Reaction Details Report a problem with these data
Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50331242
Substrate
n/a
Meas. Tech.
ChEMBL_686508 (CHEMBL1292295)
Ki
4.2±n/a nM
Citation
Surman, MD; Freeman, EE; Grabowski, JF; Hadden, M; Henderson, AJ; Jiang, G; Jiang, XM; Luche, M; Khmelnitsky, Y; Vickers, S; Viggers, J; Cheetham, S; Guzzo, PR 5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists. Bioorg Med Chem Lett 20:7015-9 (2010) [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:
BDBM50331242
Synonyms:
2-(4-chloro-2-fluorophenyl)-5-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)furo[3,2-c]pyridin-4(5H)-one | CHEMBL1290602
Type:
Small organic molecule
Emp. Form.:
C26H22ClFN4O2
Mol. Mass.:
476.93
SMILES:
Fc1cc(Cl)ccc1-c1cc2c(ccn(-c3ccc4n(CCN5CCCC5)ncc4c3)c2=O)o1