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Assay Detail

CHEMBL3106987

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Binding
Inhibition of PFKFB3 (unknown origin)
5
Total Activities
5
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

Publication

Targeting the Warburg Effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3).
Brooke DG, van Dam EM, Watts CK, Khoury A, Dziadek MA, Brooks H, Graham LJ, Flanagan JU, Denny WA.
Bioorg Med Chem (2014) 22 : 1029 -1039
PubMed 24398380 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.22 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL242739 1 6.17
CHEMBL234338 1 5.53
CHEMBL3105848 1 4.60
CHEMBL3105838 1 4.57
CHEMBL3105837 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL242739 IC50 = 670.0 nM 6.17
CHEMBL234338 IC50 = 2970.0 nM 5.53
CHEMBL3105848 IC50 = 25000.0 nM 4.60
CHEMBL3105838 IC50 = 27000.0 nM 4.57
CHEMBL3105837 IC50 > 1000000.0 nM -