Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T09572
|
||||
Former ID |
TTDC00133
|
||||
Target Name |
Melanin-concentrating hormone receptor 1
|
||||
Gene Name |
MCHR1
|
||||
Synonyms |
G protein coupled receptor 24; MCH receptor1; MCH(1) receptor; MCH-1R; MCH-R1; MCH1R; MCHR; MCHR-1; Melanin-concentrating hormone receptor subtype 1; SLC-1; Somatostatinreceptor-like protein; MCHR1
|
||||
Target Type |
Clinical Trial
|
||||
Disease | Obesity [ICD9: 278; ICD10: E66] | ||||
Obesity; Anxiety; Depression [ICD9: 278, 300, 311; ICD10: E66, F32, F40-F42] | |||||
Function |
Receptor formelanin-concentrating hormone, coupled to both G proteins that inhibit adenylyl cyclase and G proteins that activate phosphoinositide hydrolysis.
|
||||
BioChemical Class |
GPCR rhodopsin
|
||||
Target Validation |
T09572
|
||||
UniProt ID | |||||
Sequence |
MSVGAMKKGVGRAVGLGGGSGCQATEEDPLPNCGACAPGQGGRRWRLPQPAWVEGSSARL
WEQATGTGWMDLEASLLPTGPNASNTSDGPDNLTSAGSPPRTGSISYINIIMPSVFGTIC LLGIIGNSTVIFAVVKKSKLHWCNNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHF GETMCTLITAMDANSQFTSTYILTAMAIDRYLATVHPISSTKFRKPSVATLVICLLWALS FISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVRI LQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVY LYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRAVSNAQTADEERTESK GT |
||||
Drugs and Mode of Action | |||||
Drug(s) | AZD1979 | Drug Info | Phase 1 | Obesity | [524658] |
BMS-830216 | Drug Info | Phase 1 | Obesity | [550384] | |
MCH antagonist | Drug Info | Preclinical | Obesity | [536122] | |
SNAP-7941 | Drug Info | Preclinical | Obesity; Anxiety; Depression | [536122], [538804] | |
T-226293 | Drug Info | Preclinical | Obesity | [536122] | |
T-226296 | Drug Info | Preclinical | Obesity | [536122], [538805] | |
AMG 076 | Drug Info | Discontinued in Phase 1 | Obesity | [547852] | |
NGD-4715 | Drug Info | Discontinued in Phase 1 | Obesity | [548402] | |
A-798 | Drug Info | Terminated | Obesity | [548089] | |
ALB-127158(a) | Drug Info | Terminated | Obesity | [550255] | |
Inhibitor | 2-phenyl-N,N-bis(o-tolylthiomethyl)ethanamine | Drug Info | [529257] | ||
8-(1,2-Dimethyl-propoxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(1,3,3-Trimethyl-butoxy)-quinolin-2-ylamine | Drug Info | [527195] | |||
8-(1-Ethyl-propoxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(1-Methyl-butoxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(2-Cyclopropyl-ethoxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(2-Ethoxy-1-methyl-ethoxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(2-Ethyl-1-methyl-butoxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(2-Methoxy-1-methyl-ethoxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(2-Methyl-butoxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(2-Methyl-cyclohexyloxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(3,3,3-trifluoropropoxy)quinolin-2-amine | Drug Info | [527194] | |||
8-(3,3-Dimethyl-butoxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(3-Methoxy-3-methyl-butoxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(3-Methyl-butoxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(3-Methyl-cyclohexyloxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(3-Methyl-cyclopentyloxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-(4-Methyl-cyclohexyloxy)-quinolin-2-ylamine | Drug Info | [527194] | |||
8-Butoxy-quinolin-2-ylamine | Drug Info | [527194] | |||
8-Cyclobutylmethoxy-quinolin-2-ylamine | Drug Info | [527194] | |||
8-Cycloheptyloxy-quinolin-2-ylamine | Drug Info | [527194] | |||
8-Cyclohexyloxy-quinolin-2-ylamine | Drug Info | [527194] | |||
8-Cyclopentylmethoxy-quinolin-2-ylamine | Drug Info | [527194] | |||
8-Hexyloxy-quinolin-2-ylamine | Drug Info | [527194] | |||
8-Isopropoxy-quinolin-2-ylamine | Drug Info | [527194] | |||
8-Methoxy-quinolin-2-ylamine | Drug Info | [527194] | |||
8-Pentyloxy-quinolin-2-ylamine | Drug Info | [527194] | |||
8-Propoxy-quinolin-2-ylamine | Drug Info | [527194] | |||
8-sec-Butoxy-quinolin-2-ylamine | Drug Info | [527194] | |||
A-224940 | Drug Info | [527196] | |||
ADS-102891 | Drug Info | [528581] | |||
ADS-103168 | Drug Info | [528581] | |||
ADS-103214 | Drug Info | [528581] | |||
ADS-103253 | Drug Info | [528581] | |||
ADS-103254 | Drug Info | [528581] | |||
ADS-103274 | Drug Info | [528581] | |||
ADS-103293 | Drug Info | [528581] | |||
ADS-103294 | Drug Info | [528581] | |||
ADS-103316 | Drug Info | [528581] | |||
AR-129330 | Drug Info | [527629] | |||
GNF-PF-1550 | Drug Info | [527713] | |||
GNF-PF-2322 | Drug Info | [527713] | |||
N,N-bis(tosylmethyl)hexan-1-amine | Drug Info | [529257] | |||
N-(1-benzylpiperidin-4-yl)-3,5-dimethoxybenzamide | Drug Info | [528347] | |||
N-(4-amino-2-propylquinolin-6-yl)cinnamamide | Drug Info | [528381] | |||
Phenyl-N,N-bis(tosylmethyl)methanamine | Drug Info | [529257] | |||
Antagonist | 4-arylphthalazin-1(2H)-3,4-Di-F | Drug Info | [531725] | ||
7-fluorochromone-2-carboxamide | Drug Info | [528492] | |||
A-798 | Drug Info | [532063] | |||
ALB-127158(a) | Drug Info | [550255] | |||
AMG 076 | Drug Info | [536531] | |||
ATC0065 | Drug Info | [527402] | |||
AZ13483342 | Drug Info | [528866] | |||
BMS-830216 | Drug Info | [550384] | |||
compound (R)-10h | Drug Info | [531871] | |||
compound 17 | Drug Info | [528543] | |||
compound 4b | Drug Info | [530316] | |||
GW803430 | Drug Info | [528336] | |||
MCH antagonist | Drug Info | [536122] | |||
MCHR1 antagonists | Drug Info | [543715] | |||
NGD-4715 | Drug Info | [550543] | |||
pyrrolidine MCHR1 antagonist 1 | Drug Info | [531400] | |||
SB-568849 | Drug Info | [528310] | |||
SNAP-7941 | Drug Info | [536122] | |||
T-226293 | Drug Info | [536122] | |||
T-226296 | Drug Info | [536122] | |||
tetralin_urea analogue (7o) | Drug Info | [528636] | |||
TPI-1361-17 | Drug Info | [543715] | |||
[3H]SNAP-7941 | Drug Info | [526378] | |||
Modulator | AZD1979 | Drug Info | [550345] | ||
Agonist | C3 | Drug Info | [526145] | ||
melanin-concentrating hormone | Drug Info | [526070] | |||
Modulator (allosteric modulator) | MQ1 | Drug Info | [532720] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
References | |||||
Ref 524658 | ClinicalTrials.gov (NCT02072993) A First Time in Man Study to Assess the Safety, Tolerability and Pharmacokinetics of AZD1979 in Healthy Males. U.S. National Institutes of Health. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 538804 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1313). | ||||
Ref 538805 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1314). | ||||
Ref 547852 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019931) | ||||
Ref 548089 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021828) | ||||
Ref 548402 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025311) | ||||
Ref 526070 | [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor. Br J Pharmacol. 2001 Jun;133(3):371-8. | ||||
Ref 526145 | SLC-1 receptor mediates effect of melanin-concentrating hormone on feeding behavior in rat: a structure-activity study. J Pharmacol Exp Ther. 2001 Oct;299(1):137-46. | ||||
Ref 526378 | Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist. Nat Med. 2002 Aug;8(8):825-30. Epub 2002 Jul 15. | ||||
Ref 527194 | Bioorg Med Chem Lett. 2004 Oct 4;14(19):4873-7.Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1. | ||||
Ref 527195 | Bioorg Med Chem Lett. 2004 Oct 4;14(19):4879-82.Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2. | ||||
Ref 527196 | Bioorg Med Chem Lett. 2004 Oct 4;14(19):4883-6.Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3. | ||||
Ref 527402 | Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists. J Pharmacol Exp Ther. 2005 May;313(2):831-9. Epub 2005 Jan 26. | ||||
Ref 527629 | Bioorg 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. | ||||
Ref 527713 | J 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. | ||||
Ref 528310 | Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4872-8. Epub 2006 Jul 12. | ||||
Ref 528336 | The discovery and optimization of pyrimidinone-containing MCH R1 antagonists. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4723-7. Epub 2006 Jul 25. | ||||
Ref 528347 | Bioorg 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. | ||||
Ref 528381 | Bioorg Med Chem Lett. 2006 Oct 15;16(20):5275-9. Epub 2006 Aug 17.4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists. | ||||
Ref 528492 | Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety. J Med Chem. 2006 Nov 2;49(22):6569-84. | ||||
Ref 528543 | 6-(4-chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-based melanin-concentrating hormone receptor 1 antagonist. J Med Chem. 2006 Nov 30;49(24):7108-18. | ||||
Ref 528581 | Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. Epub 2006 Dec 2.Quinazoline and benzimidazole MCH-1R antagonists. | ||||
Ref 528636 | Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1718-21. Epub 2006 Dec 24. | ||||
Ref 528866 | Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4232-41. Epub 2007 May 17. | ||||
Ref 529257 | J 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. | ||||
Ref 530316 | Bioorg Med Chem Lett. 2009 Sep 15;19(18):5339-45. Epub 2009 Aug 6.Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists. | ||||
Ref 531400 | Novel pyrrolidine melanin-concentrating hormone receptor 1 antagonists with reduced hERG inhibition. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2460-7. | ||||
Ref 531725 | 4-arylphthalazin-1(2H)-one derivatives as potent antagonists of the melanin concentrating hormone receptor 1 (MCH-R1). Bioorg Med Chem Lett. 2012 Jan 1;22(1):427-30. | ||||
Ref 531871 | Synthesis, structure-activity relationship, and pharmacological studies of novel melanin-concentrating hormone receptor 1 antagonists 3-aminomethylquinolines: reducing human ether-a-go-go-related gene (hERG) associated liabilities. J Med Chem. 2012 May 10;55(9):4336-51. | ||||
Ref 532063 | Disruption of the melanin-concentrating hormone receptor 1 (MCH1R) affects thyroid function. Endocrinology. 2012 Dec;153(12):6145-54. | ||||
Ref 532720 | The MCH(1) receptor, an anti-obesity target, is allosterically inhibited by 8-methylquinoline derivatives possessing subnanomolar binding and long residence times. Br J Pharmacol. 2014 Mar;171(5):1287-98. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 536531 | Stereoselective synthesis of a MCHr1 antagonist. J Org Chem. 2007 Dec 7;72(25):9648-55. Epub 2007 Nov 13. | ||||
Ref 543715 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 280). |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.