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TargetPolyunsaturated fatty acid 5-lipoxygenase
LigandBDBM50053548
Substrate/Competitorn/a
Meas. Tech.ChEMBL_3826 (CHEMBL618012)
IC50 190±n/a nM
Citation Delorme, DDucharme, YBrideau, CChan, CCChauret, NDesmarais, SDubé, DFalgueyret, JPFortin, RGuay, JHamel, PJones, TRLépine, CLi, CMcAuliffe, MMcFarlane, CSNicoll-Griffith, DARiendeau, DYergey, JAGirard, Y Dioxabicyclooctanyl naphthalenenitriles as nonredox 5-lipoxygenase inhibitors: structure-activity relationship study directed toward the improvement of metabolic stability. J Med Chem39:3951-70 (1996) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Polyunsaturated fatty acid 5-lipoxygenase
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:
MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDE
ELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLA
RDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVL
NYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNG
CNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDP
CTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDF
HVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECG
LFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWE
AIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYL
TVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCW
HLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPY
YYLSPDRIPNSVAI
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  Blast E-value cutoff:
BDBM50053548
n/a
NameBDBM50053548
Synonyms:4-Furan-3-yl-7-[3-(3-hydroxy-6,8-dioxa-bicyclo[3.2.1]oct-3-yl)-benzyloxy]-naphthalene-2-carbonitrile | CHEMBL97380 | L-702-539
TypeSmall organic molecule
Emp. Form.C28H23NO5
Mol. Mass.453.4859
SMILESOC1(CC2COC(C1)O2)c1cccc(COc2ccc3c(cc(cc3c2)C#N)-c2ccoc2)c1 |TLB:0:1:8:5.4,THB:9:1:8:5.4|
Structure
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