compound 1 [PMID: 20005102] [Ligand Id: 8181] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL593490
  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
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  • Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
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  • ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
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  • AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
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  • p21 (RAC1) activated kinase 1/Serine/threonine-protein kinase PAK 1 in Human [ChEMBL: CHEMBL4600] [GtoPdb: 2133] [UniProtKB: Q13153]
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  • 3-phosphoinositide dependent protein kinase 1 in Human [GtoPdb: 1519] [UniProtKB: O15530]
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  • protein kinase A in Human [GtoPdb: 1694]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 GSK3-beta phosphorylation in human BT474 cells B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 679-683 [PMID:20005102]
pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
ChEMBL Inhibition of PDK1 B 7.3 pIC50 50 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 679-683 [PMID:20005102]
Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
ChEMBL Inhibition of ROCK1 B 5.8 pIC50 1580 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 673-678 [PMID:20006497]
ChEMBL Inhibition of ROCK1 B 5.8 pIC50 1580 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 679-683 [PMID:20005102]
ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
GtoPdb - - 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102]
ChEMBL Inhibition of P70S6K B 8.15 pIC50 7 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 679-683 [PMID:20005102]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of AKT1 in human BT474 cells assessed as phosphorylation of GSK3 B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 673-678 [PMID:20006497]
GtoPdb - - 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102]
ChEMBL Inhibition of full length AKT1 B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 673-678 [PMID:20006497]
ChEMBL Inhibition of AKT1 B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 679-683 [PMID:20005102]
AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
GtoPdb - - 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102]
ChEMBL Inhibition of AKT2 B 7.92 pIC50 12 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 679-683 [PMID:20005102]
AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
GtoPdb - - 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102]
ChEMBL Inhibition of AKT3 B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 679-683 [PMID:20005102]
p21 (RAC1) activated kinase 1/Serine/threonine-protein kinase PAK 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4600] [GtoPdb: 2133] [UniProtKB: Q13153]
GtoPdb - - 7.3 pIC50 31 nM IC50 Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102]
ChEMBL Inhibition of PAK1 B 7.51 pIC50 31 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 679-683 [PMID:20005102]
3-phosphoinositide dependent protein kinase 1 in Human [GtoPdb: 1519] [UniProtKB: O15530]
GtoPdb - - 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102]
protein kinase A in Human [GtoPdb: 1694]
GtoPdb - - 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102]

ChEMBL data shown on this page come from version 28:

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]