Reaction Details Report a problem with these data
Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50170200
Substrate
n/a
Meas. Tech.
ChEMBL_306788 (CHEMBL832373)
IC50
6.8±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:
BDBM50170200
Synonyms:
CHEMBL181383 | N-[4-(4-Dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-nitro-benzamide
Type:
Small organic molecule
Emp. Form.:
C23H26N6O3
Mol. Mass.:
434.4909
SMILES:
CN(C)c1nc(N[C@@H]2CC[C@@H](CC2)NC(=O)c2cccc(c2)[N+]([O-])=O)nc2ccccc12 |wU:10.13,7.6,(-2.82,1.96,;-1.49,1.21,;-.16,1.98,;-1.47,-.33,;-.13,-1.1,;-.13,-2.64,;1.2,-3.41,;2.54,-2.64,;3.88,-3.41,;5.21,-2.64,;5.21,-1.1,;3.86,-.33,;2.53,-1.1,;6.54,-.33,;7.87,-1.1,;7.87,-2.64,;9.2,-.33,;10.55,-1.1,;11.88,-.33,;11.88,1.21,;10.53,1.98,;9.2,1.19,;10.53,3.52,;11.85,4.29,;9.19,4.27,;-1.46,-3.43,;-2.79,-2.66,;-4.13,-3.44,;-5.46,-2.67,;-5.46,-1.12,;-4.13,-.35,;-2.79,-1.12,)|
Structure:
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