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Assay Detail

CHEMBL5223207

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

Binding
Inhibition of PKM2 (unknown origin)
23
Total Activities
23
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

Tumor pyruvate kinase M2 modulators: a comprehensive account of activators and inhibitors as anticancer agents.
Rathod B, Chak S, Patel S, Shard A.
RSC Med Chem (2021) 12 : 1121 -1141
PubMed 34355179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.52 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413 SIROLIMUS 4.0 1 7.30
CHEMBL3609603 1 6.19
CHEMBL126142 1 6.07
CHEMBL31574 FISETIN 2.0 1 6.05
CHEMBL28 APIGENIN 1 6.00
CHEMBL66 (+)-TAXIFOLIN 1 5.94
CHEMBL80941 1 5.88
CHEMBL15193 LAPACHOL 1 5.85
CHEMBL9470 SHIKONIN 1 5.85
CHEMBL4877010 1 5.70
CHEMBL4128703 1 5.53
CHEMBL214344 1 5.00
CHEMBL32749 FERULATE -1.0 1 4.94
CHEMBL1414 SYRINGIC ACID 1 4.86
CHEMBL3695457 1 4.70
CHEMBL15870 INDOPROFEN 4.0 1 4.68
CHEMBL265502 SURAMIN 3.0 1 4.48
CHEMBL5 NALIDIXIC ACID 4.0 1 4.28
CHEMBL477197 HEMATOXYLIN 1 -
CHEMBL5288302 1 -
CHEMBL187266 TANSHINONE IIA 1 -
CHEMBL142652 PICEID 2.0 1 -
CHEMBL25080 DL-PHENYLALANINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413 SIROLIMUS IC50 = 50.0 nM 7.30
CHEMBL3609603 IC50 = 650.0 nM 6.19
CHEMBL126142 IC50 = 850.0 nM 6.07
CHEMBL31574 FISETIN IC50 = 900.0 nM 6.05
CHEMBL28 APIGENIN IC50 = 990.0 nM 6.00
CHEMBL66 (+)-TAXIFOLIN IC50 = 1160.0 nM 5.94
CHEMBL80941 IC50 = 1330.0 nM 5.88
CHEMBL15193 LAPACHOL IC50 = 1400.0 nM 5.85
CHEMBL9470 SHIKONIN IC50 = 1420.0 nM 5.85
CHEMBL4877010 IC50 = 2000.0 nM 5.70
CHEMBL4128703 IC50 = 2950.0 nM 5.53
CHEMBL214344 IC50 = 10000.0 nM 5.00
CHEMBL32749 FERULATE IC50 = 11400.0 nM 4.94
CHEMBL1414 SYRINGIC ACID IC50 = 13800.0 nM 4.86
CHEMBL3695457 IC50 = 20000.0 nM 4.70
CHEMBL15870 INDOPROFEN IC50 = 21000.0 nM 4.68
CHEMBL265502 SURAMIN IC50 = 33000.0 nM 4.48
CHEMBL5 NALIDIXIC ACID IC50 = 53000.0 nM 4.28
CHEMBL477197 HEMATOXYLIN IC50 = 340000.0 nM -
CHEMBL5288302 IC50 - -
CHEMBL187266 TANSHINONE IIA IC50 = 1920000.0 nM -
CHEMBL142652 PICEID IC50 = 128000.0 nM -
CHEMBL25080 DL-PHENYLALANINE IC50 = 240000.0 nM -