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Assay Detail

CHEMBL974538

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

Binding
Inhibition of human liver fructose-1,6-bisphosphatase in presence of fructose-2,6-bisphosphate
44
Total Activities
44
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

Allosteric FBPase inhibitors gain 10(5) times in potency when simultaneously binding two neighboring AMP sites.
Hebeisen P, Kuhn B, Kohler P, Gubler M, Huber W, Kitas E, Schott B, Benz J, Joseph C, Ruf A.
Bioorg Med Chem Lett (2008) 18 : 4708 -4712
PubMed 18650089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 7.28 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL462979 1 8.70
CHEMBL462978 1 8.40
CHEMBL457189 1 8.40
CHEMBL457400 1 8.30
CHEMBL463183 1 8.22
CHEMBL515042 1 8.10
CHEMBL456977 1 8.10
CHEMBL515524 1 8.00
CHEMBL456978 1 7.92
CHEMBL458056 1 7.92
CHEMBL456154 1 7.92
CHEMBL456564 1 7.85
CHEMBL456155 1 7.80
CHEMBL456563 1 7.77
CHEMBL514722 1 7.75
CHEMBL456320 1 7.72
CHEMBL456321 1 7.66
CHEMBL455930 1 7.55
CHEMBL458276 1 7.24
CHEMBL456543 1 6.82
CHEMBL456319 1 6.58
CHEMBL516135 1 6.27
CHEMBL459135 1 4.97
CHEMBL457849 1 4.86
CHEMBL498538 1 4.41
CHEMBL459134 1 4.06
CHEMBL496654 1 -
CHEMBL496653 1 -
CHEMBL458055 1 -
CHEMBL456992 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL462979 IC50 = 2.0 nM 8.70
CHEMBL462978 IC50 = 4.0 nM 8.40
CHEMBL457189 IC50 = 4.0 nM 8.40
CHEMBL457400 IC50 = 5.0 nM 8.30
CHEMBL463183 IC50 = 6.0 nM 8.22
CHEMBL515042 IC50 = 8.0 nM 8.10
CHEMBL456977 IC50 = 8.0 nM 8.10
CHEMBL515524 IC50 = 10.0 nM 8.00
CHEMBL456978 IC50 = 12.0 nM 7.92
CHEMBL458056 IC50 = 12.0 nM 7.92
CHEMBL456154 IC50 = 12.0 nM 7.92
CHEMBL456564 IC50 = 14.0 nM 7.85
CHEMBL456155 IC50 = 16.0 nM 7.80
CHEMBL456563 IC50 = 17.0 nM 7.77
CHEMBL514722 IC50 = 18.0 nM 7.75
CHEMBL456320 IC50 = 19.0 nM 7.72
CHEMBL456321 IC50 = 22.0 nM 7.66
CHEMBL455930 IC50 = 28.0 nM 7.55
CHEMBL458276 IC50 = 57.0 nM 7.24
CHEMBL456543 IC50 = 151.0 nM 6.82
CHEMBL456319 IC50 = 264.0 nM 6.58
CHEMBL516135 IC50 = 542.0 nM 6.27
CHEMBL459135 IC50 = 10589.0 nM 4.97
CHEMBL457849 IC50 = 13727.0 nM 4.86
CHEMBL498538 IC50 = 38530.0 nM 4.41
CHEMBL459134 IC50 = 86763.0 nM 4.06
CHEMBL459023 IC50 - -
CHEMBL442729 IC50 - -
CHEMBL515525 IC50 - -
CHEMBL457848 IC50 - -
CHEMBL457834 IC50 - -
CHEMBL456542 IC50 - -
CHEMBL456541 IC50 - -
CHEMBL462980 IC50 - -
CHEMBL516144 IC50 - -
CHEMBL508325 IC50 - -
CHEMBL526294 IC50 - -
CHEMBL500269 IC50 = 277143.0 nM -
CHEMBL456984 IC50 = 134180.0 nM -
CHEMBL505578 IC50 = 320180.0 nM -
CHEMBL456992 IC50 = 234231.0 nM -
CHEMBL458055 IC50 > 100000.0 nM -
CHEMBL496653 IC50 - -
CHEMBL496654 IC50 > 100000.0 nM -