Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50186841
Substrate
n/a
Meas. Tech.
ChEMBL_376573 (CHEMBL866622)
Ki
3.6±n/a nM
Citation
 Wu, WLBurnett, DACaplen, MADomalski, MSBennett, CGreenlee, WJHawes, BEO'Neill, KWeig, BWeston, DSpar, BKowalski, T Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists. Bioorg Med Chem Lett 16:3674-8 (2006) [PubMed]  Article 
Target
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:
MSVGAMKKGVGRAVGLGGGSGCQATEEDPLPNCGACAPGQGGRRWRLPQPAWVEGSSARLWEQATGTGWMDLEASLLPTGPNASNTSDGPDNLTSAGSPPRTGSISYINIIMPSVFGTICLLGIIGNSTVIFAVVKKSKLHWCNNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHFGETMCTLITAMDANSQFTSTYILTAMAIDRYLATVHPISSTKFRKPSVATLVICLLWALSFISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVRILQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVYLYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRAVSNAQTADEERTESKGT
  
Inhibitor
Name:
BDBM50186841
Synonyms:
4'-[(5-fluoro-6-trifluoromethyl-1H-benzoimidazol-2-yl)-piperidin-4-ylidene-methyl]-biphenyl-3-carbonitrile | CHEMBL209993
Type:
Small organic molecule
Emp. Form.:
C27H20F4N4
Mol. Mass.:
476.4681
SMILES:
Fc1cc2[nH]c(nc2cc1C(F)(F)F)C(=C1CCNCC1)c1ccc(cc1)-c1cccc(c1)C#N |(25.89,-15.32,;25.13,-16.65,;23.6,-16.65,;22.83,-17.98,;21.33,-18.3,;21.17,-19.83,;22.58,-20.46,;23.6,-19.31,;25.13,-19.31,;25.9,-17.98,;27.44,-17.98,;28.98,-17.98,;27.44,-19.52,;27.44,-16.44,;19.84,-20.6,;19.84,-22.14,;18.5,-22.9,;18.5,-24.44,;19.83,-25.21,;21.17,-24.44,;21.17,-22.9,;18.5,-19.84,;17.17,-20.61,;15.83,-19.84,;15.83,-18.29,;17.16,-17.52,;18.5,-18.29,;14.5,-17.52,;13.18,-18.29,;11.84,-17.53,;11.84,-15.98,;13.17,-15.21,;14.5,-15.98,;13.16,-13.67,;13.16,-12.13,)|
Structure:
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