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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50492349
Substrate
n/a
Meas. Tech.
ChEMBL_971498 (CHEMBL2406560)
EC50
25±n/a nM
Citation
 Qian, Y; Conde-Knape, K; Erickson, SD; Falcioni, F; Gillespie, P; Hakimi, I; Mennona, F; Ren, Y; Salari, H; So, SS; Tilley, JW Potent MCH-1 receptor antagonists from cis-1,4-diaminocyclohexane-derived indane analogs. Bioorg Med Chem Lett 23:4216-20 (2013) [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:
BDBM50492349
Synonyms:
CHEMBL2403861
Type:
Small organic molecule
Emp. Form.:
C27H31ClN4O
Mol. Mass.:
463.014
SMILES:
CC(C)(O)c1nc2cc(Cl)ccc2n1[C@@H]1CC[C@@H](CC1)NC[C@H]1Cc2ccc(cc2C1)C#N |r,wU:14.15,17.22,22.24,(71.13,-8.4,;71.91,-9.74,;72.68,-8.4,;73.37,-10.27,;70.74,-10.74,;69.24,-10.38,;68.43,-11.69,;66.91,-11.96,;66.39,-13.41,;64.88,-13.69,;67.38,-14.59,;68.9,-14.32,;69.43,-12.87,;70.85,-12.29,;72.19,-13.07,;72.13,-14.63,;73.44,-15.44,;74.8,-14.73,;74.85,-13.16,;73.53,-12.34,;76.13,-15.51,;77.47,-14.76,;77.48,-13.22,;76.24,-12.3,;76.73,-10.84,;75.98,-9.51,;76.75,-8.19,;78.29,-8.2,;79.04,-9.54,;78.26,-10.86,;78.73,-12.32,;79.06,-6.88,;79.85,-5.55,)|
Structure:
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