Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50302551
Substrate
n/a
Meas. Tech.
ChEMBL_594562 (CHEMBL1037057)
IC50
7.6±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:
BDBM50302551
Synonyms:
CHEMBL567950 | N-((cis)-4-(4-(dimethylamino)-6-methylpyrimidin-2-ylamino)cyclohexyl)-3-methoxybenzamide
Type:
Small organic molecule
Emp. Form.:
C21H29N5O2
Mol. Mass.:
383.4873
SMILES:
COc1cccc(c1)C(=O)N[C@H]1CC[C@H](CC1)Nc1nc(C)cc(n1)N(C)C |r,wU:11.11,14.18,(6.27,-16.52,;6.27,-14.98,;4.94,-14.2,;4.95,-12.66,;3.6,-11.89,;2.27,-12.66,;2.28,-14.19,;3.61,-14.97,;.95,-14.96,;.94,-16.5,;-.39,-14.19,;-1.72,-14.95,;-1.73,-16.49,;-3.06,-17.26,;-4.39,-16.48,;-4.4,-14.95,;-3.06,-14.18,;-5.72,-17.25,;-7.06,-16.48,;-8.39,-17.26,;-9.73,-16.49,;-11.06,-17.25,;-9.72,-14.94,;-8.4,-14.17,;-7.06,-14.93,;-8.4,-12.63,;-7.07,-11.86,;-9.74,-11.86,)|
Structure:
Search PDB for entries with ligand similarity: