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Assay Detail

CHEMBL5137733

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

Binding
Activation of human recombinant full length His-tagged PKM2 (Asp354, Lys311, Glu397, Gly315 residues)
4
Total Activities
2
Compounds Tested
2
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

A Perspective on Medicinal Chemistry Approaches for Targeting Pyruvate Kinase M2.
Arora S, Joshi G, Chaturvedi A, Heuser M, Patil S, Kumar R.
J Med Chem (2022) 65 : 1171 -1205
PubMed 34726055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.23 7.42
EC90 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1089334 2 7.42
CHEMBL1085588 2 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1089334 EC50 = 38.0 nM 7.42
CHEMBL1085588 EC50 = 92.0 nM 7.04
CHEMBL1089334 EC90 = 680.0 nM -
CHEMBL1085588 EC90 = 470.0 nM -