Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50302549
Substrate
n/a
Meas. Tech.
ChEMBL_594562 (CHEMBL1037057)
IC50
25±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:
BDBM50302549
Synonyms:
CHEMBL568664 | N-((cis)-4-(4-(dimethylamino)-6-methylpyrimidin-2-ylamino)cyclohexyl)-4-fluorobenzamide
Type:
Small organic molecule
Emp. Form.:
C20H26FN5O
Mol. Mass.:
371.4517
SMILES:
CN(C)c1cc(C)nc(N[C@@H]2CC[C@@H](CC2)NC(=O)c2ccc(F)cc2)n1 |r,wU:13.16,10.9,(9.73,-3.31,;8.4,-4.08,;7.06,-3.32,;8.4,-5.62,;7.08,-6.39,;7.07,-7.94,;5.74,-8.71,;8.41,-8.71,;9.74,-7.94,;11.08,-8.7,;12.41,-7.93,;13.74,-8.71,;15.07,-7.95,;15.08,-6.4,;13.74,-5.63,;12.4,-6.4,;16.41,-5.64,;17.75,-6.41,;17.74,-7.95,;19.08,-5.64,;20.41,-6.42,;21.74,-5.66,;21.75,-4.11,;23.08,-3.34,;20.4,-3.34,;19.07,-4.11,;9.74,-6.39,)|
Structure:
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