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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50120676
Substrate
n/a
Meas. Tech.
ChEMBL_1518192 (CHEMBL3619839)
Ki
2.4±n/a nM
Citation
 Devasthale, P; Wang, W; Mignone, J; Renduchintala, K; Radhakrishnan, S; Dhanapal, J; Selvaraj, J; Kuppusamy, R; Pelleymounter, MA; Longhi, D; Huang, N; Flynn, N; Azzara, AV; Rohrbach, K; Devenny, J; Rooney, S; Thomas, M; Glick, S; Godonis, H; Harvey, S; Cullen, MJ; Zhang, H; Caporuscio, C; Stetsko, P; Grubb, M; Huang, C; Zhang, L; Freeden, C; Murphy, BJ; Robl, JA; Washburn, 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]  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:
BDBM50120676
Synonyms:
CHEMBL3618340
Type:
Small organic molecule
Emp. Form.:
C24H24ClN3O6S
Mol. Mass.:
517.982
SMILES:
CCS(=O)(=O)C[C@@H](O)COc1ccc(cc1OC)-n1cnn2cc(cc2c1=O)-c1ccc(Cl)cc1 |r|
Structure:
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