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Report error Found 397 Enz. Inhib. hit(s) with Target = 'Pyruvate kinase PKM'
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50645005(CHEMBL5572369)
Affinity DataKd:  0.0280nMAssay Description:Binding affinity to PKM2 (unknown origin) assessed as dissociation rate constant (Kd) at 3.125 to 50 uM by SPR analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM18073(L-[2,3,4,5,6-3H]phenylalanine | (2S)-2-amino-3-phe...)
Affinity DataIC50: 0.0550nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM15236(CHEMBL164 | Cannabiscetin | 3,5,7-trihydroxy-2-(3,...)
Affinity DataEC50:  0.510nMAssay Description:Activation of recombinant PKM2 (unknown origin) Phe26, Tyr390, Glu397, Asp354, Leu353 residuesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50646189(CHEMBL5590652)
Affinity DataEC50:  0.600nMAssay Description:Activation of PKM2 (unknown origin) by LDH enzyme coupled assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641060(CHEMBL5569778)
Affinity DataKd:  0.915nMAssay Description:Binding affinity to human PKM2 expressed in Escherichia coli assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50241354(Quercetin 3-O-beta-D-glucoside | quercetin 3-O-glu...)
Affinity DataEC50:  1.30nMAssay Description:Activation of recombinant PKM2 (unknown origin) Glu397, Lys3I I, Asp354, Leu353, Tyr390, His391 residuesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641057(CHEMBL5573729)
Affinity DataIC50: 1.70nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50621639(CHEMBL5403098)
Affinity DataKd:  1.80nMAssay Description:Binding affinity to PKM2 (unknown origin) by SPR assayMore data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
12/16/2024
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50645005(CHEMBL5572369)
Affinity DataKd:  2.5nMAssay Description:Binding affinity to PKM2 (unknown origin) assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50623415(CHEMBL5434086)
Affinity DataKd:  2.80nMAssay Description:Binding affinity to PKM2 (unknown origin) assessed as dissociation constant associated for 60 secs and dissociated for 90 secs by bio-layer interfero...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641071(CHEMBL5563349)
Affinity DataIC50: 4.5nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50455476(CHEBI:6922 | Micheliolide)
Affinity DataEC50:  6nMAssay Description:Activation of PKM2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50455476(CHEBI:6922 | Micheliolide)
Affinity DataEC50:  6nMAssay Description:Activation of recombinant human PKM2 expressed in Escherichia coli BL21 at 4 uM incubated for 50 mins measured over 40 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50022801(CHEMBL5274026)
Affinity DataEC50:  7.10nMAssay Description:Activation of PKM2 (unknown origin) in presence of sorafenibMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details Article
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641069(CHEMBL5570128)
Affinity DataIC50: 8.80nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641073(CHEMBL5575015)
Affinity DataIC50: 12nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50631999(CHEMBL5396216)
Affinity DataIC50: 16nMAssay Description:Binding affinity to wild type FLAG-tagged PKM2 in human PA-1 cells measured for 72 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641070(CHEMBL5595787)
Affinity DataIC50: 16nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641076(CHEMBL5590701)
Affinity DataIC50: 18nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641065(CHEMBL5571324)
Affinity DataIC50: 18nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50597714(Mitapivat | Ag-348 | Pkr-in-1 | AG-348 | MITAPIVAT...)
Affinity DataIC50: 20nMAssay Description:Inhibition of PKM2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50597714(Mitapivat | Ag-348 | Pkr-in-1 | AG-348 | MITAPIVAT...)
Affinity DataEC50:  20nMAssay Description:Activation of PKM2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50434635(CHEMBL2385099)
Affinity DataEC50:  22nMAssay Description:Activation of PKM2 in human Huh7 cells assessed as production of pyruvate and ATP by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50597704(CHEBI:28013 | Fosfructose | FOSFRUCTOSE)
Affinity DataEC50:  23nMAssay Description:Activation of PKM2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641060(CHEMBL5569778)
Affinity DataIC50: 23nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641833(CHEMBL5564394)
Affinity DataIC50: 27nMAssay Description:Inhibition of recombinant PKM2 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50361557(CHEMBL1089334)
Affinity DataEC50:  30nMAssay Description:Activation of PKM2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641064(CHEMBL5570684)
Affinity DataIC50: 33nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641075(CHEMBL5571984)
Affinity DataIC50: 36nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50597714(Mitapivat | Ag-348 | Pkr-in-1 | AG-348 | MITAPIVAT...)
Affinity DataEC50:  37nMAssay Description:Activation of PKM2 (unknown origin) Lys311, Asp354, Met30, Phe26 residuesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50361557(CHEMBL1089334)
Affinity DataEC50:  38nMAssay Description:Activation of human PKM2 assessed as ATP product formation after 1 hr by luminescent pyruvate kinase-luciferase coupled assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50361557(CHEMBL1089334)
Affinity DataEC50:  38nMAssay Description:Activation of human recombinant full length His-tagged PKM2 (Asp354, Lys311, Glu397, Gly315 residues)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50597709(CHEMBL1084625)
Affinity DataEC50:  38nMAssay Description:Activation of PKM2 (unknown origin) Phe26, Tyr390, Glu397, Leu353 residuesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50361557(CHEMBL1089334)
Affinity DataEC50:  38nMAssay Description:Activation of PKM2 (unknown origin) Asp354, Phe26, Lys311 residuesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641061(CHEMBL5592948)
Affinity DataIC50: 45nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 50nMAssay Description:Inhibition of PKM2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details Article
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641824(CHEMBL5566865)
Affinity DataIC50: 50nMAssay Description:Inhibition of recombinant PKM2 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50455474(CHEMBL4218770)
Affinity DataKi:  50nMAssay Description:Irreversible binding affinity to recombinant human PKM2 expressed in Escherichia coli BL21More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50022801(CHEMBL5274026)
Affinity DataEC50:  50nMAssay Description:Activation of PKM2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 50nMAssay Description:Inhibition of PKM2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641078(CHEMBL5565744)
Affinity DataIC50: 54nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50597712(CHEMBL5179096)
Affinity DataEC50:  56nMAssay Description:Activation of PKM2 (unknown origin) Leu353, Tyr390, Phe26, Glu397, Lys311, Asp354 residuesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50361491(CHEMBL1939112)
Affinity DataEC50:  60nMAssay Description:Activation of human PKM2 assessed as ATP product formation after 1 hr by luminescent pyruvate kinase-luciferase coupled assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641831(CHEMBL5591146)
Affinity DataIC50: 60nMAssay Description:Inhibition of recombinant PKM2 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641080(CHEMBL5564291)
Affinity DataIC50: 61nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM719702(6-((1H-pyrazol-4-yl)sulfonyl)-2-((1-cyclopropyl-1H...)
Affinity DataEC50:  64.5nMAssay Description:Human PKM2 was diluted into Assay Buffer comprising 50 mM imidazole, 50 mM KCl, 7 mM MgCl2, 0.01% Tween20, 0.05% BSA (pH 7.2) to a final concentratio...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
6/17/2025
Entry Details
Go to US Patent

TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641074(CHEMBL5595221)
Affinity DataIC50: 67nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50641077(CHEMBL5589630)
Affinity DataIC50: 68nMAssay Description:Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50434636(CHEMBL2386917)
Affinity DataEC50:  70nMAssay Description:Activation of PKM2 in human Huh7 cells assessed as production of pyruvate and ATP by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetPyruvate kinase PKM(Human)
Nanjing University of Chinese Medicine

Curated by ChEMBL
LigandPNGBDBM50361488(CHEMBL1939115)
Affinity DataEC50:  70nMAssay Description:Activation of human PKM2 assessed as ATP product formation after 1 hr by luminescent pyruvate kinase-luciferase coupled assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
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