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TargetMelanin-concentrating hormone receptor
LigandBDBM50120729
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1518192
Ki 6.5±n/a nM
Citation Devasthale PWang WMignone JRenduchintala KRadhakrishnan SDhanapal JSelvaraj JKuppusamy RPelleymounter MALonghi DHuang NFlynn NAzzara AVRohrbach KDevenny JRooney SThomas MGlick SGodonis HHarvey SCullen MJZhang HCaporuscio CStetsko PGrubb MHuang CZhang LFreeden CMurphy BJRobl JAWashburn WN Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies. Bioorg Med Chem Lett 25:4412-8 (2015) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Melanin-concentrating hormone receptor
Name:Melanin-concentrating hormone receptor
Synonyms:G-protein coupled receptor 24 | GPR24 | MCH receptor 1 | MCH-1R | MCH-R1 | MCHR | MCHR-1 | Melanin Concentrating Hormone 1 | Melanin-Concentrating Hormone Receptor 1 (MCH1R) | Melanin-concentrating hormone receptor 1 (MCH-1) | Melanin-concentrating hormone receptor 1 (MCH1) | Melanin-concentrating hormone receptor 1 (MCHR-1) | Melanin-concentrating hormone receptor 1 (MCHR1) | SLC-1 | Somatostatin receptor-like protein
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:45976.27
Organism:Homo sapiens (Human)
Description:Membranes from CHO-K1 cells stably expressing human MCH1R were used in assays.
Residue:422
Sequence:
MSVGAMKKGVGRAVGLGGGSGCQATEEDPLPNCGACAPGQGGRRWRLPQPAWVEGSSARL
WEQATGTGWMDLEASLLPTGPNASNTSDGPDNLTSAGSPPRTGSISYINIIMPSVFGTIC
LLGIIGNSTVIFAVVKKSKLHWCNNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHF
GETMCTLITAMDANSQFTSTYILTAMAIDRYLATVHPISSTKFRKPSVATLVICLLWALS
FISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVRI
LQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVY
LYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRAVSNAQTADEERTESK
GT
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BDBM50120729
n/a
NameBDBM50120729
Synonyms:CHEMBL3618345
TypeSmall organic molecule
Emp. Form.C23H19ClF2N4O4
Mol. Mass.488.871
SMILESCOc1cc(ccc1OCC1(O)CC(F)(F)C1)-n1cnn2cc(cc2c1=O)-c1ccc(Cl)cn1
Structure
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