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Assay Detail

CHEMBL3888069

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Binding
Spectrophotometrical Assay: FBPase activity was measured spectrophotometrically by employing the coupling enzymes phosphoglucose isomerase and glucose-6-phosphate dehydrogenase.17 The reduction of NADP+ to NADPH was monitored directly at 340 nm. Specifically, buffer (0.2 M Tris, 4 mM MgCl2, 4 mM (NH4)2SO4, 0.1 EDTA, pH 7.5), 0.2 mM of NADP+, 1.4 units of phosphoglucose isomerase and 0.5 units of glucose-6-phosphate dehydrogenase, 0-300M of inhibitor and 9 ng of FBPase, were mixed in a cuvette and equilibrated at 30° C. 70M of FBP was then added to initiate the reaction. Absdata were collected as a function of time using a JASCO V-630 spectrophotometer.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Fructose-1,6-bisphosphatase 1 (CHEMBL3975)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dibenzofuran derivatives as inhibitors of fructose 1,6-bisphosphatase and methods of use thereof
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.16 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1097227 1 5.22
CHEMBL1097226 1 5.09
CHEMBL242022 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1097227 IC50 = 6000.0 nM 5.22
CHEMBL1097226 IC50 = 8100.0 nM 5.09
CHEMBL242022 IC50 = 371000.0 nM -