TEPP-46 [Ligand Id: 10555] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1085588
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
pyruvate kinase M1/2/Pyruvate kinase PKM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075189] [GtoPdb: 3006] [UniProtKB: P14618]
ChEMBL Activation of recombinant human PKM2 expressed in Escherichia coli BL21 at 4 uM incubated for 50 mins measured over 40 mins B 7.04 pEC50 92 nM EC50 J Med Chem (2018) 61: 4155-4164 [PMID:29641204]
ChEMBL Activation of human recombinant full length His-tagged PKM2 (Asp354, Lys311, Glu397, Gly315 residues) B 7.04 pEC50 92 nM EC50 J Med Chem (2022) 65: 1171-1205 [PMID:34726055]
ChEMBL Activation of PKM2 (unknown origin) B 7.05 pEC50 90 nM EC50 J Med Chem (2024) 67: 3339-3357 [PMID:38408027]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]