TGF-beta RI inhibitor III [Ligand Id: 6049] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL226838 (SB-505124)
  • activin A receptor type 1B/Activin receptor type-1B in Human [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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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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  • 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]
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  • transforming growth factor beta receptor 1/TGF-beta receptor type I in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
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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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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 7.15 pIC50 70 nM IC50 J. Med. Chem. (2014) 57: 4213-4238 [PMID:24786585]
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 6.18 pIC50 668 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 5228-5231 [PMID:26483198]
ChEMBL Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as a substrate by radioisotopic protein kinase assay B 6.23 pIC50 594 nM IC50 Bioorg. Med. Chem. (2011) 19: 2633-2640 [PMID:21435890]
ChEMBL Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as a substrate by radioisotopic protein kinase assay B 6.23 pIC50 594 nM IC50 Eur. J. Med. Chem. (2012) 57: 74-84 [PMID:23047226]
ChEMBL Inhibition of recombinant human p38-alpha expressed in Escherichia coli using ATF2 as substrate by radioisotope-based assay B 6.23 pIC50 590 nM IC50 Bioorg. Med. Chem. (2014) 22: 2724-2732 [PMID:24704197]
ChEMBL Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by radioisotopic assay B 6.23 pIC50 590 nM IC50 J. Med. Chem. (2014) 57: 4213-4238 [PMID:24786585]
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 6.16 pIC50 685 nM IC50 J. Med. Chem. (2014) 57: 4213-4238 [PMID:24786585]
transforming growth factor beta receptor 1 in Human [GtoPdb: 1788] [UniProtKB: P36897]
GtoPdb Assay used purified human TGFβR1 kinase domain produced in Sf9 insect cells. - 7.27 pIC50 54 nM IC50 Eur J Med Chem (2011) 46: 3917-25 [PMID:21696866]
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 7.12 pIC50 76.6 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]
ChEMBL Antagonistic activity at TGFBR1 F 1.33 pIC50 -1.33 - logIC50 Bioorg. Med. Chem. Lett. (2010) 20: 1918-1923 [PMID:20176484]
ChEMBL Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells B 6.77 pIC50 169 nM IC50 Bioorg. Med. Chem. (2010) 18: 4459-4467 [PMID:20472445]
ChEMBL Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay B 7.26 pIC50 54.4 nM IC50 Eur. J. Med. Chem. (2012) 57: 74-84 [PMID:23047226]
ChEMBL Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay B 7.27 pIC50 54 nM IC50 J. Med. Chem. (2014) 57: 4213-4238 [PMID:24786585]
ChEMBL Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells B 7.27 pIC50 54 nM IC50 Bioorg. Med. Chem. (2011) 19: 2633-2640 [PMID:21435890]
ChEMBL Inhibition of GST-fused recombinant human ALK5 expressed in baculovirus-infected insect Sf9 cells using casein as substrate by radioisotope-based assay B 7.27 pIC50 54 nM IC50 Bioorg. Med. Chem. (2014) 22: 2724-2732 [PMID:24704197]
GtoPdb Assay used purified human TGFβR1 kinase domain produced in Sf9 insect cells. - 7.27 pIC50 54 nM IC50 Eur J Med Chem (2011) 46: 3917-25 [PMID:21696866]
ChEMBL Inhibition of GST-tagged ALK5 kinase domain (unknown origin) using GST-tagged SMAD3 as substrate in presence of [33P] gammaATP by liquid scintillation counter method B 7.33 pIC50 47 nM IC50 Bioorg Med Chem Lett (2019) 29: 2070-2075 [PMID:31303386]
ChEMBL Inhibition of ALK5 assessed as inhibition of immobilized Smad3 phosphorylation B 7.33 pIC50 47 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 4868-4872 [PMID:19616940]
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 7.36 pIC50 43.8 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 7.46 pIC50 34.9 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 5228-5231 [PMID:26483198]
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 5 pIC50 >10000 nM IC50 J. Med. Chem. (2014) 57: 4213-4238 [PMID:24786585]

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]