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Assay Detail

CHEMBL4189263

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

Binding
Activation of recombinant human PKM2 expressed in Escherichia coli BL21 at 4 uM incubated for 50 mins measured over 40 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 Intermediate

Target

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

Publication

Natural Product Micheliolide (MCL) Irreversibly Activates Pyruvate Kinase M2 and Suppresses Leukemia.
Li J, Li S, Guo J, Li Q, Long J, Ma C, Ding Y, Yan C, Li L, Wu Z, Zhu H, Li KK, Wen L, Zhang Q, Xue Q, Zhao C, Liu N, Ivanov I, Luo M, Xi R, Long H, Wang PG, Chen Y.
J Med Chem (2018) 61 : 4155 -4164
PubMed 29641204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.63 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL449579 MICHELIOLIDE 1 8.22
CHEMBL1085588 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL449579 MICHELIOLIDE EC50 = 6.0 nM 8.22
CHEMBL1085588 EC50 = 92.0 nM 7.04