Reaction Details Report a problem with these data
Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50302557
Substrate
n/a
Meas. Tech.
ChEMBL_594562 (CHEMBL1037057)
IC50
6±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:
BDBM50302557
Synonyms:
CHEMBL565551 | N-((cis)-4-(4-(dimethylamino)-5-methylpyrimidin-2-ylamino)cyclohexyl)-4-fluorobenzamide
Type:
Small organic molecule
Emp. Form.:
C20H26FN5O
Mol. Mass.:
371.4517
SMILES:
CN(C)c1nc(N[C@@H]2CC[C@@H](CC2)NC(=O)c2ccc(F)cc2)ncc1C |r,wU:10.13,7.6,(-7.01,-30.72,;-8.34,-31.5,;-9.67,-30.73,;-8.33,-33.04,;-7,-33.8,;-6.99,-35.35,;-5.66,-36.12,;-4.33,-35.35,;-2.99,-36.13,;-1.67,-35.36,;-1.66,-33.82,;-2.99,-33.05,;-4.33,-33.82,;-.32,-33.05,;1.01,-33.83,;1,-35.37,;2.34,-33.06,;3.67,-33.84,;5,-33.07,;5.01,-31.53,;6.34,-30.76,;3.67,-30.76,;2.34,-31.53,;-8.33,-36.12,;-9.66,-35.35,;-9.66,-33.81,;-11,-33.04,)|