LDN-214117 [Ligand Id: 8481] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3341789 |
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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 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]
