barasertib [Ligand Id: 7332] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL415049 (AZD-1152, Barasertib, Azd-1152, AZD1152, AZD 1152)
  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
There should be some charts here, you may need to enable JavaScript!
  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
There should be some charts here, you may need to enable JavaScript!
  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
There should be some charts here, you may need to enable JavaScript!
  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
There should be some charts here, you may need to enable JavaScript!
  • aurora kinase C/Serine/threonine-protein kinase Aurora-C in Human [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9]
There should be some charts here, you may need to enable JavaScript!
  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
There should be some charts here, you may need to enable JavaScript!
  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
There should be some charts here, you may need to enable JavaScript!
  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
ChEMBL Binding affinity to PDGFRA B 7.42 pKd 38 nM Kd J. Med. Chem. (2009) 52: 2629-2651 [PMID:19320489]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
ChEMBL Binding affinity to PDGFRB B 7.39 pKd 41 nM Kd J. Med. Chem. (2009) 52: 2629-2651 [PMID:19320489]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of aurora A (unknown origin) B 5.86 pKi 1368 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 3523-3530 [PMID:23664099]
ChEMBL Inhibition of Aurora A B 5.85 pIC50 1400 nM IC50 J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
GtoPdb - - 5.86 pIC50 1368 nM IC50 Blood (2007) 110: 2034-40 [PMID:17495131]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of aurora B (unknown origin) B 9.43 pKi 0.37 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 3523-3530 [PMID:23664099]
ChEMBL Competitive inhibition of Aurora B ATP binding site B 9 pIC50 <1 nM IC50 J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
GtoPdb - - 9.43 pIC50 0.37 nM IC50 Blood (2007) 110: 2034-40 [PMID:17495131]
ChEMBL Inhibition of Aurora B (unknown origin) B 9.43 pIC50 0.37 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 3067-3072 [PMID:27209235]
aurora kinase C/Serine/threonine-protein kinase Aurora-C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9]
ChEMBL Competitive inhibition of Aurora C ATP binding site B 7.77 pIC50 17 nM IC50 J. Med. Chem. (2010) 53: 3973-4001 [PMID:20420387]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Binding affinity to Kit B 7.77 pKd 17 nM Kd J. Med. Chem. (2009) 52: 2629-2651 [PMID:19320489]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of Flt3 B 8.1 pKd 8 nM Kd J. Med. Chem. (2009) 52: 2629-2651 [PMID:19320489]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Binding affinity to Ret B 7.1 pKd 80 nM Kd J. Med. Chem. (2009) 52: 2629-2651 [PMID:19320489]

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]