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Target
Polyunsaturated fatty acid 5-lipoxygenase
Ligand
BDBM7459
Substrate
n/a
Meas. Tech.
ChEMBL_1284181 (CHEMBL3107776)
IC50
1600±n/a nM
Citation
 Ribeiro, D; Freitas, M; Tomé, SM; Silva, AM; Porto, G; Cabrita, EJ; Marques, MM; Fernandes, E Inhibition of LOX by flavonoids: a structure-activity relationship study. Eur J Med Chem 72:137-45 (2014) [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:
BDBM7459
Synonyms:
2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one | 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-chromen-4-one | CHEMBL151 | Luteolin (27) | Luteolin (4) | acs.jmedchem.1c00409_ST.600 | cid_5280445 | luteolin | med.21724, Compound 3
Type:
Small organic molecule
Emp. Form.:
C15H10O6
Mol. Mass.:
286.2363
SMILES:
Oc1cc(O)c2c(c1)oc(cc2=O)-c1ccc(O)c(O)c1
Structure:
Search PDB for entries with ligand similarity: