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Assay Detail

CHEMBL1074153

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

Binding
Inhibition of human liver recombinant FBPase
19
Total Activities
19
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

Structure-based drug design of tricyclic 8H-indeno[1,2-d][1,3]thiazoles as potent FBPase inhibitors.
Tsukada T, Takahashi M, Takemoto T, Kanno O, Yamane T, Kawamura S, Nishi T.
Bioorg Med Chem Lett (2010) 20 : 1004 -1007
PubMed 20045638 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.70 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL589266 1 9.00
CHEMBL597891 1 8.70
CHEMBL597692 1 8.52
CHEMBL597484 1 8.10
CHEMBL597282 1 8.10
CHEMBL592639 1 8.05
CHEMBL597691 1 8.05
CHEMBL605956 1 8.05
CHEMBL609616 1 8.00
CHEMBL495498 MB-05032 2.0 1 8.00
CHEMBL592391 1 7.96
CHEMBL592390 1 7.92
CHEMBL597483 1 7.82
CHEMBL606385 1 7.55
CHEMBL603871 1 7.40
CHEMBL567704 1 6.91
CHEMBL597068 1 6.11
CHEMBL596870 1 6.04
CHEMBL603409 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL589266 IC50 = 1.0 nM 9.00
CHEMBL597891 IC50 = 2.0 nM 8.70
CHEMBL597692 IC50 = 3.0 nM 8.52
CHEMBL597484 IC50 = 8.0 nM 8.10
CHEMBL597282 IC50 = 8.0 nM 8.10
CHEMBL592639 IC50 = 9.0 nM 8.05
CHEMBL597691 IC50 = 9.0 nM 8.05
CHEMBL605956 IC50 = 9.0 nM 8.05
CHEMBL609616 IC50 = 10.0 nM 8.00
CHEMBL495498 MB-05032 IC50 = 10.0 nM 8.00
CHEMBL592391 IC50 = 11.0 nM 7.96
CHEMBL592390 IC50 = 12.0 nM 7.92
CHEMBL597483 IC50 = 15.0 nM 7.82
CHEMBL606385 IC50 = 28.0 nM 7.55
CHEMBL603871 IC50 = 40.0 nM 7.40
CHEMBL567704 IC50 = 124.0 nM 6.91
CHEMBL597068 IC50 = 772.0 nM 6.11
CHEMBL596870 IC50 = 908.0 nM 6.04
CHEMBL603409 IC50 = 995.0 nM 6.00