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 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]
