Reaction Details
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Arachidonate 5-lipoxygenase-activating protein
Ligand
BDBM50052018
Substrate
n/a
Meas. Tech.
ChEMBL_789491 (CHEMBL1924518)
IC50
1.9±n/a nM
Citation
Stock, NS; Bain, G; Zunic, J; Li, Y; Ziff, J; Roppe, J; Santini, A; Darlington, J; Prodanovich, P; King, CD; Baccei, C; Lee, C; Rong, H; Chapman, C; Broadhead, A; Lorrain, D; Correa, L; Hutchinson, JH; Evans, JF; Prasit, 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 More Info.:
Target
Name:
Arachidonate 5-lipoxygenase-activating protein
Synonyms:
5-lipoxygenase activating protein | MK-886-binding protein | 5-lipoxygenase-activating protein (FLAP) | AL5AP_HUMAN | ALOX5AP | FLAP | 5-lipoxygenase/FLAP
Type:
Enzyme
Mol. Mass.:
18159.90
Organism:
Human
Description:
P20292
Residue:
161
Sequence:
MDQETVGNVVLLAIVTLISVVQNGFFAHKVEHESRTQNGRSFQRTGTLAFERVYTANQNCVDAYPTFLAVLWSAGLLCSQVPAAFAGLMYLFVRQKYFVGYLGERTQSTPGYIFGKRIILFLFLMSVAGIFNYYLIFFFGSDFENYIKTISTTISPLLLIP
Inhibitor
Name:
BDBM50052018
Synonyms:
MK-591 | Sodium; 3-[3-tert-butylsulfanyl-1-(4-chloro-benzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionate | 3-[3-tert-Butylsulfanyl-1-(4-chloro-benzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid | CHEMBL313489
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
