ponatinib [Ligand Id: 5890] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1171837 (Ponatinib, AP-24534, Iclusig)
  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
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  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
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  • fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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  • receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
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  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • Tyrosine-protein kinase SRC in Chicken [ChEMBL: CHEMBL3655] [UniProtKB: P00523]
  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • cyclin dependent kinase 19 in Human [GtoPdb: 1972] [UniProtKB: Q9BWU1]
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  • cyclin dependent kinase 8 in Human [GtoPdb: 1980] [UniProtKB: P49336]
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  • receptor interacting serine/threonine kinase 1 in Human [GtoPdb: 2189] [UniProtKB: Q13546]
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  • receptor interacting serine/threonine kinase 3 in Human [GtoPdb: 2191] [UniProtKB: Q9Y572]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 recombinant human FGFR1 using substrate KKKSPGEYVNIEFG in presence of [33-P]ATP by kinase hotspot assay B 8.66 pIC50 2.2 nM IC50 Eur J Med Chem (2017) 126: 476-490 [PMID:27914362]
ChEMBL Inhibition of recombinant FGFR1 (unknown origin) using poly (Glu, Tyr) 4:1 after 60 mins by ELISA method B 8.92 pIC50 1.2 nM IC50 Eur J Med Chem (2017) 126: 122-132 [PMID:27750146]
ChEMBL Inhibition of FGFR1 (unknown origin) B 9.15 pIC50 0.7 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 5639-5643 [PMID:25467150]
ChEMBL Inhibition of human FGFR1 B 9.15 pIC50 0.7 nM IC50 Bioorg Med Chem (2018) 26: 5479-5493 [PMID:30293796]
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
ChEMBL Inhibition of recombinant FGFR2 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA B 8.89 pIC50 1.3 nM IC50 Eur J Med Chem (2017) 126: 122-132 [PMID:27750146]
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
ChEMBL Inhibition of recombinant FGFR3 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA B 8.03 pIC50 9.4 nM IC50 Eur J Med Chem (2017) 126: 122-132 [PMID:27750146]
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
ChEMBL Inhibition of recombinant FGFR4 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA B 8.15 pIC50 7.1 nM IC50 Eur J Med Chem (2017) 126: 122-132 [PMID:27750146]
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 Inhibition of recombinant PDGFRalpha (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA B 8.59 pIC50 2.6 nM IC50 Eur J Med Chem (2017) 126: 122-132 [PMID:27750146]
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 Inhibition of recombinant PDGFRbeta (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA B 8.92 pIC50 1.2 nM IC50 Eur J Med Chem (2017) 126: 122-132 [PMID:27750146]
receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
GtoPdb Inhibition of recombinant RIPK2 in an in vitro ADP-Glo assay (Promega). - 7.85 pIC50 14 nM IC50 Cell Rep (2015) 10: 1850-60 [PMID:25801024]
ChEMBL Inhibition of human RIPK2 expressed in Sf9 cells after 1 hr by ADP-Glo assay B 8.17 pIC50 6.7 nM IC50 J Med Chem (2018) 61: 3239-3252 [PMID:28505447]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Inhibition of cKIT V559D/T670I double mutant (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay B 8.31 pIC50 4.9 nM IC50 J. Med. Chem. (2013) 56: 5757-5772 [PMID:23773153]
ChEMBL Inhibition of wild-type cKIT (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay B 8.77 pIC50 1.7 nM IC50 J. Med. Chem. (2013) 56: 5757-5772 [PMID:23773153]
ChEMBL Inhibition of wild type KIT (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay B 8.77 pIC50 1.7 nM IC50 J Med Chem (2017) 60: 8801-8815 [PMID:28991465]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of wild type human ABL using [EAIYAAPFAKKK] peptide substrate after 1 hr by TR-FRET assay B 8.07 pIC50 8.6 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 3743-3748 [PMID:21561767]
ChEMBL Inhibition of wild type human ABL after 1 hr by TR-FRET assay B 8.07 pIC50 8.6 nM IC50 J. Med. Chem. (2010) 53: 4701-4719 [PMID:20513156]
GtoPdb - - 8.1 pIC50 8.6 nM IC50 J. Med. Chem. (2010) 53: 4701-19 [PMID:20513156]
ChEMBL Inhibition of recombinant ABL (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA B 8.11 pIC50 7.7 nM IC50 Eur J Med Chem (2017) 126: 122-132 [PMID:27750146]
ChEMBL Inhibition of human wild-type ABL (Ser229 to Gln513)-mediated phosphorylation of biotinylated poly-Glu-Tyr expressed in Escherichia coli BL21(DE3) preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay B 8.54 pIC50 2.9 nM IC50 J. Med. Chem. (2013) 56: 5757-5772 [PMID:23773153]
ChEMBL Inhibition of ABL T315I mutant autophosphorylation B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2010) 53: 4701-4719 [PMID:20513156]
ChEMBL Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay B 8.84 pIC50 1.43 nM IC50 J. Med. Chem. (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay B 8.86 pIC50 1.39 nM IC50 J. Med. Chem. (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay B 8.97 pIC50 1.08 nM IC50 J. Med. Chem. (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of ABL T315I mutant (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay B 9 pIC50 1 nM IC50 J. Med. Chem. (2013) 56: 5757-5772 [PMID:23773153]
ChEMBL ABL1 (T315I) Kinase Activity Assay: Serially diluting the compound of the present invention from 1 uM initial concentration in three-fold fashion and formulating 10 concentrations (50.8 pM, 152.0 pM, 457.0 pM, 1.37 nM, 4.12 nM, 12.3 nM, 37.0 nM, 111.0 nM, 333.0 nM and 1.0 uM). 5.0 uM Abltide was added into each well and then human T315I mutant enzyme was added. [gamma-33P] ATP was added at room temperature, with final concentration of 1.0 uM, and the reaction was performed for 120 minutes. 20 ul aliquots were transferred onto the ion exchange chromatography paper P81. The paper was thoroughly washed with a 0.75% phosphoric acid solution three times, and then washed with acetone once. Finally, gamma-33P radioactivity was measured. B 9 pIC50 1 nM IC50 US-9255107-B2. Heteroaryl alkyne compound and use thereof (2016)
ChEMBL Inhibition of breakpoint cluster region-Abelson tyrosine kinase T315I mutant (unknown origin) using [gamma-33P]ATP as substrate by radiometric kinase assay B 9.24 pIC50 0.58 nM IC50 J. Med. Chem. (2013) 56: 3531-3545 [PMID:23600806]
ChEMBL Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay B 9.3 pIC50 0.5 nM IC50 J. Med. Chem. (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay B 9.37 pIC50 0.43 nM IC50 J. Med. Chem. (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay B 9.39 pIC50 0.41 nM IC50 J. Med. Chem. (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of ABL autophosphorylation B 9.43 pIC50 0.37 nM IC50 J. Med. Chem. (2010) 53: 4701-4719 [PMID:20513156]
ChEMBL Inhibition of recombinant human ABL using peptide substrate EAIYAAPFAKKK in presence of [33-P]ATP by kinase hotspot assay B 9.43 pIC50 0.37 nM IC50 Eur J Med Chem (2017) 126: 476-490 [PMID:27914362]
ChEMBL Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay B 9.48 pIC50 0.33 nM IC50 J. Med. Chem. (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay B 9.49 pIC50 0.32 nM IC50 J. Med. Chem. (2013) 56: 879-894 [PMID:23301703]
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL Inhibition of recombinant human Lyn using peptide substrate poly[Glu:Tyr] (4:1) in presence of [33-P]ATP by kinase hotspot assay B 9.62 pIC50 0.24 nM IC50 Eur J Med Chem (2017) 126: 476-490 [PMID:27914362]
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 in human MV4-11 cells B 9.52 pIC50 0.3 nM IC50 MedChemComm (2012) 3: 22-27
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of RET (unknown origin) V804 mutant B 7.47 pIC50 33.9 nM IC50 J. Med. Chem. (2015) 58: 3672-3681 [PMID:25625428]
ChEMBL Inhibition of RET (unknown origin) B 7.59 pIC50 25.8 nM IC50 J. Med. Chem. (2015) 58: 3672-3681 [PMID:25625428]
GtoPdb - - 8.2 pIC50 7 nM IC50 Mol. Cell. Endocrinol. (2013) 377: 1-6 [PMID:23811235]
ChEMBL Inhibition of RET (unknown origin) using poly[Glu:Tyr] (4:1) as substrate after 60 mins by ELISA B 9.05 pIC50 0.9 nM IC50 Bioorg Med Chem Lett (2016) 26: 5679-5684 [PMID:27815117]
ChEMBL Inhibition of recombinant RET (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA B 9.52 pIC50 0.3 nM IC50 Eur J Med Chem (2017) 126: 122-132 [PMID:27750146]
Tyrosine-protein kinase SRC in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3655] [UniProtKB: P00523]
ChEMBL Inhibition of chicken wild-type cSRC (251 to 533)-mediated phosphorylation of biotinylated poly-Glu-Tyr expressed in Escherichia coli BL21(DE3) preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay B 9.05 pIC50 0.9 nM IC50 J. Med. Chem. (2013) 56: 5757-5772 [PMID:23773153]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of human Src B 8.52 pIC50 3 nM IC50 J. Med. Chem. (2015) 58: 3957-3974 [PMID:25835317]
ChEMBL Inhibition of recombinant c-Src (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA B 8.6 pIC50 2.5 nM IC50 Eur J Med Chem (2017) 126: 122-132 [PMID:27750146]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of VEGFR2 (unknown origin) using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA B 8.37 pIC50 4.3 nM IC50 ACS Med. Chem. Lett. (2014) 5: 673-678 [PMID:24944742]
ChEMBL Inhibition of KDR (unknown origin) using poly (Glu, Tyr) 4:1 as substrate at after 1 hr by ELISA B 8.68 pIC50 2.1 nM IC50 Eur J Med Chem (2017) 135: 370-381 [PMID:28460311]
ChEMBL Inhibition of KDR (unknown origin) B 8.77 pIC50 1.7 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 5639-5643 [PMID:25467150]
ChEMBL Inhibition of human KDR B 8.77 pIC50 1.7 nM IC50 Bioorg Med Chem (2018) 26: 5479-5493 [PMID:30293796]
ChEMBL Inhibition of recombinant human VEGFR2 using substrate poly[Glu:Tyr] (4:1) in presence of [33-P]ATP by kinase hotspot assay B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2017) 126: 476-490 [PMID:27914362]
cyclin dependent kinase 19 in Human [GtoPdb: 1972] [UniProtKB: Q9BWU1]
GtoPdb CDK19/cyclin C. - 7.92 pKd 11.9 nM Kd Nat. Chem. Biol. (2015) 11: 973-80 [PMID:26502155]
cyclin dependent kinase 8 in Human [GtoPdb: 1980] [UniProtKB: P49336]
GtoPdb CDK8/cyclin C. - 8.17 pKd 6.77 nM Kd Nat. Chem. Biol. (2015) 11: 973-80 [PMID:26502155]
receptor interacting serine/threonine kinase 1 in Human [GtoPdb: 2189] [UniProtKB: Q13546]
GtoPdb Inhibition of recombinant RIPK1 in an in vitro ADP-Glo assay (Promega). - 7.92 pIC50 12 nM IC50 Cell Rep (2015) 10: 1850-60 [PMID:25801024]
receptor interacting serine/threonine kinase 3 in Human [GtoPdb: 2191] [UniProtKB: Q9Y572]
GtoPdb Inhibition of recombinant RIPK3 in an in vitro ADP-Glo assay (Promega). - 8.8 pKi 1.6 nM Ki Cell Rep (2015) 10: 1850-60 [PMID:25801024]

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]