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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50197139
Substrate
n/a
Meas. Tech.
ChEMBL_408728 (CHEMBL908288)
IC50
3±n/a nM
Citation
 Lynch, JK; Freeman, JC; Judd, AS; Iyengar, R; Mulhern, M; Zhao, G; Napier, JJ; Wodka, D; Brodjian, S; Dayton, BD; Falls, D; Ogiela, C; Reilly, RM; Campbell, TJ; Polakowski, JS; Hernandez, L; Marsh, KC; Shapiro, R; Knourek-Segel, V; Droz, B; Bush, E; Brune, M; Preusser, LC; Fryer, RM; Reinhart, GA; Houseman, K; Diaz, G; Mikhail, A; Limberis, JT; Sham, HL; Collins, CA; Kym, PR Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety. J Med Chem 49:6569-84 (2006) [PubMed]  Article 
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:
BDBM50197139
Synonyms:
CHEMBL214021 | N-(1-(benzo[d][1,3]dioxol-5-ylmethyl)piperidin-4-yl)-7-fluoro-4-oxo-4H-chromene-2-carboxamide | N-[1-(1,3-benzodioxol-5-ylmethyl)piperidin-4-yl]-7-fluoro-4-oxo-4H-chromene-2-carboxamide
Type:
Small organic molecule
Emp. Form.:
C23H21FN2O5
Mol. Mass.:
424.4216
SMILES:
Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(Cc2ccc3OCOc3c2)CC1
Structure:
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