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Assay Detail

CHEMBL1074685

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of FBPase in human liver using fructose-2,6phosphate as a substrate
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Sulfonylureido thiazoles as fructose-1,6-bisphosphatase inhibitors for the treatment of type-2 diabetes.
Kitas E, Mohr P, Kuhn B, Hebeisen P, Wessel HP, Haap W, Ruf A, Benz J, Joseph C, Huber W, Sanchez RA, Paehler A, Benardeau A, Gubler M, Schott B, Tozzo E.
Bioorg Med Chem Lett (2010) 20 : 594 -599
PubMed 19969452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.90 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL590111 1 7.52
CHEMBL590359 1 7.52
CHEMBL589863 1 7.40
CHEMBL590597 1 7.40
CHEMBL590839 1 7.30
CHEMBL601691 1 7.30
CHEMBL590361 1 7.22
CHEMBL593282 1 7.16
CHEMBL589865 1 7.16
CHEMBL610462 1 7.10
CHEMBL595529 1 7.05
CHEMBL594444 1 7.05
CHEMBL611631 1 7.05
CHEMBL589137 1 7.00
CHEMBL595150 1 7.00
CHEMBL595149 1 6.96
CHEMBL590360 1 6.92
CHEMBL752 ADENOSINE PHOSPHATE 4.0 1 6.85
CHEMBL589862 1 6.85
CHEMBL589861 1 6.77
CHEMBL594445 1 6.72
CHEMBL590840 1 6.72
CHEMBL585620 1 6.68
CHEMBL608398 1 6.54
CHEMBL585961 1 6.46
CHEMBL594668 1 6.42
CHEMBL595067 1 6.42
CHEMBL595304 1 6.14
CHEMBL607540 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL590111 IC50 = 30.0 nM 7.52
CHEMBL590359 IC50 = 30.0 nM 7.52
CHEMBL589863 IC50 = 40.0 nM 7.40
CHEMBL590597 IC50 = 40.0 nM 7.40
CHEMBL590839 IC50 = 50.0 nM 7.30
CHEMBL601691 IC50 = 50.0 nM 7.30
CHEMBL590361 IC50 = 60.0 nM 7.22
CHEMBL593282 IC50 = 70.0 nM 7.16
CHEMBL589865 IC50 = 70.0 nM 7.16
CHEMBL610462 IC50 = 80.0 nM 7.10
CHEMBL595529 IC50 = 90.0 nM 7.05
CHEMBL594444 IC50 = 90.0 nM 7.05
CHEMBL611631 IC50 = 90.0 nM 7.05
CHEMBL589137 IC50 = 100.0 nM 7.00
CHEMBL595150 IC50 = 100.0 nM 7.00
CHEMBL595149 IC50 = 110.0 nM 6.96
CHEMBL590360 IC50 = 120.0 nM 6.92
CHEMBL752 ADENOSINE PHOSPHATE IC50 = 140.0 nM 6.85
CHEMBL589862 IC50 = 140.0 nM 6.85
CHEMBL589861 IC50 = 170.0 nM 6.77
CHEMBL594445 IC50 = 190.0 nM 6.72
CHEMBL590840 IC50 = 190.0 nM 6.72
CHEMBL585620 IC50 = 210.0 nM 6.68
CHEMBL608398 IC50 = 290.0 nM 6.54
CHEMBL585961 IC50 = 350.0 nM 6.46
CHEMBL594668 IC50 = 380.0 nM 6.42
CHEMBL595067 IC50 = 380.0 nM 6.42
CHEMBL595304 IC50 = 720.0 nM 6.14
CHEMBL607540 IC50 = 3500.0 nM 5.46