Reaction Details
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Melanin-concentrating hormone receptor 1
Ligand
BDBM50170198
Substrate
n/a
Meas. Tech.
ChEMBL_306788 (CHEMBL832373)
IC50
9.5±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 More Info.:
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:
BDBM50170198
Synonyms:
N-[4-(4-Dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-fluoro-benzamide | CHEMBL362193
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)c2cccc(F)c2)nc2ccccc12 |wU:10.13,7.6,(1.73,2.57,;.4,1.79,;-.93,2.56,;.4,.25,;1.75,-.51,;1.76,-2.06,;3.09,-2.81,;4.42,-2.05,;5.76,-2.83,;7.09,-2.06,;7.09,-.52,;5.75,.25,;4.42,-.52,;8.43,.25,;9.76,-.52,;9.76,-2.06,;11.09,.25,;12.42,-.52,;13.75,.25,;13.75,1.79,;12.41,2.56,;12.41,4.1,;11.09,1.79,;.43,-2.83,;-.91,-2.06,;-2.26,-2.85,;-3.59,-2.08,;-3.59,-.54,;-2.26,.25,;-.91,-.52,)|
