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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50171608
Substrate
n/a
Meas. Tech.
ChEMBL_321352 (CHEMBL881496)
IC50
20±n/a nM
Citation
Vasudevan, A; LaMarche, MJ; Blackburn, C; Che, JL; Luchaco-Cullis, CA; Lai, S; Marsilje, TH; Patane, MA; Souers, AJ; Wodka, D; Geddes, B; Chen, S; Brodjian, S; Falls, DH; Dayton, BD; Bush, E; Brune, M; Shapiro, RD; Marsh, KC; Hernandez, LE; Sham, HL; Collins, CA; Kym, PR Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists. Bioorg Med Chem Lett 15:4174-9 (2005) [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:
BDBM50171608
Synonyms:
CHEMBL365360 | N-(1-Benzo[1,3]dioxol-5-ylmethyl-piperidin-4-yl)-5-chloro-2-[(1H-imidazol-2-ylmethyl)-amino]-nicotinamide
Type:
Small organic molecule
Emp. Form.:
C23H25ClN6O3
Mol. Mass.:
468.936
SMILES:
Clc1cnc(NCc2ncc[nH]2)c(c1)C(=O)NC1CCN(Cc2ccc3OCOc3c2)CC1