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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM86674
Substrate
n/a
Ki
7.23±n/a nM
Comments
PDSP_5086
Citation
 Chaki, S; Funakoshi, T; Hirota-Okuno, S; Nishiguchi, M; Shimazaki, T; Iijima, M; Grottick, AJ; Kanuma, K; Omodera, K; Sekiguchi, Y; Okuyama, S; Tran, TA; Semple, G; Thomsen, W Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists. J Pharmacol Exp Ther 313:831-9 (2005) [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:
BDBM86674
Synonyms:
ATC0175
Type:
Small organic molecule
Emp. Form.:
C23H25F2N5O
Mol. Mass.:
425.4743
SMILES:
CN(C)c1nc(N[C@@H]2CC[C@@H](CC2)NC(=O)c2ccc(F)c(F)c2)nc2ccccc12 |r,wU:10.13,7.6,(-7.34,-2.98,;-7.34,-1.44,;-8.67,-.67,;-6,-.67,;-4.67,-1.44,;-3.33,-.67,;-2,-1.44,;-.67,-.67,;.67,-1.44,;2,-.67,;2,.87,;.67,1.64,;-.67,.87,;3.33,1.64,;4.67,.87,;4.67,-.67,;6,1.64,;7.34,.87,;8.67,1.64,;8.67,3.18,;10,3.95,;7.34,3.95,;7.34,5.49,;6,3.18,;-3.33,.87,;-4.67,1.64,;-4.67,3.18,;-6,3.95,;-7.34,3.18,;-7.34,1.64,;-6,.87,)|
Structure:
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