Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50302569
Substrate
n/a
Meas. Tech.
ChEMBL_594562 (CHEMBL1037057)
IC50
4±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:
BDBM50302569
Synonyms:
3,5-dichloro-N-(((cis)-4-(4-(dimethylamino)-5-methylpyrimidin-2-ylamino)cyclohexyl)methyl)benzamide | CHEMBL569204
Type:
Small organic molecule
Emp. Form.:
C21H27Cl2N5O
Mol. Mass.:
436.378
SMILES:
CN(C)c1nc(N[C@@H]2CC[C@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)ncc1C |r,wU:7.6,10.10,(22.25,-24.15,;20.92,-24.93,;19.59,-24.16,;20.93,-26.47,;22.26,-27.23,;22.27,-28.78,;23.6,-29.55,;24.93,-28.78,;26.27,-29.56,;27.59,-28.79,;27.6,-27.25,;28.94,-26.48,;30.27,-27.26,;31.6,-26.49,;31.61,-24.95,;32.93,-27.26,;34.26,-26.49,;35.6,-27.26,;36.94,-26.49,;35.6,-28.81,;34.27,-29.57,;34.26,-31.11,;32.94,-28.79,;26.27,-26.48,;24.93,-27.25,;20.93,-29.55,;19.6,-28.78,;19.6,-27.24,;18.26,-26.47,)|
Structure:
Search PDB for entries with ligand similarity: