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TargetArachidonate 5-lipoxygenase
LigandBDBM323041
Substrate/Competitorn/a
Meas. Tech.FLAP Binding Assay (Test A)
IC50 8.10±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:
BDBM323041
NameBDBM323041
Synonyms:(1R,2R)-N-(4-Oxo-4,5,6,7- tetrahydropyrazolo[1,5-a]pyrazin-3-yl)-2- [4-(1H-pyrazol-5- yl)benzoyl]cyclohexanecarboxamide | US10183947, Example 24
TypeSmall organic molecule
Emp. Form.C23H24N6O3
Mol. Mass.432.4751
SMILESO=C(Nc1cnn2CCNC(=O)c12)[C@@H]1CCCC[C@H]1C(=O)c1ccc(cc1)-c1ccn[nH]1 |r|
Structure
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n/a