LDN-214117 [Ligand Id: 8481] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3341789
  • activin A receptor type 1/Activin receptor type-1 in Human [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771]
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  • bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894]
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  • activin A receptor type IL/Serine/threonine-protein kinase receptor R3 in Human [ChEMBL: CHEMBL5311] [GtoPdb: 1784] [UniProtKB: P37023]
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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/TGF-beta receptor type I in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
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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 ALK2 using casein as substrate in presence of 10 uM [gamma33P] ATP by radioactive assay B 6.94 pIC50 115 nM IC50 J Med Chem (2020) 63: 4978-4996 [PMID:32369358]
ChEMBL Inhibition of ALK2 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay B 7.57 pIC50 27 nM IC50 J Med Chem (2014) 57: 7900-7915 [PMID:25101911]
ChEMBL Inhibition of human recombinant human ALK2 kinase after 45 mins by liquid scintillation counting in presence of ATP [gamma-32P] B 7.62 pIC50 24 nM IC50 J Med Chem (2014) 57: 7900-7915 [PMID:25101911]
ChEMBL Inhibition of human N-terminal His-tagged TEV protease site linked ALK2 Q207D mutant (201 to 499 residues) expressed in baculovirus infected Sf9 insect cells B 7.62 pIC50 24 nM IC50 J Med Chem (2020) 63: 4978-4996 [PMID:32369358]
ChEMBL Inhibition of human ALK2 using casein as substrate in presence of 10 uM [gamma33P] ATP by kinase assay B 7.62 pIC50 24 nM IC50 Eur J Med Chem (2020) 200: 112417-112417 [PMID:32505849]
GtoPdb - - 7.62 pIC50 24 nM IC50 J Med Chem (2014) 57: 7900-15 [PMID:25101911]
bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894]
GtoPdb - - 5.93 pIC50 1171 nM IC50 J Med Chem (2014) 57: 7900-15 [PMID:25101911]
ChEMBL Inhibition of ALK3 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay B 5.93 pIC50 1171 nM IC50 J Med Chem (2014) 57: 7900-7915 [PMID:25101911]
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) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay B 7.57 pIC50 27 nM IC50 J Med Chem (2014) 57: 7900-7915 [PMID:25101911]
GtoPdb - - 7.57 pIC50 27 nM IC50 J Med Chem (2014) 57: 7900-15 [PMID:25101911]
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 recombinant human RIPK2 incubated for 2 hr by ADP-Glo assay B 7 pIC50 100 nM IC50 Eur J Med Chem (2020) 200: 112417-112417 [PMID:32505849]
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 4.8 pIC50 16000 nM IC50 J Med Chem (2014) 57: 7900-7915 [PMID:25101911]
GtoPdb - - 5.52 pIC50 3000 nM IC50 J Med Chem (2014) 57: 7900-15 [PMID:25101911]
ChEMBL Inhibition of purified human ALK5 kinase after 45 mins by liquid scintillation counting in presence of ATP [gamma-32P] B 5.52 pIC50 3000 nM IC50 J Med Chem (2014) 57: 7900-7915 [PMID:25101911]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]