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Assay Detail

CHEMBL5340267

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

Binding
Activation of PKM2 (unknown origin) incubated for 30 mins
2
Total Activities
2
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

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

Publication

Discovery of Novel Sesquiterpene Lactone Derivatives as Potent PKM2 Activators for the Treatment of Ulcerative Colitis.
Wang P, Yang H, Lin W, Zhou J, Liu Y, Ma L, Li M, Hu Y, Yu C, Zhang Y, Lv Q, Liu J, Hu L.
J Med Chem (2023) 66 : 5500 -5523
PubMed 37017305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.26 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5403098 1 6.70
CHEMBL86416 COSTUNOLIDE 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5403098 EC50 = 202.0 nM 6.70
CHEMBL86416 COSTUNOLIDE EC50 = 1513.0 nM 5.82