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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50170175
Substrate
n/a
Meas. Tech.
ChEMBL_306788 (CHEMBL832373)
IC50
35±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:
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:
BDBM50170175
Synonyms:
CHEMBL178084 | cis-N*2*-[4-(4-Bromo-2-trifluoromethoxy-benzylamino)-cyclohexyl]-N*4*,N*4*-dimethyl-quinazoline-2,4-diamine
Type:
Small organic molecule
Emp. Form.:
C24H27BrF3N5O
Mol. Mass.:
538.403
SMILES:
CN(C)c1nc(NC2CCC(CC2)NCc2ccc(Br)cc2OC(F)(F)F)nc2ccccc12 |(8.32,-4.94,;6.98,-5.71,;5.64,-4.94,;6.98,-7.26,;8.32,-8.03,;8.32,-9.57,;9.66,-10.37,;10.76,-9.27,;10.76,-10.8,;12.07,-11.57,;13.42,-10.81,;13.42,-9.27,;12.09,-8.5,;14.75,-11.58,;16.09,-12.35,;17.42,-11.57,;17.4,-10.04,;18.73,-9.26,;20.07,-10.02,;21.4,-9.24,;20.08,-11.56,;18.76,-12.35,;18.76,-13.89,;20.09,-14.66,;21.61,-14.08,;21.32,-15.35,;20.37,-16.23,;6.98,-10.34,;5.64,-9.57,;4.31,-10.34,;2.98,-9.57,;2.98,-8.04,;4.31,-7.26,;5.64,-8.03,)|
Structure:
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