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Target
Arachidonate 5-lipoxygenase-activating protein
Ligand
BDBM50297385
Substrate
n/a
Meas. Tech.
ChEMBL_789604 (CHEMBL1924645)
IC50
1.1±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 | 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:
BDBM50297385
Synonyms:
3-[3-tert-Butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic Acid | CHEMBL557527
Type:
Small organic molecule
Emp. Form.:
C36H39N3O4S
Mol. Mass.:
609.778
SMILES:
COc1ccc(cn1)-c1ccc(Cn2c(CC(C)(C)C(O)=O)c(SC(C)(C)C)c3cc(OCc4ccccn4)ccc23)cc1