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Assay Detail

CHEMBL5514462

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

Binding
Inhibition of full length N-terminal His-tagged human PKL (2 to 543 residues) expressed in Escherichia coli by kinase Glo luminescence based plate reader assay
4
Total Activities
4
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 PKLR (CHEMBL1075126)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Sulfone-based human liver pyruvate kinase inhibitors - Design, synthesis and in vitro bioactivity.
Matić J, Akladios F, Battisti UM, Håversen L, Nain-Perez A, Füchtbauer AF, Kim W, Monjas L, Rivero AR, Borén J, Mardinoglu A, Uhlen M, Grøtli M.
Eur J Med Chem (2024) 269 : 116306 -116306
PubMed 38471358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.15 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6338 1 7.55
CHEMBL6246 ELLAGIC ACID 2.0 1 7.50
CHEMBL5556210 1 7.16
CHEMBL4754666 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6338 IC50 = 28.0 nM 7.55
CHEMBL6246 ELLAGIC ACID IC50 = 32.0 nM 7.50
CHEMBL5556210 IC50 = 70.0 nM 7.16
CHEMBL4754666 IC50 = 410.0 nM 6.39