Reaction Details |
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Target | Melanin-concentrating hormone receptor 1 |
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Ligand | BDBM50207677 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_454874 (CHEMBL886904) |
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IC50 | 773±n/a nM |
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Citation | Judd, AS; Souers, AJ; Wodka, D; Zhao, G; Mulhern, MM; Iyengar, RR; Gao, J; Lynch, JK; Freeman, JC; Falls, HD; Brodjian, S; Dayton, BD; Reilly, RM; Gintant, G; Limberis, JT; Mikhail, A; Leitza, ST; Houseman, KA; Diaz, G; Bush, EN; Shapiro, R; Knourek-Segel, V; Hernandez, LE; Marsh, KC; Sham, HL; Collins, CA; Kym, PR Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity. Bioorg Med Chem Lett17:2365-71 (2007) [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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BDBM50207677 |
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n/a |
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Name | BDBM50207677 |
Synonyms: | CHEMBL248296 | N-(1-(4-(3-(dimethylamino)propoxy)-3-fluorobenzyl)piperidin-4-yl)-7-fluoro-4-oxo-4H-chromene-2-carboxamide |
Type | Small organic molecule |
Emp. Form. | C27H31F2N3O4 |
Mol. Mass. | 499.5495 |
SMILES | CN(C)CCCOc1ccc(CN2CCC(CC2)NC(=O)c2cc(=O)c3ccc(F)cc3o2)cc1F |
Structure |
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