Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50302548
Substrate
n/a
Meas. Tech.
ChEMBL_594562 (CHEMBL1037057)
IC50
6.5±n/a nM
Citation
 Semple, GTran, TAKramer, BHsu, DHan, SChoi, JVallar, PCasper, MDZou, NHauser, EKThomsen, WWhelan, KSengupta, DMorgan, MSekiguchi, YKanuma, KChaki, SGrottick, AJ Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. Bioorg Med Chem Lett 19:6166-71 (2009) [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:
BDBM50302548
Synonyms:
3-chloro-N-((cis)-4-(4-(dimethylamino)-6-methylpyrimidin-2-ylamino)cyclohexyl)benzamide | CHEMBL568663
Type:
Small organic molecule
Emp. Form.:
C20H26ClN5O
Mol. Mass.:
387.906
SMILES:
CN(C)c1cc(C)nc(N[C@@H]2CC[C@@H](CC2)NC(=O)c2cccc(Cl)c2)n1 |r,wU:13.16,10.9,(-8.21,-3.25,;-9.54,-4.02,;-10.88,-3.25,;-9.54,-5.56,;-10.87,-6.33,;-10.87,-7.88,;-12.22,-8.64,;-9.54,-8.65,;-8.2,-7.87,;-6.86,-8.64,;-5.53,-7.87,;-4.2,-8.65,;-2.87,-7.88,;-2.87,-6.34,;-4.2,-5.57,;-5.54,-6.34,;-1.53,-5.58,;-.2,-6.35,;-.2,-7.89,;1.14,-5.58,;1.13,-4.05,;2.46,-3.28,;3.8,-4.05,;3.8,-5.59,;5.13,-6.37,;2.46,-6.36,;-8.2,-6.32,)|
Structure:
Search PDB for entries with ligand similarity: