Reaction Details |
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Target | Polyunsaturated fatty acid 5-lipoxygenase |
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Ligand | BDBM50059718 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_3795 (CHEMBL619870) |
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IC50 | 1000±n/a nM |
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Citation | Hamel, P; Riendeau, D; Brideau, C; Chan, CC; Desmarais, S; Delorme, D; Dubé, D; Ducharme, Y; Ethier, D; Grimm, E; Falgueyret, JP; Guay, J; Jones, TR; Kwong, E; McAuliffe, M; McFarlane, CS; Piechuta, H; Roumi, M; Tagari, P; Young, RN; Girard, Y Substituted (pyridylmethoxy)naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics of L-739,010. J Med Chem40:2866-75 (1997) [PubMed] Article |
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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 |
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 |
Type: | Enzyme |
Mol. Mass.: | 77972.74 |
Organism: | Homo sapiens (Human) |
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 |
Sequence: | MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDE
ELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLA
RDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVL
NYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNG
CNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDP
CTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDF
HVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECG
LFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWE
AIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYL
TVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCW
HLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPY
YYLSPDRIPNSVAI
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BDBM50059718 |
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n/a |
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Name | BDBM50059718 |
Synonyms: | 4-Furan-3-yl-7-[7-(4-hydroxy-tetrahydro-pyran-4-yl)-quinolin-2-ylmethoxy]-naphthalene-2-carbonitrile | CHEMBL421391 |
Type | Small organic molecule |
Emp. Form. | C30H24N2O4 |
Mol. Mass. | 476.5226 |
SMILES | OC1(CCOCC1)c1ccc2ccc(COc3ccc4c(cc(cc4c3)C#N)-c3ccoc3)nc2c1 |
Structure |
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