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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50120729
Substrate
n/a
Meas. Tech.
ChEMBL_1518193 (CHEMBL3619840)
Ki
6.5±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 | MCH1R | MCHR | MCHR-1 | MCHR1_RAT | Mchr1 | Melanin Concentrating Hormone 1 | Melanin-concentrating hormone receptor | Melanin-concentrating hormone receptor 1 | SLC-1 | Slc1 | Somatostatin receptor-like protein
Type:
Enzyme Catalytic Domain
Mol. Mass.:
39075.64
Organism:
RAT
Description:
Melanin Concentrating Hormone 1 GPR24 RAT::P97639
Residue:
353
Sequence:
MDLQTSLLSTGPNASNISDGQDNLTLPGSPPRTGSVSYINIIMPSVFGTICLLGIVGNSTVIFAVVKKSKLHWCSNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHFGETMCTLITAMDANSQFTSTYILTAMTIDRYLATVHPISSTKFRKPSMATLVICLLWALSFISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVKILQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVYLYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRTVSNAQTADEERTESKGT
  
Inhibitor
Name:
BDBM50120729
Synonyms:
CHEMBL3618345
Type:
Small organic molecule
Emp. Form.:
C23H19ClF2N4O4
Mol. Mass.:
488.871
SMILES:
COc1cc(ccc1OCC1(O)CC(F)(F)C1)-n1cnn2cc(cc2c1=O)-c1ccc(Cl)cn1
Structure:
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