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Assay Detail

CHEMBL1074686

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

Binding
Inhibition of FBPase in mouse liver
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fructose-1,6-bisphosphatase 1 (CHEMBL5360)
Type SINGLE PROTEIN
Organism Mus musculus

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
EC50 40 4.80 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL591083 1 5.62
CHEMBL605615 1 5.55
CHEMBL589863 1 5.50
CHEMBL590363 1 5.28
CHEMBL590361 1 5.26
CHEMBL601267 1 5.20
CHEMBL573056 1 5.19
CHEMBL600654 1 5.09
CHEMBL590111 1 5.05
CHEMBL601691 1 5.05
CHEMBL602789 1 5.04
CHEMBL591316 1 5.00
CHEMBL611631 1 5.00
CHEMBL590360 1 5.00
CHEMBL585620 1 4.92
CHEMBL590359 1 4.89
CHEMBL590840 1 4.85
CHEMBL590113 1 4.85
CHEMBL590362 1 4.85
CHEMBL591317 1 4.82
CHEMBL590839 1 4.75
CHEMBL589862 1 4.72
CHEMBL590597 1 4.72
CHEMBL589861 1 4.64
CHEMBL593282 1 4.62
CHEMBL595150 1 4.62
CHEMBL585961 1 4.57
CHEMBL589137 1 4.50
CHEMBL589865 1 4.47
CHEMBL600653 1 4.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL591083 EC50 = 2400.0 nM 5.62
CHEMBL605615 EC50 = 2800.0 nM 5.55
CHEMBL589863 EC50 = 3200.0 nM 5.50
CHEMBL590363 EC50 = 5300.0 nM 5.28
CHEMBL590361 EC50 = 5500.0 nM 5.26
CHEMBL601267 EC50 = 6300.0 nM 5.20
CHEMBL573056 EC50 = 6500.0 nM 5.19
CHEMBL600654 EC50 = 8100.0 nM 5.09
CHEMBL590111 EC50 = 9000.0 nM 5.05
CHEMBL601691 EC50 = 9000.0 nM 5.05
CHEMBL602789 EC50 = 9200.0 nM 5.04
CHEMBL591316 EC50 = 10000.0 nM 5.00
CHEMBL590360 EC50 = 10000.0 nM 5.00
CHEMBL611631 EC50 = 10000.0 nM 5.00
CHEMBL585620 EC50 = 12000.0 nM 4.92
CHEMBL590359 EC50 = 13000.0 nM 4.89
CHEMBL590840 EC50 = 14000.0 nM 4.85
CHEMBL590113 EC50 = 14000.0 nM 4.85
CHEMBL590362 EC50 = 14000.0 nM 4.85
CHEMBL591317 EC50 = 15000.0 nM 4.82
CHEMBL590839 EC50 = 18000.0 nM 4.75
CHEMBL590597 EC50 = 19000.0 nM 4.72
CHEMBL589862 EC50 = 19000.0 nM 4.72
CHEMBL589861 EC50 = 23000.0 nM 4.64
CHEMBL593282 EC50 = 24000.0 nM 4.62
CHEMBL595150 EC50 = 24000.0 nM 4.62
CHEMBL585961 EC50 = 27000.0 nM 4.57
CHEMBL589137 EC50 = 32000.0 nM 4.50
CHEMBL589865 EC50 = 34000.0 nM 4.47
CHEMBL600653 EC50 = 42000.0 nM 4.38
CHEMBL595149 EC50 = 49000.0 nM 4.31
CHEMBL594444 EC50 = 62000.0 nM 4.21
CHEMBL595529 EC50 = 63000.0 nM 4.20
CHEMBL608398 EC50 = 74000.0 nM 4.13
CHEMBL610462 EC50 = 87000.0 nM 4.06
CHEMBL594445 EC50 = 92000.0 nM 4.04
CHEMBL595304 EC50 > 100000.0 nM -
CHEMBL594668 EC50 > 100000.0 nM -
CHEMBL607540 EC50 > 100000.0 nM -
CHEMBL595067 EC50 = 118000.0 nM -