GSK1070916 [Ligand Id: 8358] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1090479 (GSK1070916, Gsk-1070916, GSK 1070916A)
1 CHEMBL1090479_lig_chart_1 Aurora-C/INCENP Human
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2 CHEMBL1090479_lig_chart_2 Aurora kinase A/Targeting protein for Xklp2 Human
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3 CHEMBL1090479_lig_chart_3 Aurora kinase B/Inner centromere protein Human
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
  • This target only has 0 pki data point
  • 0
4 CHEMBL1090479_lig_chart_4 Fibroblast growth factor receptor 1 Human
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
  • 6.31
5 CHEMBL1090479_lig_chart_5 Serine/threonine-protein kinase Aurora-A Human
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  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
  • 9.42
6 CHEMBL1090479_lig_chart_6 Serine/threonine-protein kinase Aurora-B Human
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  • aurora kinase C/Serine/threonine-protein kinase Aurora-C in Human [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9]
  • 8.82
7 CHEMBL1090479_lig_chart_7 Serine/threonine-protein kinase Aurora-C Human
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  • salt inducible kinase 1/Serine/threonine-protein kinase SIK1 in Human [ChEMBL: CHEMBL6082] [GtoPdb: 2197] [UniProtKB: P57059]
  • This target only has 0 pki data point
  • 0
8 CHEMBL1090479_lig_chart_8 Serine/threonine-protein kinase SIK1 Human
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  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
  • This target only has 0 pki data point
  • 0
9 CHEMBL1090479_lig_chart_9 Tyrosine-protein kinase TIE-2 Human
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  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
  • This target only has 0 pki data point
  • 0
10 CHEMBL1090479_lig_chart_10 Vascular endothelial growth factor receptor 1 Human
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  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
  • This target only has 0 pki data point
  • 0
11 CHEMBL1090479_lig_chart_11 Vascular endothelial growth factor receptor 3 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
aurora kinase C/Aurora-C/INCENP in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106141] [GtoPdb: 1938] [UniProtKB: Q9NQS7Q9UQB9]
GtoPdb - - 8.82 pKi 1.5 nM Ki J Med Chem (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Inhibition of human Aurora C/human GST-tagged INCENP pre-incubated for 30 mins before 5-FAM-PKAtide substrate addition and measured after 60 mins B 8.82 pKi 1.5 nM Ki Eur J Med Chem (2017) 140: 1-19 [PMID:28918096]
aurora kinase A/Aurora kinase A/Targeting protein for Xklp2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883304] [GtoPdb: 1936] [UniProtKB: O14965Q9ULW0]
ChEMBL Inhibition of human Aurora A/TPX2 (unknown origin) pre-incubated for 30 mins before Biotin-Ahx-RARRRLSFFFFAKKK-NH2 substrate addition and measured after 120 mins B 6.31 pKi 490 nM Ki Eur J Med Chem (2017) 140: 1-19 [PMID:28918096]
GtoPdb - - 6.31 pKi 490 nM Ki J Med Chem (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Inhibition of human recombinant aurora A/TPX2 complex after 120 mins by IMAP fluorescence polarization assay B 5.96 pIC50 1100 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2552-2555 [PMID:20335034]
aurora kinase B/Aurora kinase B/Inner centromere protein in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430907] [GtoPdb: 1937] [UniProtKB: Q96GD4Q9NQS7]
GtoPdb - - 9.42 pKi 0.38 nM Ki J Med Chem (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Inhibition of human Aurora B/INCENP pre-incubated for 30 mins before 5-FAM-PKAtide substrate addition and measured after 120 mins B 9.42 pKi 0.38 nM Ki Eur J Med Chem (2017) 140: 1-19 [PMID:28918096]
ChEMBL Inhibition of human recombinant aurora B/INCENP complex after 120 mins by IMAP fluorescence polarization assay B 8.49 pIC50 3.2 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2552-2555 [PMID:20335034]
ChEMBL Inhibition of human recombinant aurora B/INCENP complex after 120 mins by IMAP fluorescence polarization assay B 8.5 pIC50 3.16 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2552-2555 [PMID:20335034]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibition of FGFR1 B 7.12 pIC50 76 nM IC50 J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Multi-Cycle Kinetic parameter establishment of 8 compounds to gain n=3Completed over 3 identical immbolized CM5 chips B 7.82 pKd 15.07 nM Kd K4DD drug target binding kinetics data
ChEMBL Single-Cycle Kinetic parameter establishment of 8 compounds to gain n=3 B 7.89 pKd 12.96 nM Kd K4DD drug target binding kinetics data
ChEMBL Single-Cycle Kinetic parameter establishment of 8 compounds to gain n=3 B 7.91 pKd 12.3 nM Kd K4DD drug target binding kinetics data
ChEMBL Single-Cycle Kinetic parameter establishment of 8 compounds to gain n=3 B 7.93 pKd 11.82 nM Kd K4DD drug target binding kinetics data
ChEMBL Multi-Cycle Kinetic parameter establishment of 8 compounds to gain n=3 Completed over 3 identical immbolized CM5 chips B 7.97 pKd 10.65 nM Kd K4DD drug target binding kinetics data
ChEMBL Inhibition of Aurora A B 6.31 pKi 492 nM Ki J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Competitive inhibition of human Aurora A ATP binding site B 6.31 pKi 490 nM Ki J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
GtoPdb - - 6.31 pKi 490 nM Ki J Med Chem (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Inhibition of human Aurora A B 5.9 pIC50 1259 nM IC50 J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
GtoPdb - - 9.42 pKi 0.38 nM Ki J Med Chem (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Competitive inhibition of Aurora B ATP binding site B 9.42 pKi 0.38 nM Ki J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Competitive inhibition of human Aurora B ATP binding site by rapid dilution method B 9.42 pKi 0.38 nM Ki J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Inhibition of aurora B assessed as inhibition of histone H3 phosphorylation by ELISA based cellular mechanistic assay B 7.49 pIC50 32 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2552-2555 [PMID:20335034]
ChEMBL Inhibition of human Aurora B by rapid dilution method B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Inhibition of recombinant aurora B (unknown origin) B 8.46 pIC50 3.5 nM IC50 Eur J Med Chem (2017) 140: 1-19 [PMID:28918096]
aurora kinase C/Serine/threonine-protein kinase Aurora-C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9]
GtoPdb - - 8.82 pKi 1.5 nM Ki J Med Chem (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Competitive inhibition of Aurora C ATP binding site B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Competitive inhibition of human Aurora C ATP binding site B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Competitive inhibition of Aurora C ATP binding site B 8.19 pIC50 6.5 nM IC50 J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
ChEMBL Inhibition of Aurora C kinase (unknown origin) B 8.19 pIC50 6.5 nM IC50 Eur J Med Chem (2017) 140: 1-19 [PMID:28918096]
salt inducible kinase 1/Serine/threonine-protein kinase SIK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6082] [GtoPdb: 2197] [UniProtKB: P57059]
ChEMBL Inhibition of SIK B 7.15 pIC50 70 nM IC50 J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL Inhibition of TIE2 B 7.23 pIC50 59 nM IC50 J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
ChEMBL Inhibition of FLT1 B 7.38 pIC50 42 nM IC50 J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL Inhibition of FLT4 B 7.13 pIC50 74 nM IC50 J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]

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]