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Assay Detail

CHEMBL5531335

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

Binding
Activation of PKM2 (unknown origin)
5
Total Activities
5
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

Mechanistic Investigation of Thiazole-Based Pyruvate Kinase M2 Inhibitor Causing Tumor Regression in Triple-Negative Breast Cancer.
Das R, Pulugu P, Singh AA, Chatterjee DR, Baviskar S, Vyas H, Behera SK, Srivastava A, Kumar H, Shard A.
J Med Chem (2024) 67 : 3339 -3357
PubMed 38408027 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.56 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL449579 MICHELIOLIDE 1 8.22
CHEMBL4299940 MITAPIVAT 4.0 1 7.70
CHEMBL1089334 1 7.52
CHEMBL5274026 1 7.30
CHEMBL1085588 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL449579 MICHELIOLIDE EC50 = 6.0 nM 8.22
CHEMBL4299940 MITAPIVAT EC50 = 20.0 nM 7.70
CHEMBL1089334 EC50 = 30.0 nM 7.52
CHEMBL5274026 EC50 = 50.0 nM 7.30
CHEMBL1085588 EC50 = 90.0 nM 7.05