thioguanine [Ligand Id: 6845] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL727 (Lanvis, NSC-752, NSC-76504, Tabloid, Thioguanine, Thioguanine anhydrous, Thioguanine, anhydrous, Thioguanine hemihydrate, Tioguanine, Tioguanine hemihydrate)
  • 2-amino-4-hydroxy-6-hydroxymethyldihydropteridine pyrophosphokinase in Escherichia coli [ChEMBL: CHEMBL3217379] [UniProtKB: P26281]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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  • mitogen-activated protein kinase 3/MAP kinase ERK1 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
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  • xanthine dehydrogenase/Xanthine dehydrogenase in Human [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
2-amino-4-hydroxy-6-hydroxymethyldihydropteridine pyrophosphokinase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3217379] [UniProtKB: P26281]
ChEMBL Binding affinity to GST-tagged Escherichia coli HPPK expressed in Escherichia coli by SPR assay based alternative equilibrium affinity method in presence of AMP-CPP B 4.74 pKd 18000 nM Kd Bioorg Med Chem (2014) 22: 2157-2165 [PMID:24613625]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 4.91 pKi 12258 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 4.66 pIC50 21687 nM IC50 DrugMatrix in vitro pharmacology data
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) B 4.79 pIC50 16159 nM IC50 DrugMatrix in vitro pharmacology data
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 6.22 pIC50 601 nM IC50 DrugMatrix in vitro pharmacology data
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein) B 5.26 pIC50 5516 nM IC50 DrugMatrix in vitro pharmacology data
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Inhibition of [3H]hypoxanthine uptake in Plasmodium falciparum 3D7 F 4.67 pIC50 21300 nM IC50 J Med Chem (2006) 49: 7479-7486 [PMID:17149876]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 F 5 pIC50 10000 nM IC50 J Med Chem (2006) 49: 7479-7486 [PMID:17149876]
xanthine dehydrogenase/Xanthine dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989]
ChEMBL Inhibition of human xanthine oxidase B 4.03 pIC50 92420 nM IC50 Bioorg Med Chem (2007) 15: 3450-3456 [PMID:17379526]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]