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ChEMBL ligand: CHEMBL226838 (SB-505124) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]