K02288 [Ligand Id: 13266] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1230714
  • activin A receptor type 1/Activin receptor type-1 in Human [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771]
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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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  • bone morphogenetic protein receptor type IA in Human [GtoPdb: 1786] [UniProtKB: P36894]
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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 human recombinant human ALK2 kinase after 45 mins by liquid scintillation counting in presence of ATP [gamma-32P] B 7.46 pIC50 35 nM IC50 J Med Chem (2014) 57: 7900-7915 [PMID:25101911]
GtoPdb - - 8.96 pIC50 1.1 nM IC50 Bioorg Med Chem Lett (2022) 55: 128452 [PMID:34780900]
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
ChEMBL Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay B 5.47 pIC50 3400 nM IC50 J Med Chem (2014) 57: 7900-7915 [PMID:25101911]
ChEMBL Inhibition of purified human ALK5 kinase after 45 mins by liquid scintillation counting in presence of ATP [gamma-32P] B 6.55 pIC50 280 nM IC50 J Med Chem (2014) 57: 7900-7915 [PMID:25101911]
bone morphogenetic protein receptor type IA in Human [GtoPdb: 1786] [UniProtKB: P36894]
GtoPdb - - 7.46 pIC50 34.3 nM IC50 Bioorg Med Chem Lett (2022) 55: 128452 [PMID:34780900]

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]