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TargetArachidonate 5-lipoxygenase
LigandBDBM323042
Substrate/Competitorn/a
Meas. Tech.FLAP Binding Assay (Test A)
IC50 25.0±n/a nM
Citation Broddefalk JOEmtenäs HFGranberg KLLemurell MAPettersen DTPlowright ATUlander LJ Pyrazole derivatives useful as 5-lipoxygenase activating protein (FLAP) inhibitors US Patent  US10183947 Publication Date 1/22/2019
More Info.:Get all data from this article,  Assay Method
 
Arachidonate 5-lipoxygenase
Name:Arachidonate 5-lipoxygenase
Synonyms:5-LO | 5-Lipo-oxygenase (5-LOX) | 5-Lipoxygenase (5-LO) | 5-Lipoxygenase (LOX) | 5-Lipoygenase | ALOX5 | LOG5
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:
BDBM323042
n/a
NameBDBM323042
Synonyms:(1R,2R)-N-[1-Methyl-5- (melhyIsulfamoyl)-1H-pyrazol-4-yl]-2-[4- (3-methyl-1H-pyrazol-5- yl)benzoyl]cyclohexanecarboxamide | US10183947, Example 25
TypeSmall organic molecule
Emp. Form.C23H28N6O4S
Mol. Mass.484.571
SMILESCNS(=O)(=O)c1c(NC(=O)[C@@H]2CCCC[C@H]2C(=O)c2ccc(cc2)-c2cc(C)n[nH]2)cnn1C |r|
Structure
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