Reaction Details |
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Target | Polyunsaturated fatty acid 5-lipoxygenase |
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Ligand | BDBM31128 |
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Substrate/Competitor | BDBM22319 |
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Meas. Tech. | Inhibition of 5-LO Product Formation in Cell-Free Systems (IC50) and in Intact Neutrophils (EC50/IC50) |
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pH | 7.4±n/a |
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Temperature | 310.15±n/a K |
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IC50 | 95±10 nM |
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EC50 | 600±240 nM |
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Citation | Karg, EM; Luderer, S; Pergola, C; Bühring, U; Rossi, A; Northoff, H; Sautebin, L; Troschütz, R; Werz, O Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase. J Med Chem52:3474-83 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, 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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BDBM31128 |
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BDBM22319 |
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Name | BDBM31128 |
Synonyms: | 5-hydroxy-1H-benzo[g]indole-3-carboxylate, 11g |
Type | Small organic molecule |
Emp. Form. | C22H18BrNO3 |
Mol. Mass. | 424.287 |
SMILES | CCOC(=O)c1c(Cc2ccc(Br)cc2)[nH]c2c1cc(O)c1ccccc21 |
Structure |
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