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Target
Polyunsaturated fatty acid 5-lipoxygenase
Ligand
BDBM50341251
Substrate
n/a
Meas. Tech.
ChEMBL_818992 (CHEMBL2034136)
IC50
630±n/a nM
Citation
 Barzen, S; Rödl, CB; Lill, A; Steinhilber, D; Stark, H; Hofmann, B Synthesis and biological evaluation of a class of 5-benzylidene-2-phenyl-thiazolinones as potent 5-lipoxygenase inhibitors. Bioorg Med Chem 20:3575-83 (2012) [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:
BDBM50341251
Synonyms:
(Z)-2-(4-Aminophenyl)-5-(4-methoxybenzylidene)-5H-thiazol-4-one | CHEMBL1765905
Type:
Small organic molecule
Emp. Form.:
C17H14N2O2S
Mol. Mass.:
310.37
SMILES:
COc1ccc(\C=C2/SC(=NC2=O)c2ccc(N)cc2)cc1 |c:9|
Structure:
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