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Target
Polyunsaturated fatty acid 5-lipoxygenase
Ligand
BDBM50280046
Substrate
n/a
Meas. Tech.
ChEBML_724
IC50
480±n/a nM
Citation
 Yu, MJ; McCowan, JR; Bertsch, B; Ho, PP; Phebus, LA; Ruterbories, KJ; Lindstrom, TD; Smallwood, JK; Simpson, PJ Phenothiazine and phenoxazine derivatives of nafazatrom. In vitro evaluation as 5-lipoxygenase and iron-dependent lipid peroxidation inhibitors. Bioorg Med Chem Lett 2:59-62 (1992)    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:
BDBM50280046
Synonyms:
2-[2-(Naphthalen-2-yloxy)-ethyl]-3a,4,5,6-tetrahydro-2H-cyclopentapyrazol-3-one | CHEMBL154058
Type:
Small organic molecule
Emp. Form.:
C18H18N2O2
Mol. Mass.:
294.3477
SMILES:
O=c1c2CCCc2[nH]n1CCOc1ccc2ccccc2c1
Structure:
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