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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50302556
Substrate
n/a
Meas. Tech.
ChEMBL_594562 (CHEMBL1037057)
IC50
13±n/a nM
Citation
Semple, G; Tran, TA; Kramer, B; Hsu, D; Han, S; Choi, J; Vallar, P; Casper, MD; Zou, N; Hauser, EK; Thomsen, W; Whelan, K; Sengupta, D; Morgan, M; Sekiguchi, Y; Kanuma, K; Chaki, S; Grottick, AJ Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. Bioorg Med Chem Lett 19:6166-71 (2009) [PubMed] Article
More Info.:
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:
BDBM50302556
Synonyms:
CHEMBL578170 | N-((cis)-4-(4-(dimethylamino)-5-methylpyrimidin-2-ylamino)cyclohexyl)-4-methylbenzamide
Type:
Small organic molecule
Emp. Form.:
C21H29N5O
Mol. Mass.:
367.4879
SMILES:
CN(C)c1nc(N[C@@H]2CC[C@@H](CC2)NC(=O)c2ccc(C)cc2)ncc1C |r,wU:10.13,7.6,(30.97,-21.81,;29.64,-22.58,;28.3,-21.82,;29.64,-24.12,;30.98,-24.89,;30.98,-26.44,;32.32,-27.21,;33.65,-26.43,;34.98,-27.21,;36.31,-26.45,;36.32,-24.91,;34.98,-24.13,;33.64,-24.9,;37.65,-24.14,;38.98,-24.91,;38.98,-26.45,;40.32,-24.15,;41.64,-24.92,;42.98,-24.16,;42.98,-22.62,;44.32,-21.85,;41.64,-21.84,;40.31,-22.61,;29.65,-27.21,;28.31,-26.44,;28.31,-24.89,;26.98,-24.13,)|