belizatinib [Ligand Id: 10474] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2172308
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
  • This target only has 0 pki data point
  • 0
1 CHEMBL2172308_lig_chart_1 ALK tyrosine kinase receptor Human
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  • Insulin receptor in Human [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
  • This target only has 0 pki data point
  • 0
2 CHEMBL2172308_lig_chart_2 Insulin receptor Human
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  • interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617]
  • This target only has 0 pki data point
  • 0
3 CHEMBL2172308_lig_chart_3 Interleukin-1 receptor-associated kinase 1 Human
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  • leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376]
  • This target only has 0 pki data point
  • 0
4 CHEMBL2172308_lig_chart_4 Leukocyte tyrosine kinase receptor Human
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  • mitogen-activated protein kinase kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase kinase 2 in Human [ChEMBL: CHEMBL5330] [GtoPdb: 2086] [UniProtKB: Q12851]
  • This target only has 0 pki data point
  • 0
5 CHEMBL2172308_lig_chart_5 Mitogen-activated protein kinase kinase kinase kinase 2 Human
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  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
  • This target only has 0 pki data point
  • 0
6 CHEMBL2172308_lig_chart_6 Nerve growth factor receptor Trk-A Human
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  • neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
  • This target only has 0 pki data point
  • 0
7 CHEMBL2172308_lig_chart_7 Neurotrophic tyrosine kinase receptor type 2 Human
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  • neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288]
  • This target only has 0 pki data point
  • 0
8 CHEMBL2172308_lig_chart_8 NT-3 growth factor receptor Human
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  • MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
  • This target only has 0 pki data point
  • 0
9 CHEMBL2172308_lig_chart_9 Proto-oncogene tyrosine-protein kinase MER Human
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
  • This target only has 0 pki data point
  • 0
10 CHEMBL2172308_lig_chart_10 Tyrosine-protein kinase LCK Human
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
  • This target only has 0 pki data point
  • 0
11 CHEMBL2172308_lig_chart_11 Tyrosine-protein kinase receptor FLT3 Human
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  • AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
  • This target only has 0 pki data point
  • 0
12 CHEMBL2172308_lig_chart_12 Tyrosine-protein kinase receptor UFO Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
GtoPdb Binding affinity in vitro. - 9.44 pKd 0.36 nM Kd J Med Chem (2012) 55: 6523-40 [PMID:22734674]
ChEMBL Binding affinity to human ALK by Ambit titration assay B 9.44 pKd 0.36 nM Kd J. Med. Chem. (2012) 55: 6523-6540 [PMID:22734674]
ChEMBL Inhibition of ALK Tyr1604 phosphorylation by cell based assay B 8.4 pIC50 4 nM IC50 J. Med. Chem. (2012) 55: 6523-6540 [PMID:22734674]
ChEMBL Inhibition of ALK (unknown origin) B 8.92 pIC50 1.2 nM IC50 J Med Chem (2019) 62: 10927-10954 [PMID:31419130]
ChEMBL Inhibition of ALK enzyme B 9 pIC50 1 nM IC50 J. Med. Chem. (2012) 55: 6523-6540 [PMID:22734674]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of INSR expressed in CHO cells assessed as inhibition of receptor phosphorylation pre-incubated before insulin stimulation by Meso-Scale Discovery pY-IR assay B 6.64 pIC50 231 nM IC50 J. Med. Chem. (2012) 55: 6523-6540 [PMID:22734674]
interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617]
GtoPdb Binding affinity in vitro. - 8.24 pKd 5.7 nM Kd J Med Chem (2012) 55: 6523-40 [PMID:22734674]
ChEMBL Binding affinity to human IRAK1 by Ambit titration assay B 8.24 pKd 5.7 nM Kd J. Med. Chem. (2012) 55: 6523-6540 [PMID:22734674]
leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376]
GtoPdb Binding affinity in vitro. - 8.6 pKd 2.5 nM Kd J Med Chem (2012) 55: 6523-40 [PMID:22734674]
ChEMBL Binding affinity to human LTK by Ambit titration assay B 8.6 pKd 2.5 nM Kd J. Med. Chem. (2012) 55: 6523-6540 [PMID:22734674]
mitogen-activated protein kinase kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5330] [GtoPdb: 2086] [UniProtKB: Q12851]
ChEMBL Binding affinity to human MAP4K2 by Ambit titration assay B 7.96 pKd 11 nM Kd J. Med. Chem. (2012) 55: 6523-6540 [PMID:22734674]
GtoPdb Binding affinity in vitro. - 7.96 pKd 11 nM Kd J Med Chem (2012) 55: 6523-40 [PMID:22734674]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL Inhibition of TRKA (unknown origin) B 8.52 pIC50 <3 nM IC50 J Med Chem (2019) 62: 1731-1760 [PMID:30188734]
neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
ChEMBL Inhibition of TRKB (unknown origin) B 8.52 pIC50 <3 nM IC50 J Med Chem (2019) 62: 1731-1760 [PMID:30188734]
neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288]
ChEMBL Inhibition of TRKC (unknown origin) B 8.52 pIC50 <3 nM IC50 J Med Chem (2019) 62: 1731-1760 [PMID:30188734]
MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
GtoPdb Binding affinity in vitro. - 7.74 pKd 18 nM Kd J Med Chem (2012) 55: 6523-40 [PMID:22734674]
ChEMBL Binding affinity to human MER by Ambit titration assay B 7.74 pKd 18 nM Kd J. Med. Chem. (2012) 55: 6523-6540 [PMID:22734674]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
GtoPdb Binding affinity in vitro. - 7.55 pKd 28 nM Kd J Med Chem (2012) 55: 6523-40 [PMID:22734674]
ChEMBL Binding affinity to human LCK by Ambit titration assay B 7.55 pKd 28 nM Kd J. Med. Chem. (2012) 55: 6523-6540 [PMID:22734674]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Binding affinity to human FLT3 by Ambit titration assay B 7.38 pKd 42 nM Kd J. Med. Chem. (2012) 55: 6523-6540 [PMID:22734674]
GtoPdb Binding affinity in vitro. - 7.38 pKd 42 nM Kd J Med Chem (2012) 55: 6523-40 [PMID:22734674]
AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
ChEMBL Binding affinity to human AXL by Ambit titration assay B 7.54 pKd 29 nM Kd J. Med. Chem. (2012) 55: 6523-6540 [PMID:22734674]
GtoPdb Binding affinity in vitro. - 7.54 pKd 29 nM Kd J Med Chem (2012) 55: 6523-40 [PMID:22734674]

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]