Target Information
| Target General Information | Top | |||||
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| Target ID |
T09572
(Former ID: TTDC00133)
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| Target Name |
Melanin-concentrating hormone receptor 1 (MCHR1)
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| Synonyms |
Somatostatinreceptor-like protein; Somatostatin receptor-like protein; SLC1; SLC-1; Melanin-concentrating hormone receptor subtype 1; MCHR-1; MCHR; MCH1R; MCH-R1; MCH-1R; MCH(1) receptor; MCH receptor1; MCH receptor 1; GPR24; G-protein coupled receptor 24; G protein coupled receptor 24
Click to Show/Hide
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| Gene Name |
MCHR1
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Obesity [ICD-11: 5B80-5B81] | |||||
| Function |
Receptor for melanin-concentrating hormone, coupled to both G proteins that inhibit adenylyl cyclase and G proteins that activate phosphoinositide hydrolysis.
Click to Show/Hide
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MSVGAMKKGVGRAVGLGGGSGCQATEEDPLPNCGACAPGQGGRRWRLPQPAWVEGSSARL
WEQATGTGWMDLEASLLPTGPNASNTSDGPDNLTSAGSPPRTGSISYINIIMPSVFGTIC LLGIIGNSTVIFAVVKKSKLHWCNNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHF GETMCTLITAMDANSQFTSTYILTAMAIDRYLATVHPISSTKFRKPSVATLVICLLWALS FISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVRI LQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVY LYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRAVSNAQTADEERTESK GT Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | AZD1979 | Drug Info | Phase 1 | Obesity | [2] | |
| 2 | BMS-830216 | Drug Info | Phase 1 | Obesity | [3] | |
| Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
| 1 | AMG 076 | Drug Info | Discontinued in Phase 1 | Obesity | [4] | |
| 2 | NGD-4715 | Drug Info | Discontinued in Phase 1 | Obesity | [5] | |
| 3 | A-798 | Drug Info | Terminated | Obesity | [9] | |
| 4 | ALB-127158(a) | Drug Info | Terminated | Obesity | [10] | |
| Preclinical Drug(s) | [+] 3 Preclinical Drugs | + | ||||
| 1 | SNAP-7941 | Drug Info | Preclinical | Depression | [6], [7] | |
| 2 | T-226293 | Drug Info | Preclinical | Obesity | [7] | |
| 3 | T-226296 | Drug Info | Preclinical | Obesity | [7], [8] | |
| Mode of Action | [+] 5 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | AZD1979 | Drug Info | [1] | |||
| Antagonist | [+] 70 Antagonist drugs | + | ||||
| 1 | BMS-830216 | Drug Info | [3] | |||
| 2 | PMID25522065-Compound-10 | Drug Info | [11] | |||
| 3 | PMID25522065-Compound-11 | Drug Info | [11] | |||
| 4 | PMID25522065-Compound-12 | Drug Info | [11] | |||
| 5 | PMID25522065-Compound-13 | Drug Info | [11] | |||
| 6 | PMID25522065-Compound-14 | Drug Info | [11] | |||
| 7 | PMID25522065-Compound-15 | Drug Info | [11] | |||
| 8 | PMID25522065-Compound-16 | Drug Info | [11] | |||
| 9 | PMID25522065-Compound-17 | Drug Info | [11] | |||
| 10 | PMID25522065-Compound-18 | Drug Info | [11] | |||
| 11 | PMID25522065-Compound-19 | Drug Info | [11] | |||
| 12 | PMID25522065-Compound-2 | Drug Info | [11] | |||
| 13 | PMID25522065-Compound-20 | Drug Info | [11] | |||
| 14 | PMID25522065-Compound-21 | Drug Info | [11] | |||
| 15 | PMID25522065-Compound-22 | Drug Info | [11] | |||
| 16 | PMID25522065-Compound-23 | Drug Info | [11] | |||
| 17 | PMID25522065-Compound-24 | Drug Info | [11] | |||
| 18 | PMID25522065-Compound-25 | Drug Info | [11] | |||
| 19 | PMID25522065-Compound-26 | Drug Info | [11] | |||
| 20 | PMID25522065-Compound-27 | Drug Info | [11] | |||
| 21 | PMID25522065-Compound-28 | Drug Info | [11] | |||
| 22 | PMID25522065-Compound-29 | Drug Info | [11] | |||
| 23 | PMID25522065-Compound-3 | Drug Info | [11] | |||
| 24 | PMID25522065-Compound-30 | Drug Info | [11] | |||
| 25 | PMID25522065-Compound-31 | Drug Info | [11] | |||
| 26 | PMID25522065-Compound-32 | Drug Info | [11] | |||
| 27 | PMID25522065-Compound-33 | Drug Info | [11] | |||
| 28 | PMID25522065-Compound-34 | Drug Info | [11] | |||
| 29 | PMID25522065-Compound-35 | Drug Info | [11] | |||
| 30 | PMID25522065-Compound-36 | Drug Info | [11] | |||
| 31 | PMID25522065-Compound-37 | Drug Info | [11] | |||
| 32 | PMID25522065-Compound-38 | Drug Info | [11] | |||
| 33 | PMID25522065-Compound-39 | Drug Info | [11] | |||
| 34 | PMID25522065-Compound-4 | Drug Info | [11] | |||
| 35 | PMID25522065-Compound-40 | Drug Info | [11] | |||
| 36 | PMID25522065-Compound-41 | Drug Info | [11] | |||
| 37 | PMID25522065-Compound-42 | Drug Info | [11] | |||
| 38 | PMID25522065-Compound-43 | Drug Info | [11] | |||
| 39 | PMID25522065-Compound-44 | Drug Info | [11] | |||
| 40 | PMID25522065-Compound-45 | Drug Info | [11] | |||
| 41 | PMID25522065-Compound-46 | Drug Info | [11] | |||
| 42 | PMID25522065-Compound-47 | Drug Info | [11] | |||
| 43 | PMID25522065-Compound-48 | Drug Info | [11] | |||
| 44 | PMID25522065-Compound-49 | Drug Info | [11] | |||
| 45 | PMID25522065-Compound-5 | Drug Info | [11] | |||
| 46 | PMID25522065-Compound-50 | Drug Info | [11] | |||
| 47 | PMID25522065-Compound-51 | Drug Info | [11] | |||
| 48 | PMID25522065-Compound-6 | Drug Info | [11] | |||
| 49 | PMID25522065-Compound-7 | Drug Info | [11] | |||
| 50 | PMID25522065-Compound-8 | Drug Info | [11] | |||
| 51 | PMID25522065-Compound-9 | Drug Info | [11] | |||
| 52 | AMG 076 | Drug Info | [12] | |||
| 53 | NGD-4715 | Drug Info | [13] | |||
| 54 | SNAP-7941 | Drug Info | [7] | |||
| 55 | T-226293 | Drug Info | [7] | |||
| 56 | T-226296 | Drug Info | [7] | |||
| 57 | A-798 | Drug Info | [14] | |||
| 58 | ALB-127158(a) | Drug Info | [10] | |||
| 59 | 4-arylphthalazin-1(2H)-3,4-Di-F | Drug Info | [16] | |||
| 60 | 7-fluorochromone-2-carboxamide | Drug Info | [17] | |||
| 61 | ATC0065 | Drug Info | [23] | |||
| 62 | AZ13483342 | Drug Info | [24] | |||
| 63 | GW803430 | Drug Info | [27] | |||
| 64 | PMID17125263C17 | Drug Info | [32] | |||
| 65 | PMID22490048C(R)-10h | Drug Info | [33] | |||
| 66 | pyrrolidine MCHR1 antagonist 1 | Drug Info | [34] | |||
| 67 | SB-568849 | Drug Info | [35] | |||
| 68 | tetralin_urea analogue (7o) | Drug Info | [36] | |||
| 69 | TPI-1361-17 | Drug Info | [37] | |||
| 70 | [3H]SNAP-7941 | Drug Info | [38] | |||
| Inhibitor | [+] 46 Inhibitor drugs | + | ||||
| 1 | 2-phenyl-N,N-bis(o-tolylthiomethyl)ethanamine | Drug Info | [15] | |||
| 2 | 8-(1,2-Dimethyl-propoxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 3 | 8-(1,3,3-Trimethyl-butoxy)-quinolin-2-ylamine | Drug Info | [19] | |||
| 4 | 8-(1-Ethyl-propoxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 5 | 8-(1-Methyl-butoxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 6 | 8-(2-Cyclopropyl-ethoxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 7 | 8-(2-Ethoxy-1-methyl-ethoxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 8 | 8-(2-Ethyl-1-methyl-butoxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 9 | 8-(2-Methoxy-1-methyl-ethoxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 10 | 8-(2-Methyl-butoxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 11 | 8-(2-Methyl-cyclohexyloxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 12 | 8-(3,3,3-trifluoropropoxy)quinolin-2-amine | Drug Info | [18] | |||
| 13 | 8-(3,3-Dimethyl-butoxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 14 | 8-(3-Methoxy-3-methyl-butoxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 15 | 8-(3-Methyl-butoxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 16 | 8-(3-Methyl-cyclohexyloxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 17 | 8-(3-Methyl-cyclopentyloxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 18 | 8-(4-Methyl-cyclohexyloxy)-quinolin-2-ylamine | Drug Info | [18] | |||
| 19 | 8-Butoxy-quinolin-2-ylamine | Drug Info | [18] | |||
| 20 | 8-Cyclobutylmethoxy-quinolin-2-ylamine | Drug Info | [18] | |||
| 21 | 8-Cycloheptyloxy-quinolin-2-ylamine | Drug Info | [18] | |||
| 22 | 8-Cyclohexyloxy-quinolin-2-ylamine | Drug Info | [18] | |||
| 23 | 8-Cyclopentylmethoxy-quinolin-2-ylamine | Drug Info | [18] | |||
| 24 | 8-Hexyloxy-quinolin-2-ylamine | Drug Info | [18] | |||
| 25 | 8-Isopropoxy-quinolin-2-ylamine | Drug Info | [18] | |||
| 26 | 8-Methoxy-quinolin-2-ylamine | Drug Info | [18] | |||
| 27 | 8-Pentyloxy-quinolin-2-ylamine | Drug Info | [18] | |||
| 28 | 8-Propoxy-quinolin-2-ylamine | Drug Info | [18] | |||
| 29 | 8-sec-Butoxy-quinolin-2-ylamine | Drug Info | [18] | |||
| 30 | A-224940 | Drug Info | [20] | |||
| 31 | ADS-102891 | Drug Info | [21] | |||
| 32 | ADS-103168 | Drug Info | [21] | |||
| 33 | ADS-103214 | Drug Info | [21] | |||
| 34 | ADS-103253 | Drug Info | [21] | |||
| 35 | ADS-103254 | Drug Info | [21] | |||
| 36 | ADS-103274 | Drug Info | [21] | |||
| 37 | ADS-103293 | Drug Info | [21] | |||
| 38 | ADS-103294 | Drug Info | [21] | |||
| 39 | ADS-103316 | Drug Info | [21] | |||
| 40 | AR-129330 | Drug Info | [22] | |||
| 41 | GNF-PF-1550 | Drug Info | [26] | |||
| 42 | GNF-PF-2322 | Drug Info | [26] | |||
| 43 | N,N-bis(tosylmethyl)hexan-1-amine | Drug Info | [15] | |||
| 44 | N-(1-benzylpiperidin-4-yl)-3,5-dimethoxybenzamide | Drug Info | [30] | |||
| 45 | N-(4-amino-2-propylquinolin-6-yl)cinnamamide | Drug Info | [31] | |||
| 46 | Phenyl-N,N-bis(tosylmethyl)methanamine | Drug Info | [15] | |||
| Agonist | [+] 2 Agonist drugs | + | ||||
| 1 | C3 | Drug Info | [25] | |||
| 2 | melanin-concentrating hormone | Drug Info | [28] | |||
| Modulator (allosteric modulator) | [+] 1 Modulator (allosteric modulator) drugs | + | ||||
| 1 | MQ1 | Drug Info | [29] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Degree | 1 | Degree centrality | 1.07E-04 | Betweenness centrality | 0.00E+00 |
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| Closeness centrality | 1.43E-04 | Radiality | 5.80E-03 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 2.00E+00 | Topological coefficient | 1.00E+00 | Eccentricity | 2 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
| 1 | Neuroactive ligand-receptor interaction | |||||
| Reactome | [+] 3 Reactome Pathways | + | ||||
| 1 | Peptide ligand-binding receptors | |||||
| 2 | G alpha (q) signalling events | |||||
| 3 | G alpha (i) signalling events | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | GPCRs, Class A Rhodopsin-like | |||||
| 2 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| 3 | GPCR ligand binding | |||||
| 4 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Phase I clinical trial of AZD1979 for treating obesity. AstraZeneca plc | |||||
| REF 2 | 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 3 | 2011 Pipeline of Bristol-Myers Squibb. | |||||
| REF 4 | 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 5 | 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 6 | URL: 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 7 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | |||||
| REF 8 | URL: 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 9 | 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 10 | Clinical pipeline report, company report or official report of Albany Molecular Research (2011). | |||||
| REF 11 | Novel MCH1 receptor antagonists: a patent review.Expert Opin Ther Pat. 2015 Feb;25(2):193-207. | |||||
| REF 12 | Stereoselective synthesis of a MCHr1 antagonist. J Org Chem. 2007 Dec 7;72(25):9648-55. | |||||
| REF 13 | CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. | |||||
| REF 14 | Disruption of the melanin-concentrating hormone receptor 1 (MCH1R) affects thyroid function. Endocrinology. 2012 Dec;153(12):6145-54. | |||||
| REF 15 | Discovery of novel chemotypes to a G-protein-coupled receptor through ligand-steered homology modeling and structure-based virtual screening. J Med Chem. 2008 Feb 14;51(3):581-8. | |||||
| REF 16 | 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 17 | 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 18 | Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4873-7. | |||||
| REF 19 | Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4879-82. | |||||
| REF 20 | Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4883-6. | |||||
| REF 21 | Quinazoline and benzimidazole MCH-1R antagonists. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. | |||||
| REF 22 | Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1. Bioorg Med Chem Lett. 2005 Sep 1;15(17):3853-6. | |||||
| REF 23 | Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagoni... J Pharmacol Exp Ther. 2005 May;313(2):831-9. | |||||
| REF 24 | 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. | |||||
| REF 25 | 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 26 | 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and ... J Med Chem. 2005 Sep 8;48(18):5684-97. | |||||
| REF 27 | The discovery and optimization of pyrimidinone-containing MCH R1 antagonists. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4723-7. | |||||
| REF 28 | [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor. Br J Pharmacol. 2001 Jun;133(3):371-8. | |||||
| REF 29 | 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 30 | Identification of substituted 4-aminopiperidines and 3-aminopyrrolidines as potent MCH-R1 antagonists for the treatment of obesity. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5445-50. | |||||
| REF 31 | 4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5275-9. | |||||
| REF 32 | 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 33 | 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 34 | Novel pyrrolidine melanin-concentrating hormone receptor 1 antagonists with reduced hERG inhibition. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2460-7. | |||||
| REF 35 | 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. | |||||
| REF 36 | Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1718-21. | |||||
| REF 37 | URL: 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). | |||||
| REF 38 | Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist. Nat Med. 2002 Aug;8(8):825-30. | |||||
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