Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50302559
Substrate
n/a
Meas. Tech.
ChEMBL_594562 (CHEMBL1037057)
IC50
2±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:
BDBM50302559
Synonyms:
CHEMBL578049 | N-(cis-4-{[4-(Dimethylamino)-5-methylpyrimidin-2-yl]amino}-cyclohexyl)-3,4-difluorobenzamide
Type:
Small organic molecule
Emp. Form.:
C20H25F2N5O
Mol. Mass.:
389.4422
SMILES:
CN(C)c1nc(N[C@@H]2CC[C@@H](CC2)NC(=O)c2ccc(F)c(F)c2)ncc1C |r,wU:10.13,7.6,(28.7,-29.71,;27.37,-30.48,;26.03,-29.71,;27.37,-32.02,;28.71,-32.78,;28.71,-34.33,;30.05,-35.1,;31.38,-34.33,;32.71,-35.11,;34.04,-34.34,;34.05,-32.8,;32.71,-32.03,;31.37,-32.8,;35.38,-32.04,;36.72,-32.81,;36.71,-34.35,;38.05,-32.04,;38.04,-30.51,;39.37,-29.74,;40.72,-30.51,;42.05,-29.74,;40.71,-32.05,;42.04,-32.83,;39.38,-32.82,;27.38,-35.11,;26.04,-34.34,;26.05,-32.79,;24.71,-32.02,)|
Structure:
Search PDB for entries with ligand similarity: