Ki Summary

Reaction Details

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Target

Arachidonate 5-lipoxygenase-activating protein

Ligand

BDBM50006805

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_789603 (CHEMBL1924644)

IC50

2.2±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 Chem54:8013-29 (2011) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Arachidonate 5-lipoxygenase-activating protein

Name:

Arachidonate 5-lipoxygenase-activating protein

Synonyms:

Type:

Enzyme

Mol. Mass.:

18159.90

Organism:

Homo sapiens (Human)

Description:

P20292

Residue:

161

Sequence:

MDQETVGNVVLLAIVTLISVVQNGFFAHKVEHESRTQNGRSFQRTGTLAFERVYTANQNC
VDAYPTFLAVLWSAGLLCSQVPAAFAGLMYLFVRQKYFVGYLGERTQSTPGYIFGKRIIL
FLFLMSVAGIFNYYLIFFFGSDFENYIKTISTTISPLLLIP

BDBM50006805

n/a

Name

BDBM50006805

Synonyms:

3-(1-(4-chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl)-2,2-dimethylpropanoic acid | 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl)-2,2-dimethylpropanoic acid | 3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2-dimethylpropanoic acid | 3-[3-tert-Butylsulfanyl-1-(4-chloro-benzyl)-5-isopropyl-1H-indol-2-yl]-2,2-dimethyl-propionic acid | CHEMBL29097 | MK-886 | MK886 | cid_3651377

Type

Small organic molecule

Emp. Form.

C27H34ClNO2S

Mol. Mass.

472.082

SMILES

CC(C)c1ccc2n(Cc3ccc(Cl)cc3)c(CC(C)(C)C(O)=O)c(SC(C)(C)C)c2c1

Structure