923_12 | Loneliness | 8.000000e-10 |
| GCST006924_10 | Loneliness (MTAG) | 8.000000e-09 |
| GCST006942_3 | Feeling lonely | 6.000000e-09 |
| GCST007326_103 | Number of sexual partners | 1.000000e-11 |
| GCST007565_181 | Morning person | 6.000000e-14 |
| GCST007565_4 | Morning person | 2.000000e-17 |
| GCST007565_5 | Morning person | 2.000000e-18 |
| GCST007565_66 | Morning person | 9.000000e-14 |
| GCST007565_72 | Morning person | 7.000000e-18 |
| GCST007565_9 | Morning person | 4.000000e-18 |
| GCST007576_29 | Chronotype | 2.000000e-18 |
| GCST009391_1228 | Metabolite levels | 8.000000e-06 |
| GCST009391_1894 | Metabolite levels | 3.000000e-06 |
| GCST010397_33 | Gut microbiota (bacterial taxa, rank normal transformation method) | 2.000000e-06 |
| GCST010988_344 | Adult body size | 3.000000e-09 |
| GCST010989_255 | Body size at age 10 | 2.000000e-10 |
| GCST011124_18 | Caffeine consumption from tea | 1.000000e-10 |
| GCST011767_8 | Bipolar disorder | 5.000000e-09 |
EFO canonical traits (10, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007869 | wellbeing measurement |
| EFO:0008002 | physical activity measurement |
| EFO:0009592 | social interaction measurement |
| EFO:0007865 | loneliness measurement |
| EFO:0008328 | chronotype measurement |
| EFO:0010421 | triacylglycerol 54:3 measurement |
| EFO:0010414 | triacylglycerol 52:2 measurement |
| EFO:0007874 | gut microbiome measurement |
| EFO:0009819 | comparative body size at age 10, self-reported |
| EFO:0010091 | tea consumption measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL1075144 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 57,988 (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 |
|---|---|---|---|
| CHEMBL226335 | RUTIN | 3 | 57,988 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: gpcr — Neuromedin U receptors
Most potent curated ligand interactions (18 total), top 18:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| neuromedin U-25 | Agonist | 9.9 | pKi |
| [125I]neuromedin U-25 (human) | Agonist | 9.8 | pKd |
| neuromedin U-23 | Agonist | 9.7 | pKi |
| neuromedin U-25 | Agonist | 9.6 | pKi |
| neuromedin U-8 | Agonist | 9.3 | pKi |
| neuromedin S-33 | Agonist | 9.2 | pIC50 |
| [125I]neuromedin U-23 (rat) | Agonist | 9.1 | pKd |
| [125I]neuromedin U-8 (pig) | Agonist | 9.1 | pKd |
| HAS-NMU | Full agonist | 9.0 | pEC50 |
| compound 6b [PMID: 24999562] | Full agonist | 9.0 | pEC50 |
| NY0116 | Agonist | 8.77 | pEC50 |
| CPN-219 | Agonist | 8.66 | pEC50 |
| CPN-116 | Agonist | 8.19 | pEC50 |
| neuromedin U-8 | Agonist | 8.1 | pKi |
| PEG40-NMU | Full agonist | 8.0 | pEC50 |
| R-PSOP | Antagonist | 7.04 | pKB |
| NM4-C16 | Full agonist | 6.1 | pIC50 |
| compound NRA 4 [PMID: 25262941] | Full agonist | 4.85 | pEC50 |
ChEMBL bioactivities
178 potent at pChembl≥5 of 184 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.82 | EC50 | 0.15 | nM | CHEMBL4098010 |
| 9.80 | EC50 | 0.16 | nM | CHEMBL4081760 |
| 9.70 | EC50 | 0.2 | nM | CHEMBL4063341 |
| 9.70 | EC50 | 0.2 | nM | CHEMBL4074121 |
| 9.67 | EC50 | 0.2138 | nM | CHEMBL3758577 |
| 9.66 | EC50 | 0.22 | nM | CHEMBL4068681 |
| 9.55 | EC50 | 0.28 | nM | CHEMBL4088263 |
| 9.51 | EC50 | 0.31 | nM | CHEMBL4059530 |
| 9.47 | EC50 | 0.3388 | nM | CHEMBL3759452 |
| 9.47 | EC50 | 0.34 | nM | CHEMBL4061507 |
| 9.43 | EC50 | 0.37 | nM | CHEMBL4091611 |
| 9.41 | EC50 | 0.39 | nM | CHEMBL4087867 |
| 9.40 | EC50 | 0.4 | nM | CHEMBL3356083 |
| 9.39 | EC50 | 0.41 | nM | CHEMBL4073946 |
| 9.38 | EC50 | 0.42 | nM | CHEMBL4090300 |
| 9.37 | EC50 | 0.43 | nM | CHEMBL4079986 |
| 9.37 | EC50 | 0.43 | nM | CHEMBL3356083 |
| 9.33 | EC50 | 0.47 | nM | CHEMBL4063830 |
| 9.24 | EC50 | 0.58 | nM | CHEMBL4089636 |
| 9.24 | EC50 | 0.57 | nM | CHEMBL4097355 |
| 9.16 | EC50 | 0.69 | nM | CHEMBL4095998 |
| 9.15 | EC50 | 0.7 | nM | CHEMBL4177021 |
| 9.15 | EC50 | 0.71 | nM | CHEMBL4169726 |
| 9.13 | EC50 | 0.74 | nM | CHEMBL4100718 |
| 9.10 | EC50 | 0.7943 | nM | CHEMBL3315349 |
| 9.10 | EC50 | 0.8 | nM | CHEMBL4061906 |
| 9.09 | EC50 | 0.82 | nM | CHEMBL4099780 |
| 9.08 | EC50 | 0.83 | nM | CHEMBL4070175 |
| 9.08 | EC50 | 0.83 | nM | CHEMBL4172552 |
| 9.04 | EC50 | 0.92 | nM | CHEMBL3315349 |
| 9.03 | EC50 | 0.94 | nM | CHEMBL4071218 |
| 9.03 | EC50 | 0.93 | nM | CHEMBL4092033 |
| 8.92 | EC50 | 1.2 | nM | CHEMBL4060027 |
| 8.85 | EC50 | 1.4 | nM | CHEMBL4069256 |
| 8.82 | EC50 | 1.5 | nM | CHEMBL4083670 |
| 8.80 | EC50 | 1.6 | nM | CHEMBL4161902 |
| 8.77 | IC50 | 1.7 | nM | CHEMBL3356083 |
| 8.74 | EC50 | 1.8 | nM | CHEMBL4060830 |
| 8.74 | EC50 | 1.8 | nM | CHEMBL4169739 |
| 8.72 | EC50 | 1.905 | nM | CHEMBL4299242 |
| 8.72 | EC50 | 1.9 | nM | CHEMBL4092080 |
| 8.70 | EC50 | 2 | nM | CHEMBL4081819 |
| 8.70 | IC50 | 2 | nM | CHEMBL4169726 |
| 8.66 | EC50 | 2.2 | nM | CHEMBL4647192 |
| 8.62 | IC50 | 2.4 | nM | CHEMBL4177021 |
| 8.60 | EC50 | 2.5 | nM | CHEMBL3315349 |
| 8.59 | EC50 | 2.6 | nM | CHEMBL3425593 |
| 8.52 | EC50 | 3 | nM | CHEMBL4097408 |
| 8.48 | EC50 | 3.3 | nM | CHEMBL4088810 |
| 8.47 | EC50 | 3.4 | nM | CHEMBL4060571 |
PubChem BioAssay actives
182 with measured affinity, of 403 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 |
|---|---|---|---|---|
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0001 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-amino-2-methylpropanoyl)amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1273140: Agonist activity at recombinant human NMU2 expressed in HEK293 cells assessed as change in intracellular calcium flux by fluorescence assay | ec50 | 0.0002 | uM |
| (2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(4-hydroxyphenyl)-2-[(2-piperazin-1-ylacetyl)amino]propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0002 | uM |
| (2S)-4-amino-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(4-hydroxyphenyl)-2-[(2-piperazin-1-ylacetyl)amino]propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]-4-oxobutanoic acid | 1464657: Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay | ec50 | 0.0002 | uM |
| (2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(4-hydroxyphenyl)-2-[(2-piperazin-1-ylacetyl)amino]propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]-methylamino]propanoyl]amino]pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0002 | uM |
| (2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(4-hydroxyphenyl)-2-[(2-piperazin-1-ylacetyl)amino]propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0002 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1273140: Agonist activity at recombinant human NMU2 expressed in HEK293 cells assessed as change in intracellular calcium flux by fluorescence assay | ec50 | 0.0003 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-cyclohexyl-2-[[(2S)-3-(4-hydroxyphenyl)-2-[(2-piperazin-1-ylacetyl)amino]propanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0003 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-pyridin-4-ylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0003 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0003 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0004 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0004 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-6-aminohexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0004 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-oxopentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0004 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0004 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0004 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-cyclohexylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0005 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-cyclohexylpropanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0006 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-cyclohexylpropanoyl]amino]-4-methylpentanoyl]amino]-3-pyridin-4-ylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0006 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1352034: Agonist activity at human NMUR2 expressed in HEK293 cells assessed as induction of IP3 levels using myo-[2-3H(N)]-inositol after 60 mins by SPA-based topcount assay | ec50 | 0.0007 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0007 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[2-[3-[2-[2-(3-aminopropoxy)ethoxy]ethoxy]propylamino]-2-oxoethoxy]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]-methylamino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0007 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1352034: Agonist activity at human NMUR2 expressed in HEK293 cells assessed as induction of IP3 levels using myo-[2-3H(N)]-inositol after 60 mins by SPA-based topcount assay | ec50 | 0.0007 | uM |
| (4S)-5-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[(2S)-2-[[(2S)-5-carbamimidamido-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]-3-carboxypropanoyl]amino]-4-carboxybutanoyl]amino]-5-oxopentanoic acid | 1273140: Agonist activity at recombinant human NMU2 expressed in HEK293 cells assessed as change in intracellular calcium flux by fluorescence assay | ec50 | 0.0008 | uM |
| (2S)-5-[3-[2-[2-[3-[[2-[2-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(1S)-3-amino-1-carboxy-3-oxopropyl]amino]-5-[(N’-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxo-3-phenylpropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethoxy]acetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-2-[[4-[(hexadecanoylamino)methyl]cyclohexanecarbonyl]amino]-5-oxopentanoic acid | 1464657: Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay | ec50 | 0.0008 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-pyridin-4-ylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0008 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1352034: Agonist activity at human NMUR2 expressed in HEK293 cells assessed as induction of IP3 levels using myo-[2-3H(N)]-inositol after 60 mins by SPA-based topcount assay | ec50 | 0.0008 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(6-aminohexanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]-methylamino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0008 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-oxopentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0009 | uM |
| (4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-[[(2S)-3-(4-hydroxyphenyl)-2-[(2-piperazin-1-ylacetyl)amino]propanoyl]amino]-5-oxopentanoic acid | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0009 | uM |
| (4S)-4-[[(2S)-2-(3-aminopropanoylamino)-3-(4-hydroxyphenyl)propanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0012 | uM |
| (4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-[[(2S)-3-(4-hydroxyphenyl)-2-[(2-piperazin-1-ylacetyl)amino]propanoyl]amino]-5-oxopentanoic acid | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0014 | uM |
| (2S)-5-[3-[2-[2-[3-[[2-[2-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(1S)-3-amino-1-carboxy-3-oxopropyl]amino]-5-[(N’-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxo-3-phenylpropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethoxy]acetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-2-[[4-[(octadecanoylamino)methyl]cyclohexanecarbonyl]amino]-5-oxopentanoic acid | 1464657: Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay | ec50 | 0.0015 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1352034: Agonist activity at human NMUR2 expressed in HEK293 cells assessed as induction of IP3 levels using myo-[2-3H(N)]-inositol after 60 mins by SPA-based topcount assay | ec50 | 0.0016 | uM |
| (2S)-5-[3-[2-[2-[3-[[2-[2-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(1S)-3-amino-1-carboxy-3-oxopropyl]amino]-5-[(N’-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxo-3-phenylpropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethoxy]acetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-2-[[4-[(dodecanoylamino)methyl]cyclohexanecarbonyl]amino]-5-oxopentanoic acid | 1464657: Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay | ec50 | 0.0018 | uM |
| (2S)-2-[[(2S)-2-[[(2S,3aS,7aS)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1352034: Agonist activity at human NMUR2 expressed in HEK293 cells assessed as induction of IP3 levels using myo-[2-3H(N)]-inositol after 60 mins by SPA-based topcount assay | ec50 | 0.0018 | uM |
| (2S)-5-[3-[2-[2-[3-[[2-[2-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(1S)-3-amino-1-carboxy-3-oxopropyl]amino]-5-[(N’-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethoxy]acetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-2-[[4-[(octadecanoylamino)methyl]cyclohexanecarbonyl]amino]-5-oxopentanoic acid | 1464657: Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay | ec50 | 0.0019 | uM |
| (2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[2-[3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-(hexadecanoylamino)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]-2-methylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]butanediamide | 1273140: Agonist activity at recombinant human NMU2 expressed in HEK293 cells assessed as change in intracellular calcium flux by fluorescence assay | ec50 | 0.0019 | uM |
| (2S)-5-[3-[2-[2-[3-[[2-[2-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(1S)-3-amino-1-carboxy-3-oxopropyl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethoxy]acetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-2-[[4-[(octadecanoylamino)methyl]cyclohexanecarbonyl]amino]-5-oxopentanoic acid | 1464657: Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay | ec50 | 0.0020 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-(3-cyclohexylpropanoylamino)-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1659724: Agonist activity at human NMUR2 expressed in CHO cells by Fluo-4-AM dye based calcium mobilization assay | ec50 | 0.0022 | uM |
| (2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-3-(4-fluorophenyl)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-thiophen-2-ylacetyl)amino]propanoyl]amino]propanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]butanediamide | 1205846: Agonist activity at human NMUR2 expressed in CHO cells assessed as intracellular calcium flux at by Fluo-4 AM dye based fluorometric imaging method | ec50 | 0.0026 | uM |
| (2S)-5-[3-[2-[2-[3-[[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(1S)-3-amino-1-carboxy-3-oxopropyl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethoxy]acetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-2-[[4-[(hexadecanoylamino)methyl]cyclohexanecarbonyl]amino]-5-oxopentanoic acid | 1464657: Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay | ec50 | 0.0030 | uM |
| (2S)-4-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[2-(4-hexadecylpiperazin-1-yl)acetyl]amino]propanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]amino]-4-oxobutanoic acid | 1464657: Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay | ec50 | 0.0033 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-6-aminohexanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1446044: Agonist activity at human NMUR2 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay | ec50 | 0.0034 | uM |
| (2S)-4-amino-2-[[(2S)-5-carbamimidamido-2-[[(2S)-1-[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[2-(4-hexadecylpiperazin-1-yl)acetyl]amino]-3-hydroxypropanoyl]amino]pentanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]-4-oxobutanoic acid | 1464657: Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay | ec50 | 0.0035 | uM |
| (2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(3S)-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carbonyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]butanediamide | 1352034: Agonist activity at human NMUR2 expressed in HEK293 cells assessed as induction of IP3 levels using myo-[2-3H(N)]-inositol after 60 mins by SPA-based topcount assay | ec50 | 0.0035 | uM |
| (2S)-4-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[2-(4-hexadecylpiperazin-1-yl)acetyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]amino]-4-oxobutanoic acid | 1464657: Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay | ec50 | 0.0036 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-3-amino-2-[[(2S)-2-[[(2S)-2-(3-cyclohexylpropanoylamino)-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1352034: Agonist activity at human NMUR2 expressed in HEK293 cells assessed as induction of IP3 levels using myo-[2-3H(N)]-inositol after 60 mins by SPA-based topcount assay | ec50 | 0.0038 | uM |
| (2S)-4-amino-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[3-[2-[2-[2-[2-[3-[2-[2-[2-[2-(hexadecanoylamino)ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]-4-oxobutanoic acid | 1464657: Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay | ec50 | 0.0038 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3,4-dihydro-1H-naphthalene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]butanediamide | 1355079: Agonist activity at human NMUR2 expressed in HEK293 cells assessed as IP3 accumulation after 60 mins in presence of myo-[2-3H(N)]inositol by scintillation proximity assay | ec50 | 0.0038 | uM |
CTD chemical–gene interactions
7 total (human), top 7 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Benzo(a)pyrene | increases mutagenesis, decreases methylation, increases methylation | 2 |
| pirinixic acid | decreases expression, increases activity, affects binding | 1 |
| sodium arsenite | increases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| 2-palmitoylglycerol | increases expression | 1 |
| Synephrine | increases activity | 1 |
| Tobacco Smoke Pollution | increases expression | 1 |
ChEMBL screening assays
46 unique, capped per target: 33 functional, 8 binding, 5 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1107819 | Binding | Binding affinity to NMUR2 | Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach. — Eur J Med Chem |
| CHEMBL3362245 | Functional | Agonist activity at human NMUR2 expressed in HEK293 cells at 1 to 100 nM by calcium mobilization assay relative to NMU | Discovery of selective hexapeptide agonists to human neuromedin U receptors types 1 and 2. — J Med Chem |
| CHEMBL4727273 | ADMET | Agonist activity at human NMUR2 expressed in CHO cells at 10 nM by calcium mobilization assay | Design and synthesis of peptidic partial agonists of human neuromedin U receptor 1 with enhanced serum stability. — Bioorg Med Chem Lett |
Cellosaurus cell lines
1 cell lines: 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_H377 | 293T/NMU2 | Transformed cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): periodontitis