Reaction Details Report a problem with these data
Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50184921
Substrate
n/a
Meas. Tech.
ChEMBL_342542 (CHEMBL861585)
Ki
2.8±n/a nM
Citation
 McBriar, MD; Guzik, H; Shapiro, S; Paruchova, J; Xu, R; Palani, A; Clader, JW; Cox, K; Greenlee, WJ; Hawes, BE; Kowalski, TJ; O'neill, K; Spar, BD; Weig, B; Weston, DJ; Farley, C; Cook, J Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas. J Med Chem 49:2294-310 (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:
BDBM50184921
Synonyms:
CHEMBL204881 | N'-[4-fluoro-3-(trifluoromethyl)phenyl)-N-[trans-5-(4-methoxyphenyl)bicyclo[3.1.0]hex-2-yl]-N-[3-(4-methyl-1-piperazinyl)propyl]urea
Type:
Small organic molecule
Emp. Form.:
C29H36F4N4O2
Mol. Mass.:
548.6154
SMILES:
COc1ccc(cc1)[C@@]12C[C@@H]1[C@@H](CC2)N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(c1)C(F)(F)F
Structure:
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