| Reaction Details |
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 | Report a problem with these data |
| Target | Polyunsaturated fatty acid 5-lipoxygenase |
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| Ligand | BDBM50000829 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_3821 (CHEMBL618007) |
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| IC50 | 27±n/a nM |
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| Citation |  Lambert-van der Brempt, C; Bruneau, P; Lamorlette, MA; Foster, SJ Conformational analysis of 5-lipoxygenase inhibitors: role of the substituents in chiral recognition and on the active conformations of the (methoxyalkyl)thiazole and methoxytetrahydropyran series. J Med Chem37:113-24 (1994) [PubMed] |
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| More Info.: | Get all data from this article, Assay Method |
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| Polyunsaturated fatty acid 5-lipoxygenase |
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| Name: | Polyunsaturated fatty acid 5-lipoxygenase |
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| Synonyms: | 5-LO | 5-Lipo-oxygenase (5-LOX) | 5-Lipoxygenase (5-LO) | 5-Lipoxygenase (LOX) | 5-Lipoygenase | 5-lipoxygenase/FLAP | ALOX5 | Arachidonate 5-lipoxygenase | LOG5 | LOX5_HUMAN |
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| Type: | Enzyme |
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| Mol. Mass.: | 77972.74 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Recombinant protein was purified from E. coli lysate. After ammonium sulfate precipitation and subsequent steps, the supernatant (S100) was used for 5-LO activity assay.
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| Residue: | 674 |
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| Sequence: | MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDE
ELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLA
RDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVL
NYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNG
CNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDP
CTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDF
HVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECG
LFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWE
AIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYL
TVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCW
HLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPY
YYLSPDRIPNSVAI
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| BDBM50000829 |
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| n/a |
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| Name | BDBM50000829 |
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| Synonyms: | 6-((3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy)methyl)-1-methylquinolin-2(1H)-one | 6-[3-Fluoro-5-(4-methoxy-tetrahydro-pyran-4-yl)-phenoxymethyl]-1-methyl-1H-quinolin-2-one | 6-[3-Fluoro-5-(tetrahydro-pyran-4-yl)-phenoxymethyl]-1-methyl-1H-quinolin-2-one | CHEMBL20403 | ZD-2138 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H24FNO4 |
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| Mol. Mass. | 397.4394 |
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| SMILES | COC1(CCOCC1)c1cc(F)cc(OCc2ccc3n(C)c(=O)ccc3c2)c1 |
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| Structure | 
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