migalastat [Ligand Id: 10200] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL110458 (At-1001, gr-181314a, Galafold, Migalastat)
  • Alpha-galactosidase in Coffea arabica [ChEMBL: CHEMBL5217] [UniProtKB: Q42656]
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  • Alpha-galactosidase C in Aspergillus niger [ChEMBL: CHEMBL3936] [UniProtKB: Q9UUZ4]
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  • UDP-glucose ceramide glucosyltransferase/Ceramide glucosyltransferase in Human [ChEMBL: CHEMBL2063] [GtoPdb: 2528] [UniProtKB: Q16739]
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  • alpha glucosidase/Lysosomal alpha-glucosidase in Human [ChEMBL: CHEMBL2608] [GtoPdb: 2611] [UniProtKB: P10253]
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  • maltase-glucoamylase/Maltase-glucoamylase in Human [ChEMBL: CHEMBL2074] [GtoPdb: 2627] [UniProtKB: O43451]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 32:

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]