NMUR2

gene
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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

FieldValue
HGNC IDHGNC:16454
Approved symbolNMUR2
Nameneuromedin U receptor 2
Location5q33.1
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000132911
Ensembl biotypeprotein_coding
OMIM605108
Entrez56923

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

ExonStartEnd
ENSE00000767902152395459152395584
ENSE00001021222152391546152392501
ENSE00001021223152404388152405279
ENSE00003468312152398060152398144

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 IDTPM avgSamples expressed
644450.053919
644460.049221

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
tibialis anteriorUBERON:000138582.48silver quality
pancreatic ductal cellCL:000207978.52silver quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047378.23gold quality
ileal mucosaUBERON:000033178.10silver quality
oocyteCL:000002364.98gold quality
deltoidUBERON:000147663.25silver quality
corpus callosumUBERON:000233662.09gold quality
upper leg skinUBERON:000426257.64gold quality
endothelial cellCL:000011557.01gold quality
epithelial cell of pancreasCL:000008356.90gold quality
myocardiumUBERON:000234956.26gold quality
C1 segment of cervical spinal cordUBERON:000646956.23gold quality
spinal cordUBERON:000224054.76gold quality
medial globus pallidusUBERON:000247754.60silver quality
cardiac muscle of right atriumUBERON:000337954.34gold quality
left ventricle myocardiumUBERON:000656654.23gold quality
kidney epitheliumUBERON:000481953.93gold quality
upper arm skinUBERON:000426353.52gold quality
right testisUBERON:000453452.47gold quality
quadriceps femorisUBERON:000137752.42gold quality
right lungUBERON:000216751.44gold quality
hypothalamusUBERON:000189850.77gold quality
spermCL:000001950.74gold quality
left testisUBERON:000453350.34gold quality
testisUBERON:000047350.14gold quality
vastus lateralisUBERON:000137949.88gold quality
right lobe of thyroid glandUBERON:000111948.65gold quality
Brodmann (1909) area 9UBERON:001354047.96gold quality
Brodmann (1909) area 46UBERON:000648347.86gold quality
left lobe of thyroid glandUBERON:000112047.71gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3no3.90

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):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-3064-3P100.0070.091254
HSA-MIR-4692100.0067.322066
HSA-MIR-450A-1-3P100.0069.331837
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-454-3P99.9174.011925
HSA-MIR-106A-5P99.9073.942683
HSA-MIR-374A-5P99.9071.342923
HSA-MIR-374B-5P99.9069.982734
HSA-MIR-130A-3P99.9073.311861
HSA-MIR-130B-3P99.9073.271850
HSA-MIR-301A-3P99.9073.151839
HSA-MIR-301B-3P99.9073.191836
HSA-MIR-366699.9073.241833
HSA-MIR-429599.9073.111838
HSA-MIR-95-5P99.8972.173973
HSA-MIR-17-5P99.8973.832665
HSA-MIR-106B-5P99.8874.722795
HSA-MIR-20A-5P99.8874.762769
HSA-MIR-20B-5P99.8874.012621
HSA-MIR-519D-3P99.8873.972607
HSA-MIR-526B-3P99.8874.062587
HSA-MIR-93-5P99.8873.982606
HSA-MIR-548AZ-5P99.8369.943230
HSA-MIR-548T-5P99.8369.913220
HSA-MIR-6817-3P99.7968.352126
HSA-MIR-34B-5P99.7867.561175
HSA-MIR-449C-5P99.7867.631168
HSA-MIR-2682-5P99.7367.381055
HSA-MIR-519A-3P99.6771.671868
HSA-MIR-519B-3P99.6771.671868

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

OrganismSymbolGene ID
mus_musculusNmur2ENSMUSG00000037393
rattus_norvegicusNmur2ENSRNOG00000014081
drosophila_melanogasterCapaRFBGN0037100
drosophila_melanogasterPK2-R2FBGN0038139
drosophila_melanogasterPK2-R1FBGN0038140
drosophila_melanogasterPK1-RFBGN0038201
caenorhabditis_elegansWBGENE00016747
caenorhabditis_elegansWBGENE00019616

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 2Q9GZQ4 (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)

IDNameType
IPR000276GPCR_RhodpsnFamily
IPR005390NeuromedU_rcptFamily
IPR005392NeuromedU_rcpt_2Family
IPR017452GPCR_Rhodpsn_7TMDomain
IPR045561NMU-R2_CDomain

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.

PDBMethodResolution (Å)
7W55ELECTRON MICROSCOPY2.8
7W57ELECTRON MICROSCOPY3.2
7XK8ELECTRON MICROSCOPY3.3

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q9GZQ4-F179.920.51

Antibody-complex structures (SAbDab): 27W55, 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

IDPathway
R-HSA-375276Peptide ligand-binding receptors
R-HSA-416476G alpha (q) signalling events
R-HSA-418594G 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:

CategoryPathways
GPCR downstream signalling2
Class A/1 (Rhodopsin-like receptors)1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
G protein-coupled receptor signaling pathway3
cell communication2
signaling2
behavior2
neuropeptide binding2
response to dietary excess1
eating behavior1
regulation of muscle contraction1
smooth muscle contraction1
phospholipase C activator activity1
nervous system development1
system development1
multicellular organismal response to stress1
icosanoid secretion1
arachidonate transport1
calcium-mediated signaling1
regulation of calcium-mediated signaling1
positive regulation of intracellular signal transduction1
monoatomic anion transport1
inorganic anion transport1
cellular process1
regulation of cellular process1
cellular response to stimulus1
G protein-coupled receptor activity1
signal transduction1
chloride transport1
monoatomic anion transmembrane transport1
neuropeptide receptor activity1
neuromedin U binding1
transmembrane signaling receptor activity1
chloride channel activity1
ligand-gated monoatomic anion channel activity1
intracellularly calcium-gated channel activity1
guanyl ribonucleotide binding1
purine ribonucleoside triphosphate binding1
neuropeptide signaling pathway1
G protein-coupled peptide receptor activity1
binding1
membrane1
cell periphery1

Protein interactions and networks

STRING

830 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
NMUR2NMUP48645999
NMUR2NMSQ5H8A3978
NMUR2CHRNB4P30926559
NMUR2GALNT10Q86SR1473
NMUR2POMCP01189470
NMUR2MPP2Q14168462
NMUR2NPSP0C0P6446
NMUR2DLG2Q15700443
NMUR2AUTS2Q8WXX7435
NMUR2VPS54Q9P1Q0419
NMUR2PTPRDP23468415
NMUR2CFDP1Q9UEE9411
NMUR2HSD17B2P37059403
NMUR2PPT1P50897397
NMUR2NMUR1Q9HB89393

IntAct

24 interactions, top by confidence:

ABTypeScore
NMUR2psi-mi:“MI:0915”(physical association)0.560
TCF4NMUR2psi-mi:“MI:0915”(physical association)0.560
NMUR2TRAF2psi-mi:“MI:0915”(physical association)0.560
ADAMTSL4NMUR2psi-mi:“MI:0915”(physical association)0.560
NMUR2ADAMTSL4psi-mi:“MI:0915”(physical association)0.560
NMUR2TCF4psi-mi:“MI:0915”(physical association)0.560
TRAF2NMUR2psi-mi:“MI:0915”(physical association)0.560
NMUR2NOTCH2NLApsi-mi:“MI:0915”(physical association)0.490
NOTCH2NLANMUR2psi-mi:“MI:0915”(physical association)0.490
RAMP1NMUR2psi-mi:“MI:0915”(physical association)0.400
RAMP3NMUR2psi-mi:“MI:0915”(physical association)0.400
NMUR2RAMP1psi-mi:“MI:0915”(physical association)0.400
NMUR2RAMP2psi-mi:“MI:0915”(physical association)0.400
NMUR2TMEM63Apsi-mi:“MI:0914”(association)0.350
NMUR2SMPD2psi-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.

AEffectBMechanism
NMSup-regulatesNMUR2binding
NMUR2“up-regulates activity”GNAI1binding
NMUR2“up-regulates activity”GNAI3binding
NMUR2“up-regulates activity”GNAO1binding
NMUR2“up-regulates activity”GNAZbinding
NMUR2“up-regulates activity”GNAQbinding
NMUR2“up-regulates activity”GNA14binding
NMUR2“up-regulates activity”GNA15binding
NMUR2“up-regulates activity”GNA12binding
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):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance54
Likely benign4
Benign2

Top pathogenic / likely-pathogenic (0)

SpliceAI

737 predictions. Top by Δscore:

VariantEffectΔscore
5:152398058:A:ACdonor_gain1.0000
5:152398059:C:CCdonor_gain1.0000
5:152398059:CA:Cdonor_gain1.0000
5:152398059:CACAG:Cdonor_gain1.0000
5:152404380:ATACT:Adonor_loss1.0000
5:152404381:TACT:Tdonor_loss1.0000
5:152404382:AC:Adonor_loss1.0000
5:152404384:TCA:Tdonor_loss1.0000
5:152404385:CAC:Cdonor_loss1.0000
5:152404386:A:ACdonor_gain1.0000
5:152404386:A:Tdonor_loss1.0000
5:152404386:ACT:Adonor_gain1.0000
5:152404387:C:CTdonor_gain1.0000
5:152404387:CT:Cdonor_gain1.0000
5:152404387:CTC:Cdonor_gain1.0000
5:152404387:CTCT:Cdonor_gain1.0000
5:152404387:CTCTG:Cdonor_gain1.0000
5:152395582:CAA:Cacceptor_gain0.9900
5:152395585:C:CCacceptor_gain0.9900
5:152398141:TTAGC:Tacceptor_loss0.9800
5:152398142:TAG:Tacceptor_gain0.9800
5:152398142:TAGC:Tacceptor_loss0.9800
5:152398143:AGC:Aacceptor_loss0.9800
5:152398144:GCT:Gacceptor_loss0.9800
5:152398145:C:Aacceptor_loss0.9800
5:152398145:C:CCacceptor_gain0.9800
5:152398146:T:Gacceptor_loss0.9800
5:152404379:GATAC:Gdonor_loss0.9800
5:152404492:TGATG:Tdonor_gain0.9800
5:152398051:GGCAC:Gdonor_loss0.9700

AlphaMissense

2741 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
5:152404691:G:CS141R0.996
5:152404691:G:TS141R0.996
5:152404693:T:GS141R0.996
5:152404856:G:CS86R0.996
5:152404856:G:TS86R0.996
5:152404858:T:GS86R0.996
5:152395533:C:GR288P0.993
5:152395544:G:CF284L0.990
5:152395544:G:TF284L0.990
5:152395546:A:GF284L0.990
5:152404758:C:GC119S0.990
5:152404759:A:TC119S0.990
5:152404706:G:CS136R0.989
5:152404706:G:TS136R0.989
5:152404708:T:GS136R0.989
5:152404603:A:GW171R0.988
5:152404603:A:TW171R0.988
5:152404759:A:GC119R0.988
5:152404503:C:GC204S0.987
5:152404504:A:TC204S0.987
5:152404504:A:GC204R0.986
5:152392482:G:CS319R0.984
5:152392482:G:TS319R0.984
5:152392484:T:GS319R0.984
5:152404683:C:GR144P0.984
5:152404778:G:CF112L0.984
5:152404778:G:TF112L0.984
5:152404780:A:GF112L0.984
5:152395520:G:CS292R0.983
5:152395520:G:TS292R0.983

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):

StudyTraitp-value
GCST000659_1Optic nerve measurement (cup area)8.000000e-06
GCST001567_9Bipolar disorder and schizophrenia7.000000e-06
GCST002136_12Periodontitis (PAL4Q3)5.000000e-06
GCST002932_22Manganese levels2.000000e-07
GCST003766_70Subjective well-being2.000000e-08
GCST004946_41Schizophrenia4.000000e-08
GCST006913_6Sedentary behaviour duration2.000000e-08
GCST006919_3Ability to confide in someone4.000000e-06
GCST006923_1Loneliness1.000000e-07
GCST006923_12Loneliness8.000000e-10
GCST006924_10Loneliness (MTAG)8.000000e-09
GCST006942_3Feeling lonely6.000000e-09
GCST007326_103Number of sexual partners1.000000e-11
GCST007565_181Morning person6.000000e-14
GCST007565_4Morning person2.000000e-17
GCST007565_5Morning person2.000000e-18
GCST007565_66Morning person9.000000e-14
GCST007565_72Morning person7.000000e-18
GCST007565_9Morning person4.000000e-18
GCST007576_29Chronotype2.000000e-18
GCST009391_1228Metabolite levels8.000000e-06
GCST009391_1894Metabolite levels3.000000e-06
GCST010397_33Gut microbiota (bacterial taxa, rank normal transformation method)2.000000e-06
GCST010988_344Adult body size3.000000e-09
GCST010989_255Body size at age 102.000000e-10
GCST011124_18Caffeine consumption from tea1.000000e-10
GCST011767_8Bipolar disorder5.000000e-09

EFO canonical traits (10, from GWAS)

EFO IDTrait name
EFO:0007869wellbeing measurement
EFO:0008002physical activity measurement
EFO:0009592social interaction measurement
EFO:0007865loneliness measurement
EFO:0008328chronotype measurement
EFO:0010421triacylglycerol 54:3 measurement
EFO:0010414triacylglycerol 52:2 measurement
EFO:0007874gut microbiome measurement
EFO:0009819comparative body size at age 10, self-reported
EFO:0010091tea 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).

MoleculeNamePhasePatents
CHEMBL226335RUTIN357,988

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:

LigandActionAffinityParameter
neuromedin U-25Agonist9.9pKi
[125I]neuromedin U-25 (human)Agonist9.8pKd
neuromedin U-23Agonist9.7pKi
neuromedin U-25Agonist9.6pKi
neuromedin U-8Agonist9.3pKi
neuromedin S-33Agonist9.2pIC50
[125I]neuromedin U-23 (rat)Agonist9.1pKd
[125I]neuromedin U-8 (pig)Agonist9.1pKd
HAS-NMUFull agonist9.0pEC50
compound 6b [PMID: 24999562]Full agonist9.0pEC50
NY0116Agonist8.77pEC50
CPN-219Agonist8.66pEC50
CPN-116Agonist8.19pEC50
neuromedin U-8Agonist8.1pKi
PEG40-NMUFull agonist8.0pEC50
R-PSOPAntagonist7.04pKB
NM4-C16Full agonist6.1pIC50
compound NRA 4 [PMID: 25262941]Full agonist4.85pEC50

ChEMBL bioactivities

178 potent at pChembl≥5 of 184 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.82EC500.15nMCHEMBL4098010
9.80EC500.16nMCHEMBL4081760
9.70EC500.2nMCHEMBL4063341
9.70EC500.2nMCHEMBL4074121
9.67EC500.2138nMCHEMBL3758577
9.66EC500.22nMCHEMBL4068681
9.55EC500.28nMCHEMBL4088263
9.51EC500.31nMCHEMBL4059530
9.47EC500.3388nMCHEMBL3759452
9.47EC500.34nMCHEMBL4061507
9.43EC500.37nMCHEMBL4091611
9.41EC500.39nMCHEMBL4087867
9.40EC500.4nMCHEMBL3356083
9.39EC500.41nMCHEMBL4073946
9.38EC500.42nMCHEMBL4090300
9.37EC500.43nMCHEMBL4079986
9.37EC500.43nMCHEMBL3356083
9.33EC500.47nMCHEMBL4063830
9.24EC500.58nMCHEMBL4089636
9.24EC500.57nMCHEMBL4097355
9.16EC500.69nMCHEMBL4095998
9.15EC500.7nMCHEMBL4177021
9.15EC500.71nMCHEMBL4169726
9.13EC500.74nMCHEMBL4100718
9.10EC500.7943nMCHEMBL3315349
9.10EC500.8nMCHEMBL4061906
9.09EC500.82nMCHEMBL4099780
9.08EC500.83nMCHEMBL4070175
9.08EC500.83nMCHEMBL4172552
9.04EC500.92nMCHEMBL3315349
9.03EC500.94nMCHEMBL4071218
9.03EC500.93nMCHEMBL4092033
8.92EC501.2nMCHEMBL4060027
8.85EC501.4nMCHEMBL4069256
8.82EC501.5nMCHEMBL4083670
8.80EC501.6nMCHEMBL4161902
8.77IC501.7nMCHEMBL3356083
8.74EC501.8nMCHEMBL4060830
8.74EC501.8nMCHEMBL4169739
8.72EC501.905nMCHEMBL4299242
8.72EC501.9nMCHEMBL4092080
8.70EC502nMCHEMBL4081819
8.70IC502nMCHEMBL4169726
8.66EC502.2nMCHEMBL4647192
8.62IC502.4nMCHEMBL4177021
8.60EC502.5nMCHEMBL3315349
8.59EC502.6nMCHEMBL3425593
8.52EC503nMCHEMBL4097408
8.48EC503.3nMCHEMBL4088810
8.47EC503.4nMCHEMBL4060571

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.

CompoundAssayTypeValueUnit
(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]butanediamide1446044: 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 assayec500.0001uM
(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]butanediamide1273140: Agonist activity at recombinant human NMU2 expressed in HEK293 cells assessed as change in intracellular calcium flux by fluorescence assayec500.0002uM
(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]butanediamide1446044: 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 assayec500.0002uM
(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 acid1464657: 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 assayec500.0002uM
(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]butanediamide1446044: 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 assayec500.0002uM
(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]butanediamide1446044: 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 assayec500.0002uM
(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]butanediamide1273140: Agonist activity at recombinant human NMU2 expressed in HEK293 cells assessed as change in intracellular calcium flux by fluorescence assayec500.0003uM
(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]butanediamide1446044: 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 assayec500.0003uM
(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]butanediamide1446044: 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 assayec500.0003uM
(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]butanediamide1446044: 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 assayec500.0003uM
(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]butanediamide1446044: 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 assayec500.0004uM
(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]butanediamide1446044: 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 assayec500.0004uM
(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]butanediamide1446044: 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 assayec500.0004uM
(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]butanediamide1446044: 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 assayec500.0004uM
(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]butanediamide1446044: 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 assayec500.0004uM
(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]butanediamide1446044: 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 assayec500.0004uM
(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]butanediamide1446044: 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 assayec500.0005uM
(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]butanediamide1446044: 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 assayec500.0006uM
(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]butanediamide1446044: 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 assayec500.0006uM
(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]butanediamide1352034: 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 assayec500.0007uM
(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]butanediamide1446044: 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 assayec500.0007uM
(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]butanediamide1446044: 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 assayec500.0007uM
(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]butanediamide1352034: 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 assayec500.0007uM
(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 acid1273140: Agonist activity at recombinant human NMU2 expressed in HEK293 cells assessed as change in intracellular calcium flux by fluorescence assayec500.0008uM
(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 acid1464657: 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 assayec500.0008uM
(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]butanediamide1446044: 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 assayec500.0008uM
(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]butanediamide1352034: 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 assayec500.0008uM
(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]butanediamide1446044: 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 assayec500.0008uM
(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]butanediamide1446044: 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 assayec500.0009uM
(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 acid1446044: 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 assayec500.0009uM
(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 acid1446044: 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 assayec500.0012uM
(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 acid1446044: 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 assayec500.0014uM
(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 acid1464657: 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 assayec500.0015uM
(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]butanediamide1352034: 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 assayec500.0016uM
(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 acid1464657: 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 assayec500.0018uM
(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]butanediamide1352034: 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 assayec500.0018uM
(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 acid1464657: 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 assayec500.0019uM
(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]butanediamide1273140: Agonist activity at recombinant human NMU2 expressed in HEK293 cells assessed as change in intracellular calcium flux by fluorescence assayec500.0019uM
(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 acid1464657: 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 assayec500.0020uM
(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]butanediamide1659724: Agonist activity at human NMUR2 expressed in CHO cells by Fluo-4-AM dye based calcium mobilization assayec500.0022uM
(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]butanediamide1205846: Agonist activity at human NMUR2 expressed in CHO cells assessed as intracellular calcium flux at by Fluo-4 AM dye based fluorometric imaging methodec500.0026uM
(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 acid1464657: 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 assayec500.0030uM
(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 acid1464657: 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 assayec500.0033uM
(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]butanediamide1446044: 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 assayec500.0034uM
(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 acid1464657: 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 assayec500.0035uM
(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]butanediamide1352034: 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 assayec500.0035uM
(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 acid1464657: 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 assayec500.0036uM
(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]butanediamide1352034: 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 assayec500.0038uM
(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 acid1464657: 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 assayec500.0038uM
(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]butanediamide1355079: 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 assayec500.0038uM

CTD chemical–gene interactions

7 total (human), top 7 by PubMed support.

ChemicalActions (top 5)PubMed papers
Benzo(a)pyreneincreases mutagenesis, decreases methylation, increases methylation2
pirinixic aciddecreases expression, increases activity, affects binding1
sodium arseniteincreases expression1
CGP 52608affects binding, increases reaction1
2-palmitoylglycerolincreases expression1
Synephrineincreases activity1
Tobacco Smoke Pollutionincreases expression1

ChEMBL screening assays

46 unique, capped per target: 33 functional, 8 binding, 5 admet

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1107819BindingBinding affinity to NMUR2Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach. — Eur J Med Chem
CHEMBL3362245FunctionalAgonist activity at human NMUR2 expressed in HEK293 cells at 1 to 100 nM by calcium mobilization assay relative to NMUDiscovery of selective hexapeptide agonists to human neuromedin U receptors types 1 and 2. — J Med Chem
CHEMBL4727273ADMETAgonist activity at human NMUR2 expressed in CHO cells at 10 nM by calcium mobilization assayDesign 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):

CellosaurusNameCategorySex
CVCL_H377293T/NMU2Transformed cell lineFemale

Clinical trials (associated diseases)

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

  • Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): periodontitis