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TargetArachidonate 5-lipoxygenase
LigandBDBM323031
Substrate/Competitorn/a
Meas. Tech.FLAP Binding Assay (Test A)
IC50 8.60±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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM323031
NameBDBM323031
Synonyms:(1R,2R)-N-[5-(Difluoromethyl)-1H- pyrazol-4-yl]-2-[4-(5-methyl-1H-pyrazol- 3-yl)benzoyl]cyclohexanecarboxamide | US10183947, Example 15
TypeSmall organic molecule
Emp. Form.C22H23F2N5O2
Mol. Mass.427.4471
SMILESCc1cc(n[nH]1)-c1ccc(cc1)C(=O)[C@@H]1CCCC[C@H]1C(=O)Nc1cn[nH]c1C(F)F |r|
Structure
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n/a