Reaction Details |
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Target | Melanin-concentrating hormone receptor 1 |
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Ligand | BDBM50120787 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1518192 (CHEMBL3619839) |
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Ki | 9.0±n/a nM |
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Citation | Devasthale, P; Wang, W; Mignone, J; Renduchintala, K; Radhakrishnan, S; Dhanapal, J; Selvaraj, J; Kuppusamy, R; Pelleymounter, MA; Longhi, D; Huang, N; Flynn, N; Azzara, AV; Rohrbach, K; Devenny, J; Rooney, S; Thomas, M; Glick, S; Godonis, H; Harvey, S; Cullen, MJ; Zhang, H; Caporuscio, C; Stetsko, P; Grubb, M; Huang, C; Zhang, L; Freeden, C; Murphy, BJ; Robl, JA; Washburn, WN Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies. Bioorg Med Chem Lett25:4412-8 (2015) [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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BDBM50120787 |
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n/a |
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Name | BDBM50120787 |
Synonyms: | CHEMBL3618348 |
Type | Small organic molecule |
Emp. Form. | C22H18ClF2N5O4 |
Mol. Mass. | 489.859 |
SMILES | COc1cc(ccc1OCC1(O)CC(F)(F)C1)-n1cnn2cc(cc2c1=O)-c1ncc(Cl)cn1 |
Structure |
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