vactosertib [Ligand Id: 8107] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3260567 (Ew-7197, Tew 7197, Tew-7197, TEW-7197, Vactosertib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| activin A receptor type 1/Activin receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771] | ||||||||
| ChEMBL | Inhibition of ALK2 (unknown origin) by radioisotopic assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2014) 57: 4213-4238 [PMID:24786585] |
| 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 | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2014) 57: 4213-4238 [PMID:24786585] |
| GtoPdb | Measured using Reaction Biology Corporation's HotSpot kinase assay | - | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2014) 57: 4213-38 [PMID:24786585] |
| bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894] | ||||||||
| ChEMBL | Inhibition of ALK3 (unknown origin) by radioisotopic assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2014) 57: 4213-4238 [PMID:24786585] |
| bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238] | ||||||||
| ChEMBL | Inhibition of ALK6 (unknown origin) by radioisotopic assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2014) 57: 4213-4238 [PMID:24786585] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG channel expressed in HEK293 cells after 3 to 5.7 mins by whole-cell patch clamp technique | B | 4.51 | pIC50 | 31040 | 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 untagged p38alpha expressed in Escherichia coli using ATF2 as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method | B | 5.53 | pIC50 | 2950 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 2070-2075 [PMID:31303386] |
| ChEMBL | Inhibition of recombinant human p38alpha expressed in Escherichia coli assessed as incoporation of [33]Pi after 60 mins in presence of [gamma-33P]-ATP by microplate scintillation counter method | B | 5.53 | pIC50 | 2950 | nM | IC50 | Eur J Med Chem (2021) 216: 113311-113311 [PMID:33677350] |
| ChEMBL | Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by proprietary radioisotopic protein kinase assay | B | 5.66 | pIC50 | 2180 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5228-5231 [PMID:26483198] |
| ChEMBL | Inhibition of human recombinant untagged p38alpha expressed in Escherichia coli using ATF2 as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay | B | 5.66 | pIC50 | 2180 | nM | IC50 | Eur J Med Chem (2019) 180: 15-27 [PMID:31299584] |
| ChEMBL | Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by radioisotopic assay | B | 5.76 | pIC50 | 1720 | nM | IC50 | J Med Chem (2014) 57: 4213-4238 [PMID:24786585] |
| activin A receptor type IL/Serine/threonine-protein kinase receptor R3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5311] [GtoPdb: 1784] [UniProtKB: P37023] | ||||||||
| ChEMBL | Inhibition of ALK1 (unknown origin) by radioisotopic assay | B | 5 | pIC50 | >10000 | 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 | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (2014) 57: 4213-4238 [PMID:24786585] |
| transforming growth factor beta receptor 1 in Human [GtoPdb: 1788] [UniProtKB: P36897] | ||||||||
| GtoPdb | Measured using Reaction Biology Corporation's HotSpot kinase assay. | - | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2014) 57: 4213-38 [PMID:24786585] |
| 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 | 7.92 | pIC50 | 12.1 | 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 | Competitive inhibition of ALK5 (unknown origin) by Michaelis-Menten plot analysis in presence of ATP | B | 7.69 | pKi | 20.59 | nM | Ki | J Med Chem (2014) 57: 4213-4238 [PMID:24786585] |
| ChEMBL | Competitive inhibition of ALK5 (unknown origin) assessed as enzyme/ATP complex by Michaelis-Menten plot analysis in presence of ATP | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (2014) 57: 4213-4238 [PMID:24786585] |
| 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 | 7.78 | pIC50 | 16.5 | nM | IC50 | J Med Chem (2014) 57: 4213-4238 [PMID:24786585] |
| ChEMBL | Inhibition of recombinant human GST-fused ALK5 expressed in baculovirus infected Sf9 cells assessed as incoporation of [33]Pi after 60 mins in presence of [gamma-33P]-ATP by microplate scintillation counter method | B | 7.85 | pIC50 | 14 | nM | IC50 | Eur J Med Chem (2021) 216: 113311-113311 [PMID:33677350] |
| ChEMBL | Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 2070-2075 [PMID:31303386] |
| ChEMBL | Inhibition of TGFBR1 (unknown origin) | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2019) 163: 413-427 [PMID:30530193] |
| GtoPdb | Measured using Reaction Biology Corporation's HotSpot kinase assay. | - | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2014) 57: 4213-38 [PMID:24786585] |
| ChEMBL | Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2019) 180: 15-27 [PMID:31299584] |
| ChEMBL | Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay | B | 8.01 | pIC50 | 9.67 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5228-5231 [PMID:26483198] |
| ChEMBL | Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2014) 57: 4213-4238 [PMID:24786585] |
| 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 | 7.01 | pIC50 | 97 | 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]
