Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50492365
Substrate
n/a
Meas. Tech.
ChEMBL_971499 (CHEMBL2406561)
IC50
230±n/a nM
Citation
 Qian, YConde-Knape, KErickson, SDFalcioni, FGillespie, PHakimi, IMennona, FRen, YSalari, HSo, SSTilley, 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:
BDBM50492365
Synonyms:
CHEMBL2403860
Type:
Small organic molecule
Emp. Form.:
C27H31ClF3N3O
Mol. Mass.:
506.003
SMILES:
CC(C)(O)c1nc2cc(Cl)ccc2n1[C@@H]1CC[C@@H](CC1)NCC1Cc2ccc(cc2C1)C(F)(F)F |r,wU:14.15,17.22,(26.9,-6.63,;27.68,-7.97,;28.45,-6.62,;29.13,-8.49,;26.51,-8.97,;25.01,-8.6,;24.2,-9.91,;22.67,-10.19,;22.16,-11.64,;20.65,-11.92,;23.15,-12.82,;24.67,-12.55,;25.2,-11.09,;26.62,-10.52,;27.96,-11.3,;27.89,-12.86,;29.21,-13.67,;30.56,-12.95,;30.62,-11.39,;29.3,-10.57,;31.89,-13.74,;33.23,-12.98,;33.25,-11.44,;32,-10.53,;32.49,-9.07,;31.74,-7.74,;32.52,-6.42,;34.06,-6.43,;34.81,-7.77,;34.03,-9.09,;34.5,-10.55,;34.84,-5.1,;36.38,-5.12,;34.08,-3.76,;35.6,-3.76,)|
Structure:
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