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TargetPolyunsaturated fatty acid 5-lipoxygenase
LigandBDBM24566
Substrate/CompetitorBDBM22319
Meas. Tech.Determination of 5-LO Product Formation in Intact Cells (EC50/IC50)
pH7.4±n/a
Temperature310.15±n/a K
CommentsNo inhibition of 5-LO product formation in Intact cells @ 10 uM.
Citation Werz, OGreiner, CKoeberle, AHoernig, CGeorge, SPopescu, LSyha, ISchubert-Zsilavecz, MSteinhilber, 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
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Polyunsaturated fatty acid 5-lipoxygenase
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.
Residue:674
Sequence:
MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDE
ELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLA
RDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVL
NYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNG
CNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDP
CTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDF
HVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECG
LFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWE
AIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYL
TVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCW
HLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPY
YYLSPDRIPNSVAI
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  Blast E-value cutoff:
BDBM24566
BDBM22319
NameBDBM24566
Synonyms:2-({4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl}sulfanyl)acetic acid | CHEMBL295416 | JMC515449 Compound 1 | Pirinixic acid | Wyeth 14,643
TypeSmall organic molecule
Emp. Form.C14H14ClN3O2S
Mol. Mass.323.798
SMILESCc1cccc(Nc2cc(Cl)nc(SCC(O)=O)n2)c1C
Structure
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