Reaction Details |
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Target | Polyunsaturated fatty acid 5-lipoxygenase |
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Ligand | BDBM24561 |
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Substrate/Competitor | BDBM22319 |
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Meas. Tech. | Determination of 5-LO Product Formation in Cell-Free Systems (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 | 19000±n/a nM |
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EC50 | 600±n/a nM |
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Citation | Werz, O; Greiner, C; Koeberle, A; Hoernig, C; George, S; Popescu, L; Syha, I; Schubert-Zsilavecz, M; Steinhilber, D Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid. J Med Chem51:5449-53 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM24561 |
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BDBM22319 |
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Name | BDBM24561 |
Synonyms: | CHEMBL459722 | Pirinixic acid-based compound, 6d | ethyl 2-{[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl}octanoate |
Type | Small organic molecule |
Emp. Form. | C23H27ClN4O2S |
Mol. Mass. | 459.004 |
SMILES | CCCCCCC(Sc1nc(Cl)cc(Nc2ccc3ncccc3c2)n1)C(=O)OCC |
Structure |
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