Reaction Details |
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Target | Melanin-concentrating hormone receptor 1 |
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Ligand | BDBM30156 |
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Substrate/Competitor | BDBM30157 |
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Meas. Tech. | Radioligand Binding Assay (IC50) and Functional Assay (EC50/IC50) |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 5.9±n/a nM |
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EC50 | 21±n/a nM |
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Citation | Moriya, M; Kishino, H; Sakuraba, S; Sakamoto, T; Suga, T; Takahashi, H; Suzuki, T; Ito, M; Ito, J; Moriya, R; Takenaga, N; Iwaasa, H; Ishihara, A; Kanatani, A; Fukami, T Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists. Bioorg Med Chem Lett19:3568-72 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, 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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BDBM30156 |
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BDBM30157 |
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Name | BDBM30156 |
Synonyms: | 2-aminobenzimidazole-based compound, 8 |
Type | Small organic molecule |
Emp. Form. | C21H23F3N4O |
Mol. Mass. | 404.4287 |
SMILES | CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(cc3)C(F)(F)F)cc2[nH]1 |
Structure |
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