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Assay Detail

CHEMBL4182153

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

Binding
Inhibition of recombinant human N-terminal His6/SUMO-tagged PKM2 expressed in Escherichia coli BL21 using PEP as substrate incubated for 30 mins in presence of ADP by spectrophotometric based LDH enzyme coupled assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Pyruvate kinase PKM (CHEMBL1075189)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Scutellarin inhibits Hela cell growth and glycolysis by inhibiting the activity of pyruvate kinase M2.
You L, Zhu H, Wang C, Wang F, Li Y, Li Y, Wang Y, He B.
Bioorg Med Chem Lett (2017) 27 : 5404 -5408
PubMed 29157862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.37 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9470 SHIKONIN 1 6.30
CHEMBL214344 1 4.90
CHEMBL55415 SCUTELLAREIN 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9470 SHIKONIN IC50 = 500.0 nM 6.30
CHEMBL214344 IC50 = 12500.0 nM 4.90
CHEMBL55415 SCUTELLAREIN IC50 = 12500.0 nM 4.90