Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00133

Target Information
NameMelanin-concentrating hormone receptor 1    
Type of targetDiscontinued target    
SynonymsG protein coupled receptor 24    
MCH receptor 1    
MCH(1) receptor    
MCH-1R    
MCH-R1    
MCH1R    
MCHR    
MCHR-1    
MCHR1    
Melanin-concentrating hormone receptor subtype 1    
SLC-1    
Somatostatin receptor-like protein    
DiseaseObesity
[ICD9: 278   ICD10: E66]
[1][2]
Social anxiety disorder
[ICD9: 300   ICD10: F40-F42]
[2]
Vitiligo
[ICD9: 709.01   ICD10: L80]
[3]
Drug(s)ALB-127158(a)Phase IObesity[4]
BMS-830216Phase IObesity[5]
AMG 076Discontinued in Phase IObesity[1]
NGD-4715Discontinued in Phase IObesity[6]
MCH antagonistPreclinicalObesity[7]
SNAP-7941PreclinicalObesity, Anxiety, Depression[7]
T-226293PreclinicalObesity[7]
T-226296PreclinicalObesity[7]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDQ99705
FunctionReceptor for melanin-concentrating hormone, coupled to both G proteins that inhibit adenylyl cyclase and G proteins that activate phosphoinositide hydrolysis.    
SequenceMSVGAMKKGVGRAVGLGGGSGCQATEEDPLPNCGACAPGQGGRRWRLPQPAWVEGSSARL WEQATGTGWMDLEASLLPTGPNASNTSDGPDNLTSAGSPPRTGSISYINIIMPSVFGTIC LLGIIGNSTVIFAVVKKSKLHWCNNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHF GETMCTLITAMDANSQFTSTYILTAMAIDRYLATVHPISSTKFRKPSVATLVICLLWALS FISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVRI LQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVY LYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRAVSNAQTADEERTESK GT
Target ValidationClick to Find Target Validation Information.    
Inhibitor2-phenyl-N,N-bis (o-tolylthiomethyl)ethanamine[8]
8- (1,2-Dimethyl-propoxy)-quinolin-2-ylamine[9]
8- (1,3,3-Trimethyl-butoxy)-quinolin-2-ylamine[10]
8- (1-Ethyl-propoxy)-quinolin-2-ylamine[9]
8- (1-Methyl-butoxy)-quinolin-2-ylamine[9]
8- (2-Cyclopropyl-ethoxy)-quinolin-2-ylamine[9]
8- (2-Ethoxy-1-methyl-ethoxy)-quinolin-2-ylamine[9]
8- (2-Ethyl-1-methyl-butoxy)-quinolin-2-ylamine[9]
8- (2-Methoxy-1-methyl-ethoxy)-quinolin-2-ylamine[9]
8- (2-Methyl-butoxy)-quinolin-2-ylamine[9]
8- (2-Methyl-cyclohexyloxy)-quinolin-2-ylamine[9]
8- (3,3,3-trifluoropropoxy)quinolin-2-amine[9]
8- (3,3-Dimethyl-butoxy)-quinolin-2-ylamine[9]
8- (3-Methoxy-3-methyl-butoxy)-quinolin-2-ylamine[9]
8- (3-Methyl-butoxy)-quinolin-2-ylamine[9]
8- (3-Methyl-cyclohexyloxy)-quinolin-2-ylamine[9]
8- (3-Methyl-cyclopentyloxy)-quinolin-2-ylamine[9]
8- (4-Methyl-cyclohexyloxy)-quinolin-2-ylamine[9]
8-Butoxy-quinolin-2-ylamine[9]
8-Cyclobutylmethoxy-quinolin-2-ylamine[9]
8-Cycloheptyloxy-quinolin-2-ylamine[9]
8-Cyclohexyloxy-quinolin-2-ylamine[9]
8-Cyclopentylmethoxy-quinolin-2-ylamine[9]
8-Hexyloxy-quinolin-2-ylamine[9]
8-Isopropoxy-quinolin-2-ylamine[9]
8-Methoxy-quinolin-2-ylamine[9]
8-Pentyloxy-quinolin-2-ylamine[9]
8-Propoxy-quinolin-2-ylamine[9]
8-sec-Butoxy-quinolin-2-ylamine[9]
A-224940[11]
ADS-102891[12]
ADS-103168[12]
ADS-103214[12]
ADS-103253[12]
ADS-103254[12]
ADS-103274[12]
ADS-103293[12]
ADS-103294[12]
ADS-103316[12]
AR-129330[13]
AR-129330[14]
ATC-0175[15]
GNF-PF-1550[16]
GNF-PF-2322[16]
N,N-bis (tosylmethyl)hexan-1-amine[8]
N- (1-benzylpiperidin-4-yl)-3,5-dimethoxybenzamide[17]
N- (4-amino-2-propylquinolin-6-yl)cinnamamide[18]
phenyl-N,N-bis (tosylmethyl)methanamine[8]
AntagonistALB-127158 (a)[4]
AMG 076[1]
BMS-830216[5]
MCH antagonist[7]
NGD-4715[6]
SNAP-7941[7]
T-226293[7]
T-226296[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Stereoselective synthesis of a MCHr1 antagonist. J Org Chem. 2007 Dec 7;72(25):9648-55. Epub 2007 Nov 13. To Reference
Ref 2Molecular cloning and functional characterization of MCH2, a novel human MCH receptor. J Biol Chem. 2001 Jun 8;276(23):20125-9. Epub 2001 Mar 27. To Reference
Ref 3The melanin-concentrating hormone receptor 1, a novel target of autoantibody responses in vitiligo. J Clin Invest. 2002 Apr;109(7):923-30. To Reference
Ref 42011 Pipeline of Albany Molecular Research. To Reference
Ref 52011 Pipeline of Bristol-Myers Squibb. To Reference
Ref 6CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 7Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. To Reference
Ref 8J Med Chem. 2008 Feb 14;51(3):581-8. Epub 2008 Jan 17.Discovery of novel chemotypes to a G-protein-coupled receptor through ligand-steered homology modeling and structure-based virtual screening. To Reference
Ref 9Bioorg Med Chem Lett. 2004 Oct 4;14(19):4873-7.Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1. To Reference
Ref 10Bioorg Med Chem Lett. 2004 Oct 4;14(19):4879-82.Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2. To Reference
Ref 11Bioorg Med Chem Lett. 2004 Oct 4;14(19):4883-6.Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3. To Reference
Ref 12Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. Epub 2006 Dec 2.Quinazoline and benzimidazole MCH-1R antagonists. To Reference
Ref 13Bioorg Med Chem Lett. 2005 Sep 1;15(17):3853-6.Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1. To Reference
Ref 14Bioorg Med Chem Lett. 2005 May 16;15(10):2565-9.Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1. To Reference
Ref 15Bioorg Med Chem Lett. 2009 Nov 1;19(21):6166-71. Epub 2009 Sep 6.Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. To Reference
Ref 16J Med Chem. 2005 Sep 8;48(18):5684-97.6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode. To Reference
Ref 17Bioorg Med Chem Lett. 2006 Oct 15;16(20):5445-50. Epub 2006 Aug 1.Identification of substituted 4-aminopiperidines and 3-aminopyrrolidines as potent MCH-R1 antagonists for the treatment of obesity. To Reference
Ref 18Bioorg Med Chem Lett. 2006 Oct 15;16(20):5275-9. Epub 2006 Aug 17.4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists. To Reference



 

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