Target
Arachidonate 5-lipoxygenase-activating protein
Ligand
BDBM50052018
Substrate
n/a
Meas. Tech.
ChEMBL_789496 (CHEMBL1924523)
IC50
80±n/a nM
Citation
 Stock, NSBain, GZunic, JLi, YZiff, JRoppe, JSantini, ADarlington, JProdanovich, PKing, CDBaccei, CLee, CRong, HChapman, CBroadhead, ALorrain, DCorrea, LHutchinson, JHEvans, JFPrasit, P 5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor. J Med Chem 54:8013-29 (2011) [PubMed]  Article 
Target
Name:
Arachidonate 5-lipoxygenase-activating protein
Synonyms:
5-lipoxygenase activating protein | 5-lipoxygenase-activating protein (FLAP) | 5-lipoxygenase/FLAP | AL5AP_HUMAN | ALOX5AP | FLAP | MK-886-binding protein
Type:
Enzyme
Mol. Mass.:
18159.90
Organism:
Homo sapiens (Human)
Description:
P20292
Residue:
161
Sequence:
MDQETVGNVVLLAIVTLISVVQNGFFAHKVEHESRTQNGRSFQRTGTLAFERVYTANQNCVDAYPTFLAVLWSAGLLCSQVPAAFAGLMYLFVRQKYFVGYLGERTQSTPGYIFGKRIILFLFLMSVAGIFNYYLIFFFGSDFENYIKTISTTISPLLLIP
  
Inhibitor
Name:
BDBM50052018
Synonyms:
3-[3-tert-Butylsulfanyl-1-(4-chloro-benzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid | CHEMBL313489 | MK-591 | Sodium; 3-[3-tert-butylsulfanyl-1-(4-chloro-benzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionate
Type:
Small organic molecule
Emp. Form.:
C34H34ClN2O3S
Mol. Mass.:
586.164
SMILES:
CC(C)(C)Sc1c(CC(C)(C)C([O-])=O)n(Cc2ccc(Cl)cc2)c2ccc(OCc3ccc4ccccc4n3)cc12
Structure:
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