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TargetPolyunsaturated fatty acid 5-lipoxygenase
LigandBDBM50443830
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1277574 (CHEMBL3096450)
IC50 300±n/a nM
Citation Hanke, TDehm, FLiening, SPopella, SDMaczewsky, JPillong, MKunze, JWeinigel, CBarz, DKaiser, AWurglics, MLämmerhofer, MSchneider, GSautebin, LSchubert-Zsilavecz, MWerz, O Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo. J Med Chem56:9031-44 (2013) [PubMed]  Article
More Info.:Get all data from this article,  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:
BDBM50443830
n/a
NameBDBM50443830
Synonyms:CHEMBL3091500
TypeSmall organic molecule
Emp. Form.C21H22BrClN4O2S2
Mol. Mass.541.912
SMILESCCCCCCC(Sc1nc(Cl)cc(Nc2nc(cs2)-c2ccc(Br)cc2)n1)C(O)=O
Structure
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