Target
Polyunsaturated fatty acid 5-lipoxygenase
Ligand
BDBM50058590
Substrate
n/a
Meas. Tech.
ChEMBL_90070 (CHEMBL701321)
IC50
100±n/a nM
Citation
 Stewart, AOBhatia, PAMartin, JGSummers, JBRodriques, KEMartin, MBHolms, JHMoore, JLCraig, RAKolasa, TRatajczyk, JDMazdiyasni, HKerdesky, FADeNinno, SLMaki, RGBouska, JBYoung, PRLanni, CBell, RLCarter, GWBrooks, CD Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors. J Med Chem 40:1955-68 (1997) [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:
BDBM50058590
Synonyms:
CHEMBL293743 | Fenleuton | N-{3-[3-(4-fluorophenoxy)phenyl]-1-methylprop-2-ynyl}-N-hydroxyurea
Type:
Small organic molecule
Emp. Form.:
C17H15FN2O3
Mol. Mass.:
314.311
SMILES:
CC(C#Cc1cccc(Oc2ccc(F)cc2)c1)N(O)C(N)=O
Structure:
Search PDB for entries with ligand similarity: