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MLNR

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Summary

MLNR (motilin receptor, HGNC:4495) is a protein-coding gene on chromosome 13q14.2, encoding Motilin receptor (O43193). Receptor for motilin.

Motilin is a 22 amino acid peptide hormone expressed throughout the gastrointestinal (GI) tract. The protein encoded by this gene is a motilin receptor which is a member of the G-protein coupled receptor 1 family. This member is a multi-pass transmembrane protein, and is an important therapeutic target for the treatment of hypomotility disorders.

Source: NCBI Gene 2862 — RefSeq curated summary.

At a glance

  • Clinical variants (ClinVar): 63 total
  • Druggable target: yes — 76 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_001507

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:4495
Approved symbolMLNR
Namemotilin receptor
Location13q14.2
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000102539
Ensembl biotypeprotein_coding
OMIM602885
Entrez2862

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000218721, ENST00000850988

RefSeq mRNA: 1 — MANE Select: NM_001507 NM_001507

CCDS: CCDS9414

Canonical transcript exons

ENST00000218721 — 2 exons

ExonStartEnd
ENSE000042831604922204049222377
ENSE000042831614922033849221238

Expression profiles

Bgee: expression breadth broad, 34 present calls, max score 98.12.

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047398.12gold quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099162.45gold quality
deciduaUBERON:000245056.55gold quality
bone marrow cellCL:000209254.73gold quality
ileal mucosaUBERON:000033154.32silver quality
hair follicleUBERON:000207352.43gold quality
deltoidUBERON:000147650.02gold quality
bone marrowUBERON:000237149.90gold quality
pancreatic ductal cellCL:000207949.76silver quality
tibialis anteriorUBERON:000138549.72silver quality
epithelial cell of pancreasCL:000008349.42gold quality
Brodmann (1909) area 46UBERON:000648349.30gold quality
cervix squamous epitheliumUBERON:000692249.20gold quality
quadriceps femorisUBERON:000137749.02gold quality
olfactory bulbUBERON:000226448.92gold quality
myocardiumUBERON:000234948.87gold quality
type B pancreatic cellCL:000016948.83gold quality
cardiac muscle of right atriumUBERON:000337948.55gold quality
CA1 field of hippocampusUBERON:000388148.50gold quality
vastus lateralisUBERON:000137948.25gold quality
left ventricle myocardiumUBERON:000656648.24gold quality
orbitofrontal cortexUBERON:000416748.20gold quality
upper arm skinUBERON:000426348.06gold quality
cervix epitheliumUBERON:000480148.04gold quality
oviduct epitheliumUBERON:000480448.00gold quality
tongue squamous epitheliumUBERON:000691947.92gold quality
mucosa of urinary bladderUBERON:000125947.80gold quality
metanephric glomerulusUBERON:000473647.45gold quality
thymusUBERON:000237047.42gold quality
kidney epitheliumUBERON:000481947.39gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3no0.65

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 9)

  • The motilin pharmacophore in CHO cells expressing the human motilin receptor (PMID:12054506)
  • motilin receptor extracellular domains have roles in peptide and non-peptidyl agonist binding and activity (PMID:16531413)
  • action by different chemical classes of agonists that are known to interact with distinct regions of the motilin receptor likely yield a common activation state of the cytosolic face of this receptor (PMID:18032475)
  • The motilin receptor is expressed in human colonic and ileal smooth muscle. Further, motilin receptor expression was also shown in the mucosa. (PMID:18183601)
  • Desensitization and internalization of MLNR is independent of the C-terminal tail. (PMID:18420306)
  • The data suggested that in species expressing both motilin-MR and ghrelin-GHSR, there is a compensatory relationship in vivo. (PMID:22465164)
  • data support important roles of new regions in the TM domains of the motilin receptor for erythromycin action, suggesting differential mechanisms of actions by peptidyl and non-peptidyl ligands (PMID:23142315)
  • human motilin receptor transgenic (Tg) mice were tested with experiments evaluating the effects of motilin, erythromycin (EM), and ghrelin. (PMID:30934667)
  • Motilin Receptor Expression Found in the Human Main and Accessory Lacrimal Glands. (PMID:33974477)

Cross-species orthologs

1 orthologs

OrganismSymbolGene ID
danio_reriomlnrENSDARG00000091207

Paralogs (15): NTSR1 (ENSG00000101188), BRS3 (ENSG00000102239), GHSR (ENSG00000121853), GRPR (ENSG00000126010), NMUR2 (ENSG00000132911), NMBR (ENSG00000135577), EDNRB (ENSG00000136160), EDNRA (ENSG00000151617), NTSR2 (ENSG00000169006), GPR37L1 (ENSG00000170075), GPR37 (ENSG00000170775), NMUR1 (ENSG00000171596), GPR148 (ENSG00000173302), TRHR (ENSG00000174417), GPR39 (ENSG00000183840)

Protein

Protein identifiers

Motilin receptor — O43193 (reviewed: O43193)

Alternative names: G-protein coupled receptor 38

All UniProt accessions (1): O43193

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for motilin.

Subcellular location. Cell membrane.

Tissue specificity. Expressed only in thyroid, stomach, and bone marrow.

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

Isoforms (2)

UniProt IDNamesCanonical?
O43193-1Ayes
O43193-2B

RefSeq proteins (1): NP_001498* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000276GPCR_RhodpsnFamily
IPR003905GHS-R/MTLRFamily
IPR017452GPCR_Rhodpsn_7TMDomain

Pfam: PF00001

UniProt features (33 total): helix 12, topological domain 8, transmembrane region 7, glycosylation site 2, chain 1, disulfide bond 1, splice variant 1, turn 1

Structure

Experimental structures (PDB)

4 structures.

PDBMethodResolution (Å)
9JMCELECTRON MICROSCOPY2.57
9JMDELECTRON MICROSCOPY2.74
8IBVELECTRON MICROSCOPY3.19
8IBUELECTRON MICROSCOPY3.51

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-O43193-F177.990.44

Antibody-complex structures (SAbDab): 3 — 8IBU, 8IBV, 9JMD

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): 111–235

Glycosylation sites (2): 6, 192

Function

Pathways and Gene Ontology

Reactome pathways

7 pathways

IDPathway
R-HSA-375276Peptide ligand-binding receptors
R-HSA-416476G alpha (q) signalling events
R-HSA-162582Signal Transduction
R-HSA-372790Signaling by GPCR
R-HSA-373076Class A/1 (Rhodopsin-like receptors)
R-HSA-388396GPCR downstream signalling
R-HSA-500792GPCR ligand binding

MSigDB gene sets: 29 (showing top): REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOMF_PEPTIDE_RECEPTOR_ACTIVITY, MULLIGHAN_NPM1_SIGNATURE_3_DN, chr13q14, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, REACTOME_G_ALPHA_Q_SIGNALLING_EVENTS, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, MULLIGHAN_NPM1_MUTATED_SIGNATURE_1_DN, MARTENS_TRETINOIN_RESPONSE_UP, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GSE13411_NAIVE_VS_SWITCHED_MEMORY_BCELL_UP, WP_GPCRS_CLASS_A_RHODOPSINLIKE, ZBED5_TARGET_GENES

GO Biological Process (2): G protein-coupled receptor signaling pathway (GO:0007186), signal transduction (GO:0007165)

GO Molecular Function (3): G protein-coupled peptide receptor activity (GO:0008528), hormone binding (GO:0042562), G protein-coupled receptor activity (GO:0004930)

GO Cellular Component (3): cytosol (GO:0005829), plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

CategoryPathways
Signaling by GPCR2
Class A/1 (Rhodopsin-like receptors)1
GPCR downstream signalling1
Signal Transduction1
GPCR ligand binding1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
G protein-coupled receptor activity2
cellular anatomical structure2
signal transduction1
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
peptide receptor activity1
binding1
transmembrane signaling receptor activity1
G protein-coupled receptor signaling pathway1
cytoplasm1
membrane1
cell periphery1

Protein interactions and networks

STRING

480 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
MLNRMLNP12872994
MLNRGHRLQ9UBU3680
MLNRCAB39LQ9H9S4649
MLNRFNDC3AQ9Y2H6649
MLNRCDADC1Q9BWV3589
MLNRSETDB2Q96T68541
MLNRRCBTB1Q8NDN9534
MLNRPHF11Q9UIL8475
MLNRRCBTB2O95199460
MLNRITM2BQ9Y287458
MLNRGNAQP50148428
MLNRNTSP30990419
MLNRNMUP48645404
MLNRSPRYD7Q5W111390
MLNRUBA3Q8TBC4385

IntAct

10 interactions, top by confidence:

ABTypeScore
MLNRRAMP1psi-mi:“MI:0915”(physical association)0.400
RAMP2MLNRpsi-mi:“MI:0915”(physical association)0.400
MLNRRAMP3psi-mi:“MI:0915”(physical association)0.400
RAMP3MLNRpsi-mi:“MI:0915”(physical association)0.400
MLNRNBASpsi-mi:“MI:0914”(association)0.350
OR11G2MLNRpsi-mi:“MI:0914”(association)0.350

BioGRID (64): GHRL (Reconstituted Complex), ATM (Affinity Capture-MS), ATP12A (Affinity Capture-MS), RAB3A (Affinity Capture-MS), ADCK1 (Affinity Capture-MS), UFL1 (Affinity Capture-MS), ACAD10 (Affinity Capture-MS), HEATR1 (Affinity Capture-MS), SAAL1 (Affinity Capture-MS), IPO7 (Affinity Capture-MS), IPO8 (Affinity Capture-MS), GOLPH3 (Affinity Capture-MS), PDS5B (Affinity Capture-MS), NBAS (Affinity Capture-MS), STK17B (Affinity Capture-MS)

ESM2 similar proteins: A0A287A2K5, F1MV99, O08858, O43193, O77808, O97772, P28646, P30098, P30552, P30553, P30796, P30872, P30873, P30937, P30938, P31391, P32239, P32300, P32307, P32745, P33533, P35346, P35370, P35377, P41143, P41146, P46095, P46627, P47748, P48044, P49660, P51651, P56481, P58406, P79266, P79292, Q49LX5, Q5D0K2, Q6W5G4, Q6YNI2

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

7 interactions.

AEffectBMechanism
MLNR“up-regulates activity”GNAI1binding
MLNR“up-regulates activity”GNAI3binding
MLNR“up-regulates activity”GNAQbinding
MLNR“up-regulates activity”GNA14binding
MLNR“up-regulates activity”GNA12binding
Motilin“up-regulates activity”MLNR“chemical activation”
MLNup-regulatesMLNRbinding

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 significance58
Likely benign3
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

447 predictions. Top by Δscore:

VariantEffectΔscore
13:49222038:A:AGacceptor_gain1.0000
13:49222038:AGT:Aacceptor_gain1.0000
13:49222039:G:GGacceptor_gain1.0000
13:49222039:GTG:Gacceptor_gain1.0000
13:49221237:GC:Gdonor_gain0.9900
13:49221239:G:GGdonor_gain0.9900
13:49222039:GT:Gacceptor_gain0.9800
13:49222039:GTGGT:Gacceptor_gain0.9800
13:49221307:C:Gdonor_gain0.9700
13:49221235:CTGC:Cdonor_gain0.9500
13:49221236:TGC:Tdonor_gain0.9500
13:49221236:TGCGT:Tdonor_loss0.9500
13:49221237:GCG:Gdonor_gain0.9500
13:49221238:CGTAA:Cdonor_loss0.9500
13:49221239:GTAA:Gdonor_loss0.9500
13:49221240:T:TCdonor_loss0.9500
13:49221241:A:ATdonor_loss0.9500
13:49221242:A:ACdonor_loss0.9500
13:49221243:G:Cdonor_loss0.9400
13:49222033:GTTGC:Gacceptor_loss0.9200
13:49222034:TTGCA:Tacceptor_loss0.9200
13:49222035:TGCAG:Tacceptor_loss0.9200
13:49222036:GCAGT:Gacceptor_loss0.9200
13:49222037:CAGT:Cacceptor_loss0.9200
13:49222038:A:Tacceptor_loss0.9200
13:49222038:AGTG:Aacceptor_gain0.9200
13:49222039:GTGG:Gacceptor_gain0.9200
13:49222025:T:TAacceptor_loss0.9100
13:49222083:C:Gacceptor_gain0.9100
13:49221527:A:Tdonor_gain0.9000

AlphaMissense

2596 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
13:49220572:A:CS79R0.996
13:49220574:C:AS79R0.996
13:49220574:C:GS79R0.996
13:49222177:A:CS347R0.993
13:49222179:C:AS347R0.993
13:49222179:C:GS347R0.993
13:49220734:A:CS133R0.991
13:49220736:C:AS133R0.991
13:49220736:C:GS133R0.991
13:49220588:A:TD84V0.990
13:49220649:G:CW104C0.990
13:49220649:G:TW104C0.990
13:49220824:T:AW163R0.990
13:49220824:T:CW163R0.990
13:49220588:A:CD84A0.987
13:49222057:T:CF307L0.987
13:49222059:T:AF307L0.987
13:49222059:T:GF307L0.987
13:49222066:T:CC310R0.987
13:49222078:T:CF314L0.987
13:49222080:C:AF314L0.987
13:49222080:C:GF314L0.987
13:49222193:C:AP352Q0.987
13:49220505:C:AN56K0.986
13:49220505:C:GN56K0.986
13:49220491:G:AG52R0.985
13:49220491:G:CG52R0.985
13:49222068:C:GC310W0.984
13:49220632:T:AW99R0.983
13:49220632:T:CW99R0.983

dbSNP variants (sampled 300 via entrez): RS1000320863 (13:49222801 T>G), RS1001521180 (13:49222070 G>A), RS1002393036 (13:49221307 C>A), RS1002551915 (13:49220694 G>A,C), RS1002730919 (13:49221541 T>G), RS1003013052 (13:49219195 T>C), RS1003322299 (13:49220251 C>A,G,T), RS1003521232 (13:49218731 G>A), RS1003804987 (13:49220137 A>C), RS1003960417 (13:49219034 C>T), RS1004122761 (13:49220270 C>G,T), RS1004892819 (13:49221473 G>A,C), RS1005466875 (13:49222004 C>A), RS1005891869 (13:49219854 G>A), RS1006397695 (13:49219494 C>T)

Disease associations

OMIM: gene MIM:602885 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2203 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

76 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 325,043 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL1008BEPRIDIL411,776
CHEMBL1014CANDESARTAN CILEXETIL411,194
CHEMBL1078261PROPIVERINE44,890
CHEMBL1085ACETOPHENAZINE45,134
CHEMBL111RIMONABANT415,726
CHEMBL1112ARIPIPRAZOLE424,205
CHEMBL1159650CLOBETASOL PROPIONATE430,865
CHEMBL116AMPRENAVIR429,221
CHEMBL1163ATAZANAVIR422,094
CHEMBL1171837PONATINIB48,955
CHEMBL1175DULOXETINE428,527
CHEMBL1198857VILANTEROL42,552
CHEMBL1200848HYDROXYPROGESTERONE CAPROATE416,548
CHEMBL1201284CINACALCET45,917
CHEMBL1201303PYRVINIUM41,797
CHEMBL1201304INDOCYANINE GREEN ACID FORM47,044
CHEMBL1201309NAFARELIN4
CHEMBL12713SERTINDOLE48,984
CHEMBL1287853FEDRATINIB43,554
CHEMBL1336SORAFENIB486,060
CHEMBL1401NITAZOXANIDE4
CHEMBL1423PIMOZIDE4
CHEMBL14370REBOXETINE4
CHEMBL146095GLAFENINE4
CHEMBL1617RIFAXIMIN4
CHEMBL1626CLEMASTINE4
CHEMBL163RITONAVIR4
CHEMBL1648ISRADIPINE4
CHEMBL1651990FENTICONAZOLE4
CHEMBL1729CISAPRIDE4

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Motilin receptor

Most potent curated ligand interactions (29 total), top 25:

LigandActionAffinityParameter
[125I]motilin (human)Full agonist10.0pKd
motilinFull agonist9.7pIC50
[nLeu13,Glu14]motilin (human)Full agonist9.5pIC50
motilin-(1-13) (human)Full agonist9.5pIC50
motilin-(1-19) (human)Full agonist9.5pIC50
motilinFull agonist9.3pIC50
MA-2029Antagonist9.2pA2
[Leu13]motilin (human)Full agonist9.0pIC50
motilin-(1-12) (human)Full agonist9.0pIC50
[Phe3,Leu13]motilin (human)Full agonist8.9pIC50
motilinFull agonist8.7pKi
DS-3801b free baseAgonist8.28pEC50
camicinalFull agonist7.9pEC50
[Bpa1,Ile13]motilin (human)Full agonist7.9pKi
mitemcinalFull agonist7.8pEC50
motilin-(2-22) (human)Full agonist7.5pIC50
GM-109Antagonist7.5pA2
[L-Bpa5,Ile13]motilin (human)Full agonist7.3pKi
KOS1326Full agonist7.2pIC50
alemcinalFull agonist7.2pIC50
motilin-(1-11) (human)Full agonist6.8pIC50
EM-523Full agonist6.6pIC50
ME67Full agonist6.5pIC50
erythromycinFull agonist6.5pIC50
[D-Bpa5,Ile13]motilin (human)Full agonist6.4pKi

ChEMBL bioactivities

349 potent at pChembl≥5 of 399 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
10.40EC500.03981nMCHEMBL525634
10.33EC500.047nMCHEMBL297494
9.82EC500.15nMMOTILIN
9.66EC500.22nMCHEMBL296748
9.60EC500.2512nMCHEMBL2364292
9.60EC500.2512nMCHEMBL2364312
9.50EC500.3162nMCHEMBL2364317
9.46EC500.35nMCHEMBL297494
9.44Ki0.36nMMOTILIN
9.40EC500.3981nMCHEMBL2364285
9.40EC500.3981nMCHEMBL2364318
9.20EC500.631nMCHEMBL2364282
9.15Ki0.7nMCHEMBL297494
9.10EC500.7943nMCHEMBL2364302
9.10EC500.7943nMCHEMBL2364330
9.01EC500.97nMCHEMBL525634
9.00Ki1nMCHEMBL297494
9.00EC501nMCHEMBL2364297
9.00EC501nMCHEMBL2364326
8.90EC501.259nMCHEMBL2364281
8.90EC501.259nMCHEMBL2364301
8.90EC501.259nMCHEMBL2364329
8.80EC501.585nMCHEMBL2364277
8.80EC501.585nMCHEMBL2364284
8.80EC501.585nMCHEMBL2364288
8.80EC501.585nMCHEMBL2364315
8.80EC501.585nMCHEMBL2364320
8.80EC501.6nMCHEMBL5192530
8.74EC501.8nMCHEMBL5179573
8.70Ki2nMCHEMBL296748
8.70EC501.995nMCHEMBL2364286
8.70EC501.995nMCHEMBL2364299
8.70EC501.995nMCHEMBL2364321
8.70EC501.995nMCHEMBL2364323
8.70IC502nMCHEMBL393315
8.70EC502nMCHEMBL5179543
8.70EC501.995nMCHEMBL465917
8.68EC502.1nMCHEMBL5187928
8.60EC502.512nMCHEMBL2364276
8.60EC502.512nMCHEMBL2364283
8.60EC502.512nMCHEMBL2364328
8.60EC502.512nMCHEMBL518618
8.60EC502.512nMCHEMBL1080046
8.59EC502.6nMCHEMBL5192584
8.58Ki2.63nMCHEMBL2313632
8.57Ki2.7nMCHEMBL298224
8.52IC503nMCHEMBL233711
8.51Ki3.1nMMOTILIN
8.50EC503.162nMCHEMBL2364275
8.50EC503.162nMCHEMBL2364295

PubChem BioAssay actives

236 with measured affinity, of 1636 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
N-[(2S)-1-[[(2S)-1-amino-1-oxo-4-phenylbutan-2-yl]amino]-1-oxo-4-phenylbutan-2-yl]-2-(1,3-benzodioxol-5-ylmethyl)-1,3-dioxospiro[7,8-dihydro-6H-[1,2,4]triazolo[1,2-a]pyridazine-5,4’-piperidine]-8-carboxamide125429: In vitro effective concentration towards human motilin receptorec50<0.0001uM
(2S)-5-amino-2-[[2-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-oxopentanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]acetyl]amino]-5-oxopentanoic acid347506: Agonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assayec50<0.0001uM
(2S)-5-amino-2-[[2-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2R)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-oxopentanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]acetyl]amino]-5-oxopentanoic acid125429: In vitro effective concentration towards human motilin receptorec500.0001uM
N-[(2S)-1-[[(2S)-1-amino-1-oxo-4-phenylbutan-2-yl]amino]-1-oxo-4-phenylbutan-2-yl]-2-(1,3-benzodioxol-5-ylmethyl)-1,3-dioxospiro[8H-[1,2,4]triazolo[1,2-a]pyridazine-5,4’-piperidine]-8-carboxamide125429: In vitro effective concentration towards human motilin receptorec500.0002uM
N-methyl-N-[3-methyl-4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]-4-[3-[2-oxo-2-(propan-2-ylamino)ethyl]phenoxy]cyclohexane-1-carboxamide1889088: Agonist activity at human GPR38 expressed in COS-7 cellsec500.0016uM
4-[4-chloro-3-(hydroxymethyl)phenoxy]-N-methyl-N-[3-methyl-4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]cyclohexane-1-carboxamide1889088: Agonist activity at human GPR38 expressed in COS-7 cellsec500.0018uM
[4-(3,4-difluoroanilino)piperidin-1-yl]-[3-[4-[[(3S,5R)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]-2-pyridinyl]methanone411908: Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assayec500.0020uM
(6R,9R,12S)-9-propan-2-yl-12-(pyrrolidin-1-ylmethyl)-6-[[3-(trifluoromethyl)phenyl]methyl]-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione299537: Antagonist activity against human motilin receptor in aequoscreen cells assessed as inhibition of motilin induced calcium release by aequorin assayic500.0020uM
N-[3-chloro-4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]-4-(4-fluorophenoxy)-N-methylcyclohexane-1-carboxamide1889088: Agonist activity at human GPR38 expressed in COS-7 cellsec500.0020uM
4-(4-fluorophenoxy)-N-methyl-N-[3-methyl-4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]cyclohexane-1-carboxamide1889088: Agonist activity at human GPR38 expressed in COS-7 cellsec500.0021uM
[2-[4-[[(3R,5S)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]phenyl]-[4-(4-fluoroanilino)piperidin-1-yl]methanone411908: Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assayec500.0025uM
4-butyl-N-[3-(1H-pyrazol-5-ylmethyl)-1,2,4,5-tetrahydro-3-benzazepin-7-yl]benzenesulfonamide471696: Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assayec500.0025uM
(2R,5S)-3-amino-2-[(3-tert-butyl-4-hydroxyphenyl)methyl]-N-ethyl-5-[[(2S)-3-(4-fluorophenyl)-2-(methylamino)propanoyl]-methylamino]-6-methyl-4-oxoheptanamide;hydrochloride723497: Agonist activity at MLNR (unknown origin)ki0.0026uM
4-[3-(ethoxymethyl)anilino]-N-methyl-N-[3-methyl-4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]cyclohexane-1-carboxamide1889088: Agonist activity at human GPR38 expressed in COS-7 cellsec500.0026uM
N-[(2R)-1-[[(2R)-1-amino-1-oxo-4-phenylbutan-2-yl]amino]-1-oxo-4-phenylbutan-2-yl]-2-(1,3-benzodioxol-5-ylmethyl)-1,3-dioxospiro[7,8-dihydro-6H-[1,2,4]triazolo[1,2-a]pyridazine-5,4’-piperidine]-8-carboxamide125430: In vitro binding affinity towards human motilin receptorki0.0027uM
(6R,9R,12S)-12-(methylaminomethyl)-9-propan-2-yl-6-[[3-(trifluoromethyl)phenyl]methyl]-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione299537: Antagonist activity against human motilin receptor in aequoscreen cells assessed as inhibition of motilin induced calcium release by aequorin assayic500.0030uM
N-[[2-[4-[[(3R,5S)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]phenyl]methyl]-N-methyl-2-phenylsulfanylacetamide411908: Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assayec500.0032uM
4-butyl-N-[3-[(5-methyl-1H-imidazol-4-yl)methyl]-1,2,4,5-tetrahydro-3-benzazepin-7-yl]benzenesulfonamide471696: Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assayec500.0032uM
(2R,3S,4R,5R,8R,9S,10S,11R,12R)-5-ethyl-11-[(2S,3R,4S,6R)-4-[ethyl(methyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-3-hydroxy-9-[(2S,4S,6R)-4-methoxy-4,6-dimethyloxan-2-yl]oxy-2,4,8,10,12,14-hexamethyl-6,15-dioxabicyclo[10.2.1]pentadec-1(14)-en-7-one125430: In vitro binding affinity towards human motilin receptorki0.0034uM
3-[[1-[2-[4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]acetyl]piperidin-4-yl]amino]benzonitrile347506: Agonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assayec500.0040uM
[3-[4-[[(3R,5S)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]-2-pyridinyl]-[4-(4-fluoroanilino)piperidin-1-yl]methanone347506: Agonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assayec500.0040uM
[3-[4-[[(3R,5S)-3,5-dimethylpiperazin-1-yl]methyl]-3-fluorophenyl]-2-pyridinyl]-[4-(4-fluoroanilino)piperidin-1-yl]methanone411908: Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assayec500.0040uM
(2S,4R,5R,8R,9S,10S,11R,12S)-5-ethyl-9-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-11-[(2S,3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-4-methoxy-2,4,8,10,12,14-hexamethyl-6,15-dioxabicyclo[10.2.1]pentadec-1(14)-ene-3,7-dione723495: Antagonist activity at MLNR (unknown origin)ic500.0040uM
4-propan-2-yloxy-N-[3-(1H-pyrazol-5-ylmethyl)-1,2,4,5-tetrahydro-3-benzazepin-7-yl]benzenesulfonamide471696: Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assayec500.0040uM
4-[3-(2-hydroxy-2-methylpropyl)phenoxy]-N-methyl-N-[3-methyl-4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]cyclohexane-1-carboxamide1889088: Agonist activity at human GPR38 expressed in COS-7 cellsec500.0043uM
4-[(5-fluoro-2-pyridinyl)oxy]-N-methyl-N-[3-methyl-4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]cyclohexane-1-carboxamide1889088: Agonist activity at human GPR38 expressed in COS-7 cellsec500.0046uM
4-[3-(2-hydroxyethyl)phenoxy]-N-methyl-N-[3-methyl-4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]cyclohexane-1-carboxamide1889088: Agonist activity at human GPR38 expressed in COS-7 cellsec500.0047uM
[3-[4-[[(3S,5R)-3,5-dimethylpiperazin-1-yl]methyl]-3-methoxyphenyl]-2-pyridinyl]-[4-(4-fluoroanilino)piperidin-1-yl]methanone411908: Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assayec500.0050uM
(4-anilinopiperidin-1-yl)-[2-[4-[[(3S,5R)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]phenyl]methanone411908: Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assayec500.0050uM
2,2-dimethyl-N-[3-(1H-pyrazol-5-ylmethyl)-1,2,4,5-tetrahydro-3-benzazepin-7-yl]-3,4-dihydrochromene-6-sulfonamide471696: Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assayec500.0050uM
7-[[6-(4-fluorophenyl)-3-pyridinyl]sulfonylmethyl]-2,3,4,5-tetrahydro-1H-3-benzazepine471696: Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assayec500.0050uM
4-[3-(hydroxymethyl)phenoxy]-N-methyl-N-[3-methyl-4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]cyclohexane-1-carboxamide1889088: Agonist activity at human GPR38 expressed in COS-7 cellsec500.0053uM
4-[5-(hydroxymethyl)-2-methylphenoxy]-N-methyl-N-[3-methyl-4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]cyclohexane-1-carboxamide1889088: Agonist activity at human GPR38 expressed in COS-7 cellsec500.0056uM
2-[[(6R,9R,12S)-6-[(4-chlorophenyl)methyl]-7,10,13-trioxo-9-propan-2-yl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-trien-12-yl]methyl]guanidine299536: Displacement of [125I]motilin from human motilin receptor expressed in CHO cellski0.0060uM
2-[[(6R,9R,12S)-7,10,13-trioxo-9-propan-2-yl-6-[[3-(trifluoromethyl)phenyl]methyl]-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-trien-12-yl]methyl]guanidine299536: Displacement of [125I]motilin from human motilin receptor expressed in CHO cellski0.0060uM
[3-[4-[[(3S,5R)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]-2-pyridinyl]-[4-(3-fluoroanilino)piperidin-1-yl]methanone411908: Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assayec500.0063uM
6-morpholin-4-yl-N-[3-(1H-pyrazol-5-ylmethyl)-1,2,4,5-tetrahydro-3-benzazepin-7-yl]pyridine-3-sulfonamide471696: Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assayec500.0063uM
4-[4-fluoro-3-(hydroxymethyl)phenoxy]-N-methyl-N-[3-methyl-4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]cyclohexane-1-carboxamide1889088: Agonist activity at human GPR38 expressed in COS-7 cellsec500.0075uM
2-[4-[[(3R,5S)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]-N-ethyl-N-(2-phenylethyl)benzamide411908: Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assayec500.0079uM
N-[3-(1H-pyrazol-5-ylmethyl)-1,2,4,5-tetrahydro-3-benzazepin-7-yl]-5-pyridin-2-ylthiophene-2-sulfonamide471696: Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assayec500.0079uM
4-butyl-N-[3-(1H-imidazol-5-ylmethyl)-1,2,4,5-tetrahydro-3-benzazepin-7-yl]benzenesulfonamide471696: Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assayec500.0079uM
7-[[6-(4-chlorophenyl)-3-pyridinyl]sulfonylmethyl]-2,3,4,5-tetrahydro-1H-3-benzazepine471696: Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assayec500.0079uM
(6R,9R,12S)-6-[(4-methoxyphenyl)methyl]-9-propan-2-yl-12-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione272565: Displacement of [125I]motilin from human MOTRki0.0080uM
(6R,9R,12S)-12-(aminomethyl)-9-propan-2-yl-6-[[3-(trifluoromethyl)phenyl]methyl]-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione299537: Antagonist activity against human motilin receptor in aequoscreen cells assessed as inhibition of motilin induced calcium release by aequorin assayic500.0080uM
(6R,9R,12S)-6-(naphthalen-1-ylmethyl)-9-propan-2-yl-12-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione272565: Displacement of [125I]motilin from human MOTRki0.0083uM
[3-[4-[[(3S,5R)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]-2-pyridinyl]-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]methanone411908: Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assayec500.0100uM
1-[4-(4-fluoroanilino)piperidin-1-yl]-2-[4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]ethanone347506: Agonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assayec500.0100uM
[3-[4-[[(3S,5R)-3,5-dimethylpiperazin-1-yl]methyl]-3-fluorophenyl]-2-pyridinyl]-[4-(3-fluoroanilino)piperidin-1-yl]methanone411908: Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assayec500.0100uM
3-cyclohexyl-1-[[2-[4-[[(3S,5R)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]phenyl]methyl]-1-[2-(3-methoxyphenyl)ethyl]urea371528: Agonist activity at human recombinant motilin receptor expressed in CHO cells by calcium mobilization-based FLIPR assayec500.0100uM
2-(benzenesulfonyl)-N-[[2-[4-[[(3R,5S)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]phenyl]methyl]-N-methylacetamide411908: Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assayec500.0100uM

CTD chemical–gene interactions

14 total (human), top 14 by PubMed support.

ChemicalActions (top 5)PubMed papers
aminomethylphosphonic acid (AMPA)decreases expression1
bisphenol Adecreases methylation1
S-(1,2-dichlorovinyl)cysteineaffects cotreatment, decreases expression1
abrinedecreases expression1
N-(3-fluorophenyl)-1-((4-(((3S)-3-methyl-1-piperazinyl)methyl)phenyl)acetyl)-4-piperidinamineincreases activity, affects binding1
theaflavin-3,3’-digallateaffects expression1
Benzo(a)pyreneincreases methylation1
Diethylhexyl Phthalatedecreases expression1
Erythromycinincreases activity, affects binding1
Lipopolysaccharidesaffects cotreatment, decreases expression1
Tobacco Smoke Pollutionincreases expression1
Valproic Acidincreases methylation1
2,4-Dichlorophenoxyacetic Aciddecreases expression1
Antirheumatic Agentsdecreases expression1

ChEMBL screening assays

71 unique, capped per target: 51 binding, 20 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1000183BindingBinding affinity to motilin receptorSynthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. — J Med Chem
CHEMBL1008005FunctionalAgonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assayDiscovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. — J Med Chem

Cellosaurus cell lines

3 cell lines: 2 spontaneously immortalized cell line, 1 cancer cell line

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

CellosaurusNameCategorySex
CVCL_H468CHO-K1/MTLR/Galpha15Spontaneously immortalized cell lineFemale
CVCL_KY34PathHunter CHO-K1 MLNR beta-arrestinSpontaneously immortalized cell lineFemale
CVCL_LA83PathHunter U2OS MLNR Activated GPCR InternalizationCancer cell lineFemale

Clinical trials (associated diseases)

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

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

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This page pulls from 80 datasets indexed by BioBTree:

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