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TargetMelanin-concentrating hormone receptor 1
LigandBDBM50094882
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1502789 (CHEMBL3591192)
IC50 1173±n/a nM
Citation Devasthale, PWang, WHernandez, ASMoore, FRenduchintala, KSridhar, RPelleymounter, MALonghi, DHuang, NFlynn, NAzzara, AVRohrbach, KDevenny, JRooney, SThomas, MGlick, SGodonis, HHarvey, SCullen, MJZhang, HCaporuscio, CStetsko, PGrubb, MHuang, CZhang, LFreeden, CLi, YXMurphy, BJRobl, JAWashburn, WN Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. Bioorg Med Chem Lett25:2793-9 (2015) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Melanin-concentrating hormone receptor 1
Name:Melanin-concentrating hormone receptor 1
Synonyms:G-protein coupled receptor 24 | GPR24 | MCH receptor 1 | MCH-1R | MCH-R1 | MCHR | MCHR-1 | MCHR1 | MCHR1_HUMAN | Melanin Concentrating Hormone 1 | Melanin-Concentrating Hormone Receptor 1 (MCH1R) | Melanin-concentrating hormone receptor | 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 | SLC1 | 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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BDBM50094882
n/a
NameBDBM50094882
Synonyms:CHEMBL3589135
TypeSmall organic molecule
Emp. Form.C22H22ClN3O4
Mol. Mass.427.881
SMILESCOc1cc(ccc1OCC(C)(C)O)N1Cc2cn(nc2C1=O)-c1ccc(Cl)cc1
Structure
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