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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50207673
Substrate
n/a
Meas. Tech.
ChEMBL_454873 (CHEMBL886902)
IC50
26±n/a nM
Citation
 Judd, AS; Souers, AJ; Wodka, D; Zhao, G; Mulhern, MM; Iyengar, RR; Gao, J; Lynch, JK; Freeman, JC; Falls, HD; Brodjian, S; Dayton, BD; Reilly, RM; Gintant, G; Limberis, JT; Mikhail, A; Leitza, ST; Houseman, KA; Diaz, G; Bush, EN; Shapiro, R; Knourek-Segel, V; Hernandez, LE; Marsh, KC; Sham, HL; Collins, CA; Kym, PR Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity. Bioorg Med Chem Lett 17:2365-71 (2007) [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:
BDBM50207673
Synonyms:
CHEMBL246259 | N-(1-(2-methoxy-4-((2-(pyrrolidin-1-yl)ethyl)carbamoyl)benzyl)piperidin-4-yl)-7-fluoro-4-oxo-4H-chromene-2-carboxamide
Type:
Small organic molecule
Emp. Form.:
C30H35FN4O5
Mol. Mass.:
550.6211
SMILES:
COc1cc(ccc1CN1CCC(CC1)NC(=O)c1cc(=O)c2ccc(F)cc2o1)C(=O)NCCN1CCCC1
Structure:
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