Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50184942
Substrate
n/a
Meas. Tech.
ChEMBL_342542 (CHEMBL861585)
Ki
161±n/a nM
Citation
 McBriar, MDGuzik, HShapiro, SParuchova, JXu, RPalani, AClader, JWCox, KGreenlee, WJHawes, BEKowalski, TJO'neill, KSpar, BDWeig, BWeston, DJFarley, CCook, 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:
BDBM50184942
Synonyms:
CHEMBL380692 | N'-(3-chloro-4-fluorophenyl)-N-[trans-3-(3-cyanophenyl)cyclopentyl]-N-[3-(4-methyl-1-piperazinyl)propyl]urea
Type:
Small organic molecule
Emp. Form.:
C27H33ClFN5O
Mol. Mass.:
498.035
SMILES:
CN1CCN(CCCN([C@@H]2CC[C@H](C2)c2cccc(c2)C#N)C(=O)Nc2ccc(F)c(Cl)c2)CC1
Structure:
Search PDB for entries with ligand similarity: