Reaction Details Report a problem with these data
Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50170192
Substrate
n/a
Meas. Tech.
ChEMBL_306788 (CHEMBL832373)
IC50
4.9±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:
BDBM50170192
Synonyms:
cis-N*2*-{4-[(4-Bromo-2-trifluoromethoxy-benzylamino)-methyl]-cyclohexyl}-N*4*,N*4*-dimethyl-quinazoline-2,4-diamine | CHEMBL181466
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
CN(C)c1nc(NC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 |(9.05,-31.64,;7.7,-32.41,;6.37,-31.64,;7.7,-33.96,;9.05,-34.73,;9.05,-36.27,;10.39,-37.07,;11.49,-35.97,;11.48,-37.5,;12.8,-38.28,;14.15,-37.51,;15.48,-38.28,;16.81,-37.51,;18.14,-38.28,;19.48,-37.49,;19.46,-35.97,;20.79,-35.17,;22.13,-35.95,;23.46,-35.17,;22.14,-37.49,;20.82,-38.26,;20.82,-39.8,;22.15,-40.58,;23.67,-39.99,;23.38,-41.28,;22.42,-42.17,;14.15,-35.97,;12.81,-35.2,;7.7,-37.04,;6.37,-36.27,;5.03,-37.04,;3.7,-36.27,;3.7,-34.75,;5.03,-33.96,;6.37,-34.73,)|
Structure:
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