Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50295690
Substrate
n/a
Meas. Tech.
ChEMBL_597858 (CHEMBL1039121)
IC50
0.36±n/a nM
Citation
 Suzuki, TKameda, MAndo, MMiyazoe, HSekino, EIto, SMasutani, KKamijo, KTakezawa, AMoriya, MIto, MIto, JNakase, KMatsushita, HIshihara, ATakenaga, NTokita, SKanatani, ASato, NFukami, T Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists. Bioorg Med Chem Lett 19:5339-45 (2009) [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:
BDBM50295690
Synonyms:
(+/-)-2-(3,4-difluorophenyl)-N-ethyl-N-(3-(6-fluoro-3H-spiro[isobenzofuran-1,4''-piperidine]-1''-yl)propyl)-2-(4-(methylsulfonyl)-2-oxopiperazin-1-yl)acetamide | 2-(3,4-difluorophenyl)-N-ethyl-N-(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)-2-(4-(methylsulfonyl)-2-oxopiperazin-1-yl)acetamide | CHEMBL538424 | CHEMBL538425
Type:
Small organic molecule
Emp. Form.:
C30H37F3N4O5S
Mol. Mass.:
622.699
SMILES:
CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc21)C(=O)C(N1CCN(CC1=O)S(C)(=O)=O)c1ccc(F)c(F)c1
Structure:
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