galunisertib [Ligand Id: 7797] 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: CHEMBL2364611 (Galunisertib, LY-2157299)
  • activin A receptor type 1B/Activin receptor type-1B in Human [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896]
  • This target only has 0 pki data point
1 CHEMBL2364611_lig_chart_1 Activin receptor type-1B Human
There should be some charts here, you may need to enable JavaScript!
  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
  • This target only has 0 pki data point
2 CHEMBL2364611_lig_chart_2 MAP kinase p38 alpha Human
There should be some charts here, you may need to enable JavaScript!
  • receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
  • This target only has 0 pki data point
3 CHEMBL2364611_lig_chart_3 Serine/threonine-protein kinase RIPK2 Human
There should be some charts here, you may need to enable JavaScript!
  • transforming growth factor beta receptor 1 in Human [GtoPdb: 1788] [UniProtKB: P36897]
  • transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Mouse [ChEMBL: CHEMBL2021750] [GtoPdb: 1788] [UniProtKB: Q64729]
  • This target only has 0 pki data point
4 CHEMBL2364611_lig_chart_4 transforming growth factor beta receptor 1 HumanMouse
There should be some charts here, you may need to enable JavaScript!
  • transforming growth factor beta receptor 1/TGF-beta receptor type I in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
  • This target only has 0 pki data point
5 CHEMBL2364611_lig_chart_5 TGF-beta receptor type I Human
There should be some charts here, you may need to enable JavaScript!
  • transforming growth factor beta receptor 2/TGF-beta receptor type II in Human [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173]
  • This target only has 0 pki data point
6 CHEMBL2364611_lig_chart_6 TGF-beta receptor type II Human
There should be some charts here, you may need to enable JavaScript!
  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
  • This target only has 0 pki data point
7 CHEMBL2364611_lig_chart_7 Vascular endothelial growth factor receptor 2 Human
There should be some charts here, you may need to enable JavaScript!
  • bone morphogenetic protein receptor type IB in Human [GtoPdb: 1789] [UniProtKB: O00238]
  • This target only has 0 pki data point
8 CHEMBL2364611_lig_chart_8 bone morphogenetic protein receptor type IB Human
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
activin A receptor type 1B/Activin receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896]
ChEMBL Inhibition of ALK4 (unknown origin) by radioisotopic assay B 6.7 pIC50 199 nM IC50 J. Med. Chem. (2014) 57: 4213-4238 [PMID:24786585]
GtoPdb Value determined usinfg the DiscoverX KINOMEscan platform. - 7.11 pIC50 78 nM IC50 Oncotarget (2018) 9: 6659-6677 [PMID:29467918]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by proprietary radioisotopic protein kinase assay B 6.39 pIC50 405 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 5228-5231 [PMID:26483198]
receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
ChEMBL Inhibition of RIPK2 (unknown origin) by radioisotopic assay B 7.36 pIC50 44 nM IC50 J. Med. Chem. (2014) 57: 4213-4238 [PMID:24786585]
transforming growth factor beta receptor 1 in Human [GtoPdb: 1788] [UniProtKB: P36897]
GtoPdb Result from a DiscoverX KINOMEscan platform kinase activity assay. - 6.76 pIC50 172 nM IC50 Oncotarget (2018) 9: 6659-6677 [PMID:29467918]
GtoPdb Inhibition of a 6×-HIS tagged cytoplasmic kinase domain representing TGFβR1 - 7.25 pIC50 56 nM IC50
transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2021750] [GtoPdb: 1788] [UniProtKB: Q64729]
ChEMBL Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay B 7 pIC50 >100 nM IC50 J. Med. Chem. (2014) 57: 4213-4238 [PMID:24786585]
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
GtoPdb Result from a DiscoverX KINOMEscan platform kinase activity assay. - 6.76 pIC50 172 nM IC50 Oncotarget (2018) 9: 6659-6677 [PMID:29467918]
ChEMBL Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay B 7 pIC50 >100 nM IC50 J. Med. Chem. (2014) 57: 4213-4238 [PMID:24786585]
ChEMBL Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay B 7.16 pIC50 69.4 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 5228-5231 [PMID:26483198]
GtoPdb Inhibition of a 6×-HIS tagged cytoplasmic kinase domain representing TGFβR1 - 7.25 pIC50 56 nM IC50
ChEMBL Inhibition of human ALK5 expressed in Sf9 insect cells using casein as substrate in presence of [gamma-33P]ATP B 7.29 pIC50 51 nM IC50 Eur J Med Chem (2017) 127: 632-642 [PMID:28135685]
ChEMBL Inhibition of human His-tagged TGFbetaR1 T204D mutant expressed in Sf9 insect cells after 1 hr by HTRF assay B 8.39 pIC50 4.1 nM IC50 Bioorg Med Chem (2018) 26: 1026-1034 [PMID:29422332]
transforming growth factor beta receptor 2/TGF-beta receptor type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173]
ChEMBL Inhibition of wild type His-tagged TGFbetaR2 (unknown origin) after 1 hr by HTRF assay B 5.89 pIC50 1300 nM IC50 Bioorg Med Chem (2018) 26: 1026-1034 [PMID:29422332]
GtoPdb Value determined usinfg the DiscoverX KINOMEscan platform. - 6.68 pIC50 208 nM IC50 Oncotarget (2018) 9: 6659-6677 [PMID:29467918]
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) by radioisotopic assay B 6.35 pIC50 442 nM IC50 J. Med. Chem. (2014) 57: 4213-4238 [PMID:24786585]
bone morphogenetic protein receptor type IB in Human [GtoPdb: 1789] [UniProtKB: O00238]
GtoPdb Value determined usinfg the DiscoverX KINOMEscan platform. - 6.33 pIC50 471 nM IC50 Oncotarget (2018) 9: 6659-6677 [PMID:29467918]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]