Reaction Details |
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Target | Melanin-concentrating hormone receptor 1 |
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Ligand | BDBM50162116 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_306651 (CHEMBL832988) |
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IC50 | 1.4±n/a nM |
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Citation | Souers, AJ; Gao, J; Brune, M; Bush, E; Wodka, D; Vasudevan, A; Judd, AS; Mulhern, M; Brodjian, S; Dayton, B; Shapiro, R; Hernandez, LE; Marsh, KC; Sham, HL; Collins, CA; Kym, PR Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity. J Med Chem48:1318-21 (2005) [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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BDBM50162116 |
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n/a |
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Name | BDBM50162116 |
Synonyms: | 2-(4-(benzyloxy)phenyl)-N-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-6-yl)acetamide | 2-(4-Benzyloxy-phenyl)-N-[1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]-acetamide | CHEMBL179501 |
Type | Small organic molecule |
Emp. Form. | C28H30N4O2 |
Mol. Mass. | 454.5634 |
SMILES | O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 |
Structure |
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