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TargetPolyunsaturated fatty acid 5-lipoxygenase
LigandBDBM50045643
Substrate/Competitorn/a
Meas. Tech.ChEBML_3830
IC50 3±n/a nM
Citation Hutchinson, JHRiendeau, DBrideau, CChan, CDelorme, DDenis, DFalgueyret, JPFortin, RGuay, JHamel, P Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation of L-691,816. J Med Chem36:2771-87 (1993) [PubMed]
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:
BDBM50045643
n/a
NameBDBM50045643
Synonyms:3-[1-(4-Chloro-benzyl)-4-methyl-6-(quinolin-2-ylmethoxy)-4,5-dihydro-1H-3-thia-1-aza-acenaphthylen-2-yl]-2,2-dimethyl-propionic acid | 3-[1-(4-Chloro-benzyl)-4-methyl-6-(quinolin-2-ylmethoxy)-4,5-dihydro-1H-thiopyrano[2,3,4-cd]indol-2-yl]-2,2-dimethyl-propionic acid | CHEMBL50170
TypeSmall organic molecule
Emp. Form.C33H31ClN2O3S
Mol. Mass.571.129
SMILESCC1Cc2c(OCc3ccc4ccccc4n3)ccc3n(Cc4ccc(Cl)cc4)c(CC(C)(C)C(O)=O)c(S1)c23
Structure
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