Reaction Details |
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Target | Melanin-concentrating hormone receptor 1 |
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Ligand | BDBM50184948 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_342542 (CHEMBL861585) |
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Ki | 2.3±n/a nM |
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Citation | McBriar, MD; Guzik, H; Shapiro, S; Paruchova, J; Xu, R; Palani, A; Clader, JW; Cox, K; Greenlee, WJ; Hawes, BE; Kowalski, TJ; O'neill, K; Spar, BD; Weig, B; Weston, DJ; Farley, C; Cook, J Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas. J Med Chem49:2294-310 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Melanin-concentrating hormone receptor 1 |
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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: | MSVGAMKKGVGRAVGLGGGSGCQATEEDPLPNCGACAPGQGGRRWRLPQPAWVEGSSARL
WEQATGTGWMDLEASLLPTGPNASNTSDGPDNLTSAGSPPRTGSISYINIIMPSVFGTIC
LLGIIGNSTVIFAVVKKSKLHWCNNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHF
GETMCTLITAMDANSQFTSTYILTAMAIDRYLATVHPISSTKFRKPSVATLVICLLWALS
FISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVRI
LQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVY
LYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRAVSNAQTADEERTESK
GT
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BDBM50184948 |
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n/a |
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Name | BDBM50184948 |
Synonyms: | CHEMBL206616 | N-[trans-5-(3-fluorophenyl)bicyclo[3.1.0]hex-2-yl]-N'-[4-fluoro-3-(trifluoromethyl)phenyl)-N-[3-(4-methyl-1-piperazinyl)propyl]-urea |
Type | Small organic molecule |
Emp. Form. | C28H33F5N4O |
Mol. Mass. | 536.5798 |
SMILES | CN1CCN(CCCN([C@@H]2CC[C@@]3(C[C@H]23)c2cccc(F)c2)C(=O)Nc2ccc(F)c(c2)C(F)(F)F)CC1 |
Structure |
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