Reaction Details Report a problem with these data
Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50170185
Substrate
n/a
Meas. Tech.
ChEMBL_306788 (CHEMBL832373)
IC50
38±n/a nM
Citation
 Kanuma, K; Omodera, K; Nishiguchi, M; Funakoshi, T; Chaki, S; Semple, G; Tran, TA; Kramer, B; Hsu, D; Casper, M; Thomsen, B; Sekiguchi, Y Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1. Bioorg Med Chem Lett 15:3853-6 (2005) [PubMed]  Article 
Target
Name:
Melanin-concentrating hormone receptor 1
Synonyms:
Somatostatin receptor-like protein | MCHR | Melanin-concentrating hormone receptor 1 (MCH-1) | Melanin-concentrating hormone receptor 1 (MCHR1) | MCH-1R | MCH-R1 | Melanin-concentrating hormone receptor 1 (MCHR-1) | Melanin Concentrating Hormone 1 | MCHR-1 | Melanin-concentrating hormone receptor 1 (MCH1) | G-protein coupled receptor 24 | MCH receptor 1 | SLC-1 | Melanin-Concentrating Hormone Receptor 1 (MCH1R) | MCHR1_HUMAN | MCHR1 | GPR24 | SLC1 | Melanin-concentrating hormone receptor
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
45976.27
Organism:
Human
Description:
Membranes from CHO-K1 cells stably expressing human MCH1R were used in assays.
Residue:
422
Sequence:
MSVGAMKKGVGRAVGLGGGSGCQATEEDPLPNCGACAPGQGGRRWRLPQPAWVEGSSARLWEQATGTGWMDLEASLLPTGPNASNTSDGPDNLTSAGSPPRTGSISYINIIMPSVFGTICLLGIIGNSTVIFAVVKKSKLHWCNNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHFGETMCTLITAMDANSQFTSTYILTAMAIDRYLATVHPISSTKFRKPSVATLVICLLWALSFISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVRILQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVYLYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRAVSNAQTADEERTESKGT
  
Inhibitor
Name:
BDBM50170185
Synonyms:
N-[4-(4-Dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-2,3,4-trifluoro-benzamide | CHEMBL360159
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
CN(C)c1nc(N[C@@H]2CC[C@@H](CC2)NC(=O)c2ccc(F)c(F)c2F)nc2ccccc12 |wU:10.13,7.6,(-4.15,2.37,;-2.8,1.6,;-1.47,2.38,;-2.79,.06,;-1.46,-.7,;-1.45,-2.25,;-.12,-2.99,;1.22,-2.24,;2.55,-3.02,;3.88,-2.25,;3.88,-.71,;2.55,.06,;1.21,-.71,;5.23,.06,;6.56,-.71,;6.56,-2.25,;7.89,.06,;9.22,-.71,;10.55,.06,;10.55,1.6,;11.88,2.37,;9.2,2.37,;9.2,3.91,;7.89,1.6,;6.54,2.37,;-2.78,-3.02,;-4.12,-2.25,;-5.45,-3.03,;-6.78,-2.26,;-6.78,-.72,;-5.45,.06,;-4.12,-.71,)|
Structure:
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