migalastat [Ligand Id: 10200] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL110458 (At-1001, gr-181314a, Galafold, Migalastat) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| Alpha-galactosidase in Coffea arabica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5217] [UniProtKB: Q42656] | ||||||||
| ChEMBL | Inhibition of alpha-galactosidase green coffee beans | B | 7.89 | pKi | 13 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4077-4079 [PMID:20610152] |
| ChEMBL | Inhibition of coffee bean alpha-galactosidase assessed as p-nitrophenol release at pH 6.5 by spectrometric analysis | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2010) 18: 3790-3794 [PMID:20457528] |
| Alpha-galactosidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2524] [UniProtKB: P06280] | ||||||||
| ChEMBL | Inhibitory concentration against human alpha-galactosidase | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2005) 48: 2036-2044 [PMID:15771446] |
| ChEMBL | Inhibition of human lysosome alpha-galactosidase assessed as p-nitrophenol release by spectrometric analysis | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem (2010) 18: 3790-3794 [PMID:20457528] |
| ChEMBL | Inhibition of recombinant human alpha GAL-A using 4-methylumbelliferyl alpha-D-galactopyranoside as substrate at pH 4.6 after 15 mins by fluorescence assay | B | 7.38 | pIC50 | 42 | nM | IC50 | Eur J Med Chem (2017) 126: 1-6 [PMID:27744182] |
| ChEMBL | Inhibition of recombinant human alpha GAL-A using 4-methylumbelliferyl alpha-D-galactopyranoside as substrate at pH 7 after 15 mins by fluorescence assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2017) 126: 1-6 [PMID:27744182] |
| Alpha-galactosidase C in Aspergillus niger (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3936] [UniProtKB: Q9UUZ4] | ||||||||
| ChEMBL | Inhibitory concentration against alpha-galactosidase of Aspergillus niger | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2005) 48: 2036-2044 [PMID:15771446] |
| Beta-galactosidase in Sinorhizobium meliloti (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3484] [UniProtKB: Q59750] | ||||||||
| ChEMBL | Inhibition of Agrobacterium sp. beta-galactosidase | B | 4.9 | pKi | 12500 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2067-2070 [PMID:16481162] |
| Beta-galactosidase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293264] [UniProtKB: Q8VNN2] | ||||||||
| ChEMBL | Inhibition of Escherichia coli beta-galactosidase | B | 4.89 | pKi | 13000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4077-4079 [PMID:20610152] |
| Beta-galactosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2522] [UniProtKB: P16278] | ||||||||
| ChEMBL | Inhibitory concentration against human beta-galactosidase | B | 4.05 | pIC50 | 90000 | nM | IC50 | J Med Chem (2005) 48: 2036-2044 [PMID:15771446] |
| Beta-galactosidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2680] [UniProtKB: D3ZUM4] | ||||||||
| ChEMBL | Inhibitory concentration against beta-galactosidase of rat | B | 4.62 | pIC50 | 24000 | nM | IC50 | J Med Chem (2005) 48: 2036-2044 [PMID:15771446] |
| Beta-glucosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3761] [UniProtKB: Q9HCG7] | ||||||||
| ChEMBL | Inhibition of GBA2 by HPLC | B | 4 | pIC50 | 100000 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| UDP-glucose ceramide glucosyltransferase/Ceramide glucosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2063] [GtoPdb: 2528] [UniProtKB: Q16739] | ||||||||
| ChEMBL | Inhibition of GCS by cell-based assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| Glycogen debranching enzyme in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5272] [UniProtKB: P35573] | ||||||||
| ChEMBL | Inhibition of glycogen glycogen de-branching enzyme by HPLC | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| Lactase-glycosylceramidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3389] [UniProtKB: Q02401] | ||||||||
| ChEMBL | Inhibition of rat intestinal lactase assessed as p-nitrophenol release by spectrometric analysis | B | 4.14 | pIC50 | 72000 | nM | IC50 | Bioorg Med Chem (2010) 18: 3790-3794 [PMID:20457528] |
| Lactase-phlorizin hydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075131] [UniProtKB: P09848] | ||||||||
| ChEMBL | Inhibition of lactase by HPLC | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| alpha glucosidase/Lysosomal alpha-glucosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2608] [GtoPdb: 2611] [UniProtKB: P10253] | ||||||||
| ChEMBL | Inhibition of lysosomal alpha-glucosidase by HPLC | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| GtoPdb | - | - | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Biochem (2000) 267: 4179-86 [PMID:10866822] |
| maltase-glucoamylase/Maltase-glucoamylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2074] [GtoPdb: 2627] [UniProtKB: O43451] | ||||||||
| ChEMBL | Inhibition of maltase by HPLC | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| Sucrase-isomaltase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2748] [UniProtKB: P14410] | ||||||||
| ChEMBL | Inhibition of sucrase by HPLC | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
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]
