| Compound ID |
Cluster
|
Compound Type
|
Target/Cell | Structure | Activity | Assay Description | Source | ||||
|---|---|---|---|---|---|---|---|---|---|---|---|
|
Type
|
Relation
|
Value
|
Unit
|
||||||||
| NAs.000008 | 7 | all-match | Fructose-1,6-bisphosphatase |  |
IC50 | > | 10000.0 | nM | Inhibition of human liver FBPase expressed in Escherichia coli by spectrophotometry | CHEMBL1138458 | |
| NAs.000008 | 7 | all-match | Fructose-1,6-bisphosphatase | |
Other | > | 25.0 | % | Inhibition of human liver FBPase expressed in Escherichia coli at 10 uM by spectrophotometry | CHEMBL1138458 | |
| NAs.000716 | 7 | all-match | Fructose-1,6-bisphosphatase |  |
IC50 | = | 13000.0 | nM | Inhibition of human liver FBPase expressed in Escherichia coli by spectrophotometry | CHEMBL1138458 | |
| NAs.001004 | 7 | all-match | Fructose-1,6-bisphosphatase |  |
IC50 | > | 100000.0 | nM | Inhibition of human liver FBPase expressed in Escherichia coli by spectrophotometry | CHEMBL1138458 | |
| NAs.001004 | 7 | all-match | Fructose-1,6-bisphosphatase | |
Other | > | 25.0 | % | Inhibition of human liver FBPase expressed in Escherichia coli at 100 uM by spectrophotometry | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Fructose-1,6-bisphosphatase |  |
IC50 | = | 800.0 | nM | Inhibition of human liver FBPase 1 | CHEMBL1156817 | |
| NAs.001258 | 7 | all-match | Unchecked | |
Other | > | 480.0 | None | Selectivity ratio of IC50 for porcine heart AMP deaminase to IC50 for human liver FBPase | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Rattus norvegicus | |
Other | = | 10.0 | None | Increase in fructose-1,6-bisphosphate level in overnight-fasted Sprague-Dawley rat liver at 20 mg/kg, ip relative to control | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Liver | |
Other | = | 51.3 | nmol/g | Drug concentration in overnight-fasted Sprague-Dawley rat liver at 20 mg/kg, ip after 1 hr | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Rattus norvegicus | |
Other | = | 65.0 | % | Reduction in blood glucose level in overnight-fasted Sprague-Dawley rat at 20 mg/kg, ip within 1 hr | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Rattus norvegicus | |
Other | = | 38.5 | uM | Plasma concentration in overnight-fasted Sprague-Dawley rat at 20 mg/kg, ip after 1 hr | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Hepatocyte | |
Other | None | None | None | Increase in fructose-1,6-bisphosphate substrate level in rat primary hepatocytes at 5 to 50 uM by enzyme-coupled spectrophotometry | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Hepatocyte | |
EC50 | = | 90000.0 | nM | Inhibition of glucose production in rat primary hepatocytes treated for 15 to 30 mins prior to gluconeogenic substrate dihydroxyacetone addition | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Unchecked | |
Other | < | 2.0 | None | Selectivity ratio of IC50 for rat liver FBPase to IC50 for human liver FBPase | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Rattus norvegicus | |
Other | = | 1.6 | % | Oral bioavailability in fasted Sprague-Dawley rat assessed as urinary excretion of phosphonic acid up to 300 mg/kg | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Hepatocyte | |
Other | None | None | None | Inhibition of glucose production in rat primary hepatocytes treated for 15 to 30 mins prior to gluconeogenic substrate dihydroxyacetone addition | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Fructose-1,6-bisphosphatase | |
IC50 | = | 1250.0 | nM | Inhibition of rat liver FBPase | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Adenosine kinase | |
IC50 | > | 100000.0 | nM | Inhibition of human recombinant adenosine kinase expressed in Escherichia coli | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Adenylate kinase isoenzyme 1 | |
IC50 | > | 500000.0 | nM | Inhibition of rabbit muscle adenylate kinase | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Fructose-1,6-bisphosphatase | |
IC50 | = | 800.0 | nM | Inhibition of human liver FBPase expressed in Escherichia coli by spectrophotometry | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Glycogen phosphorylase, muscle form | |
EC50 | > | 100000.0 | nM | Inhibition of rabbit muscle glycogen phosphorylase | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Unchecked | |
EC50 | > | 100000.0 | nM | Inhibition of New Zealand white rabbit liver phosphofructokinase | CHEMBL1138458 | |
| NAs.001258 | 7 | all-match | Unchecked | |
IC50 | = | 390000.0 | nM | Inhibition of pig heart AMP deaminase | CHEMBL1138458 | |
| NAs.001949 | 7 | all-match | Fructose-1,6-bisphosphatase |  |
IC50 | = | 1100.0 | nM | Inhibition of human liver FBPase expressed in Escherichia coli by spectrophotometry | CHEMBL1138458 | |
| NAs.001949 | 7 | all-match | Hepatocyte | |
EC50 | = | 8500.0 | nM | Inhibition of glucose production in rat primary hepatocytes treated for 15 to 30 mins prior to gluconeogenic substrate dihydroxyacetone addition | CHEMBL1138458 | |
| NAs.001949 | 7 | all-match | Fructose-1,6-bisphosphatase | |
IC50 | = | 4000.0 | nM | Inhibition of rat liver FBPase | CHEMBL1138458 | |
| NAs.001959 | 7 | all-match | Fructose-1,6-bisphosphatase |  |
IC50 | = | 5500.0 | nM | Inhibition of human liver FBPase expressed in Escherichia coli by spectrophotometry | CHEMBL1138458 | |
| NAs.002704 | 7 | all-match | Fructose-1,6-bisphosphatase |  |
IC50 | > | 10000.0 | nM | Inhibition of human liver FBPase expressed in Escherichia coli by spectrophotometry | CHEMBL1138458 | |
| NAs.002704 | 7 | all-match | Fructose-1,6-bisphosphatase | |
Other | > | 25.0 | % | Inhibition of human liver FBPase expressed in Escherichia coli at 10 uM by spectrophotometry | CHEMBL1138458 | |
| NAs.002801 | 7 | all-match | Fructose-1,6-bisphosphatase |  |
IC50 | > | 10000.0 | nM | Inhibition of human liver FBPase expressed in Escherichia coli by spectrophotometry | CHEMBL1138458 | |
| NAs.002801 | 7 | all-match | Fructose-1,6-bisphosphatase | |
Other | > | 25.0 | % | Inhibition of human liver FBPase expressed in Escherichia coli at 10 uM by spectrophotometry | CHEMBL1138458 | |