GF109203X [Ligand Id: 5193] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL7463 (GF-109203, GF-109203X)
  • Anthrax lethal factor in Bacillus anthracis [ChEMBL: CHEMBL4372] [UniProtKB: P15917]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Rat [ChEMBL: CHEMBL3669] [GtoPdb: 2030] [UniProtKB: P18266]
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  • sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6]
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  • sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
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  • protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
  • protein kinase C alpha in Bovine [GtoPdb: 1482]
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  • protein kinase C beta/Protein kinase C beta in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
  • protein kinase C beta in Bovine [GtoPdb: 1483]
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  • protein kinase C delta/Protein kinase C delta in Human [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
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  • protein kinase C epsilon/Protein kinase C epsilon in Human [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
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  • protein kinase C eta/Protein kinase C eta in Human [ChEMBL: CHEMBL3616] [GtoPdb: 1487] [UniProtKB: P24723]
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  • protein kinase C gamma/Protein kinase C gamma in Human [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129]
  • protein kinase C gamma in Bovine [GtoPdb: 1484]
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  • protein kinase C iota/Protein kinase C iota in Human [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743]
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  • protein kinase C theta/Protein kinase C theta in Human [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
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  • protein kinase C zeta/Protein kinase C zeta in Human [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513]
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  • Protein kinase Pfmrk in Plasmodium falciparum [ChEMBL: CHEMBL4090] [UniProtKB: P90584]
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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Anthrax lethal factor in Bacillus anthracis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4372] [UniProtKB: P15917]
ChEMBL Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay B 5.82 pIC50 1500 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 2403-2411 [PMID:17485504]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067P06493P14635Q8WWL7]
ChEMBL Inhibitory concentration was determined by measuring phosphorylation of H1 histone using active human Cell division cycle 2-cyclin B complex B 4.72 pIC50 19000 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 1019-1022 [PMID:9871700]
ChEMBL Inhibition of CDK1/cyclinB B 5.64 pIC50 2300 nM IC50 Trends Pharmacol. Sci. (2004) 25: 471-480 [PMID:15559249]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020P24864P24941]
ChEMBL Inhibitory activity against Cyclin E-cyclin-dependent kinase 2 by measuring phosphorylation of RbING substrate B 4.99 pIC50 10180 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 3841-3846 [PMID:14552792]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802P24385]
ChEMBL Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring phosphorylation of RbING substrate B 6 pIC50 990 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 3841-3846 [PMID:14552792]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of GSK3beta (unknown origin) expressed in Sf9 cells using GS1 as substrate and [gamma32]ATP after 30 min by scinitllation counting B 6.72 pIC50 190.55 nM IC50 Med Chem Res (2007) 16: 461-467
ChEMBL Inhibition of GSK3-beta B 6.72 pIC50 190 nM IC50 Trends Pharmacol. Sci. (2004) 25: 471-480 [PMID:15559249]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3669] [GtoPdb: 2030] [UniProtKB: P18266]
ChEMBL Inhibition of Wistar rat GSK-3beta using RRAAEELDSRAGS(P)PQL as substrate after 15 mins in presence of [gamma-32P]-ATP by scintillation counting method B 6.44 pIC50 360 nM IC50 Bioorg Med Chem (2018) 26: 4209-4224 [PMID:30026041]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 6 pIC50 1000 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6]
ChEMBL Inhibition of human SIRT1 B 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2006) 49: 7307-7316 [PMID:17149860]
ChEMBL Inhibition of human SIRT1 by fluorescent deacetylase assay B 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2006) 49: 7307-7316 [PMID:17149860]
ChEMBL Inhibition of human SIRT1 by radioactive deacetylase assay B 4.64 pIC50 23000 nM IC50 J. Med. Chem. (2006) 49: 7307-7316 [PMID:17149860]
sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
ChEMBL Inhibition of human recombinant SIRT2 by radioactive deacetylase assay B 4.93 pIC50 11700 nM IC50 J. Med. Chem. (2006) 49: 7307-7316 [PMID:17149860]
ChEMBL Inhibition of human recombinant SIRT2 B 5.14 pIC50 7300 nM IC50 J. Med. Chem. (2006) 49: 7307-7316 [PMID:17149860]
ChEMBL Inhibition of human recombinant SIRT2 by fluorescent deacetylase assay B 5.14 pIC50 7300 nM IC50 J. Med. Chem. (2006) 49: 7307-7316 [PMID:17149860]
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Inhibition of Protein kinase C alpha B 8 pIC50 10 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 497-500
ChEMBL Inhibition of PKCalpha by SPA B 8.64 pIC50 2.3 nM IC50 J. Med. Chem. (2009) 52: 6193-6196 [PMID:19827831]
protein kinase C alpha in Bovine [GtoPdb: 1482]
GtoPdb - - 7.7 pIC50 20 nM IC50 J. Biol. Chem. (1991) 266: 15771-81 [PMID:1874734]
protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Inhibition of PKCbeta1 by SPA B 8.8 pIC50 1.6 nM IC50 J. Med. Chem. (2009) 52: 6193-6196 [PMID:19827831]
protein kinase C beta in Bovine [GtoPdb: 1483]
GtoPdb - - 7.8 pIC50 16 nM IC50 J. Biol. Chem. (1991) 266: 15771-81 [PMID:1874734]
protein kinase C delta/Protein kinase C delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
ChEMBL Inhibition of human PKCdelta B 7.49 pIC50 32 nM IC50 J. Biol. Chem. (2007) 282: 33052-33063 [PMID:17875639]
ChEMBL Inhibition of PKCdelta by SPA B 8.06 pIC50 8.7 nM IC50 J. Med. Chem. (2009) 52: 6193-6196 [PMID:19827831]
protein kinase C epsilon/Protein kinase C epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
ChEMBL Inhibition of human PKCepsilon type M486A mutant B 7.92 pIC50 12 nM IC50 J. Biol. Chem. (2007) 282: 33052-33063 [PMID:17875639]
ChEMBL Inhibition of PKCepsilon by SPA B 8.18 pIC50 6.6 nM IC50 J. Med. Chem. (2009) 52: 6193-6196 [PMID:19827831]
ChEMBL Inhibition of human PKCepsilon B 8.22 pIC50 6 nM IC50 J. Biol. Chem. (2007) 282: 33052-33063 [PMID:17875639]
protein kinase C eta/Protein kinase C eta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3616] [GtoPdb: 1487] [UniProtKB: P24723]
ChEMBL Inhibition of PKCeta by SPA B 8 pIC50 10 nM IC50 J. Med. Chem. (2009) 52: 6193-6196 [PMID:19827831]
protein kinase C gamma/Protein kinase C gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129]
ChEMBL Inhibition of human PKCgamma B 7.52 pIC50 30 nM IC50 J. Biol. Chem. (2007) 282: 33052-33063 [PMID:17875639]
protein kinase C gamma in Bovine [GtoPdb: 1484]
GtoPdb - - 7.7 pIC50 20 nM IC50 J. Biol. Chem. (1991) 266: 15771-81 [PMID:1874734]
protein kinase C iota/Protein kinase C iota in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743]
ChEMBL Inhibition of human PKCiota B 5.46 pIC50 3463 nM IC50 J. Biol. Chem. (2007) 282: 33052-33063 [PMID:17875639]
protein kinase C theta/Protein kinase C theta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
ChEMBL Inhibition of PKCtheta by SPA B 8.17 pIC50 6.7 nM IC50 J. Med. Chem. (2009) 52: 6193-6196 [PMID:19827831]
protein kinase C zeta/Protein kinase C zeta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513]
ChEMBL Inhibition of PKCzeta B 5.24 pIC50 5800 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
Protein kinase Pfmrk in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4090] [UniProtKB: P90584]
ChEMBL Inhibition of Plasmodium falciparum cyclin-dependent kinase B 4.62 pIC50 24000 nM IC50 J. Med. Chem. (2004) 47: 5418-5426 [PMID:15481979]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL Binding affinity to non phosphorylated PIM1 B 8 pKd 10 nM Kd J. Med. Chem. (2005) 48: 7604-7614 [PMID:16302800]
ChEMBL Inhibitory activity against PIM1 B 7.57 pIC50 27 nM IC50 J. Med. Chem. (2005) 48: 7604-7614 [PMID:16302800]
ChEMBL Inhibition of human recombinant Pim1 by ATP depletion assay B 7.57 pIC50 27 nM IC50 J. Med. Chem. (2009) 52: 74-86 [PMID:19072652]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]