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Literature summary for 2.4.1.1 extracted from

  • Sparks, S.M.; Banker, P.; Bickett, D.M.; Carter, H.L.; Clancy, D.C.; Dickerson, S.H.; Dwornik, K.A.; Garrido, D.M.; Golden, P.L.; Nolte, R.T.; Peat, A.J.; Sheckler, L.R.; Tavares, F.X.; Thomson, S.A.; Wang, L.; Weiel, J.E.
    Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes: 1. Identification of 1-amino-1-cycloalkyl carboxylic acid headgroups (2009), Bioorg. Med. Chem. Lett., 19, 976-980.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]heptanoic acid
-
 Homo sapiens
N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-norleucine potent in vitro inhibition, low potential for P450 inhibition, and good pharmacokinetic properties Homo sapiens
O-(1-methylcyclopentyl)-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-allothreonine
-
 Homo sapiens
O-tert-butyl-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-allothreonine potent in vitro inhibition, low potential for P450 inhibition, and good pharmacokinetic properties Homo sapiens
O-tert-butyl-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-serine potent in vitro inhibition, low potential for P450 inhibition, and good pharmacokinetic properties Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P06737 phosphorylase a
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000006
-
-
 Homo sapiens O-(1-methylcyclopentyl)-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-allothreonine
0.000007
-
-
 Homo sapiens O-tert-butyl-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-allothreonine
0.000009
-
-
 Homo sapiens (2S)-2-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]heptanoic acid
0.000023
-
-
 Homo sapiens N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-norleucine
0.000044
-
-
 Homo sapiens O-tert-butyl-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-serine