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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50163481
Substrate
n/a
Meas. Tech.
ChEMBL_1572136 (CHEMBL3796860)
IC50
16±n/a nM
Citation
 Igawa, H; Takahashi, M; Shirasaki, M; Kakegawa, K; Kina, A; Ikoma, M; Aida, J; Yasuma, T; Okuda, S; Kawata, Y; Noguchi, T; Yamamoto, S; Fujioka, Y; Kundu, M; Khamrai, U; Nakayama, M; Nagisa, Y; Kasai, S; Maekawa, T Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel 1-(1H-benzimidazol-6-yl)pyridin-2(1H)-one derivatives and design to avoid CYP3A4 time-dependent inhibition. Bioorg Med Chem 24:2486-503 (2016) [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:
BDBM50163481
Synonyms:
CHEMBL3794306
Type:
Small organic molecule
Emp. Form.:
C22H18F3N3O2S
Mol. Mass.:
445.457
SMILES:
Cn1c(nc2ccc(cc12)-n1ccc(OCc2ccc(s2)C(F)(F)F)cc1=O)C1CC1
Structure:
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