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Literature summary for 2.4.1.1 extracted from

  • Sparks, S.M.; Banker, P.; Bickett, D.M.; Clancy, D.C.; Dickerson, S.H.; Garrido, D.M.; Golden, P.L.; Peat, A.J.; Sheckler, L.R.; Tavares, F.X.; Thomson, S.A.; Weiel, J.E.
    Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of Type 2 diabetes: 2. Optimization of serine and threonine ether amino acid residues (2009), Bioorg. Med. Chem. Lett., 19, 981-985.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-cyclohexyl-2-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]propanoic acid potent in vitro inhibition, reduced inhibition of CYP2C9 and good pharmacokinetic properties Homo sapiens
(2S)-cyclohexyl[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]ethanoic acid
-
Homo sapiens
(2S)-cyclopentyl[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]ethanoic acid
-
Homo sapiens
1-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]cyclodecanecarboxylic acid
-
Homo sapiens
1-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]cyclooctanecarboxylic acid potent in vitro inhibition, reduced inhibition of CYP2C9 and good pharmacokinetic properties Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
phosphorylase a
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000005
-
-
Homo sapiens 1-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]cyclooctanecarboxylic acid
0.000006
-
-
Homo sapiens (2S)-cyclohexyl[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]ethanoic acid
0.00001
-
-
Homo sapiens (2R)-2-cyclohexyl-2-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]propanoic acid
0.000014
-
-
Homo sapiens (2S)-cyclopentyl[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]ethanoic acid
0.000014
-
-
Homo sapiens 1-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]cyclodecanecarboxylic acid