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Literature summary for 2.7.1.6 extracted from

  • Liu, L.; Tang, M.; Walsh, M.J.; Brimacombe, K.R.; Pragani, R.; Tanega, C.; Rohde, J.M.; Baker, H.L.; Fernandez, E.; Blackman, B.; Bougie, J.M.; Leister, W.H.; Auld, D.S.; Shen, M.; Lai, K.; Boxer, M.B.
    Structure activity relationships of human galactokinase inhibitors (2015), Bioorg. Med. Chem. Lett., 25, 721-727.
    View publication on PubMed
Search for more literature for 2.7.1.6

Application

Application Comment Organism
medicine in primary fibroblasts of patients suffering Classic Galactosemia, inhibitor 2-(1,3-benzoxazol-2-ylamino)-4-(4-chloro-1H-pyrazol-3-yl)-4,6,7,8-tetrahydroquinazolin-5(1H)-one is able to lower galactose 1-phosphate levels without significant effect on viability of cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(1,3-benzoxazol-2-ylamino)-4-(4-chloro-1H-pyrazol-3-yl)-4,6,7,8-tetrahydroquinazolin-5(1H)-one inhibitory to isoform Galk1, no inhibition of isoform Galk2 up to 40 microM. Uncompetitive with respect to galactose, compound directly competes with ATP at the binding site, and galactose may be required to bind first. Compound is able to lower galactose 1-phosphate levels in primary fibroblasts of patients suffering Classic Galactosemia without significant effect on viability of cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0047
-
 isoform Galk1, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(1,3-benzoxazol-2-ylamino)-4-(4-chloro-1H-pyrazol-3-yl)-4,6,7,8-tetrahydroquinazolin-5(1H)-one