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Target
Polyunsaturated fatty acid 5-lipoxygenase
Ligand
BDBM50059715
Substrate
n/a
Meas. Tech.
ChEBML_4072
IC50
20±n/a nM
Citation
 Dubé, D; Blouin, M; Brideau, C; Chan, CC; Desmarais, S; Ethier, D; Falgueyret, JP; Friesen, RW; Girard, M; Girard, Y; Guay, J; Riendeau, D; Tagari, P; Young, RN Quinolines as potent 5-lipoxygenase inhibitors: synthesis and biological profile of L-746,530. Bioorg Med Chem Lett 8:1255-60 (1999) [PubMed]  Article 
Target
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:
MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDEELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLARDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVLNYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNGCNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDPCTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDFHVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECGLFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWEAIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYLTVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCWHLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPYYYLSPDRIPNSVAI
  
Inhibitor
Name:
BDBM50059715
Synonyms:
4-Furan-3-yl-7-[6-(3-hydroxy-6,8-dioxa-bicyclo[3.2.1]oct-3-yl)-pyridin-2-ylmethoxy]-naphthalene-2-carbonitrile | CHEMBL278293
Type:
Small organic molecule
Emp. Form.:
C27H22N2O5
Mol. Mass.:
454.474
SMILES:
OC1(CC2COC(C1)O2)c1cccc(COc2ccc3c(cc(cc3c2)C#N)-c2ccoc2)n1 |TLB:0:1:8:5.4,THB:9:1:8:5.4|
Structure:
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