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ChEMBL ligand: CHEMBL206468 (Afegostat, Isofagomine) |
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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 green coffee bean alpha-galactosidase | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2016) 7: 365-370 |
Alpha-glucosidase in Schizosaccharomyces pombe (strain 972 / ATCC 24843) (Fission yeast) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784909] [UniProtKB: Q9C0Y4] | ||||||||
ChEMBL | Inhibition of Saccharomyces cerevisiae alpha glucosidase | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2016) 7: 365-370 |
Beta-galactosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2522] [UniProtKB: P16278] | ||||||||
ChEMBL | Inhibition of beta-galactosidase derived from human peripheral blood mononuclear cell lysate using 4-methylumbelliferyl beta-D-galactopyranoside as substrate after 2 hrs by fluorescence analysis | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2018) 26: 5462-5469 [PMID:30270003] |
Beta-galactosidase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3482] [UniProtKB: Q58D55] | ||||||||
ChEMBL | Inhibition of bovine liver beta-galactosidase assessed as production of p-nitrophenol by spectrophotometry | B | 5.44 | pIC50 | 3600 | nM | IC50 | Bioorg Med Chem (2011) 19: 3558-3568 [PMID:21546253] |
Beta-galactosidase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4603] [UniProtKB: P00722] | ||||||||
ChEMBL | Inhibition of Escherichia coli beta-galactosidase | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2016) 7: 365-370 |
glucosylceramidase beta/Beta-glucocerebrosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2179] [GtoPdb: 2978] [UniProtKB: P04062] | ||||||||
ChEMBL | Competitive inhibition of human recombinant imiglucerase using 4-MU-beta-D-Glu as substrate at pH 5.2 after 30 mins by fluorometry based Lineweaver-Burk plot analysis | B | 6.66 | pKi | 220 | nM | Ki | Medchemcomm (2016) 7: 365-370 |
ChEMBL | Inhibition of human recombinant imiglucerase using 4-MU-beta-D-Glu as substrate at pH 7.0 after 30 mins by fluorometric analysis | B | 5.82 | pIC50 | 1520 | nM | IC50 | Medchemcomm (2016) 7: 365-370 |
ChEMBL | Inhibition of human recombinant imiglucerase using 4-MU-beta-D-Glu as substrate at pH 5.2 after 30 mins by fluorometric analysis | B | 6.13 | pIC50 | 740 | nM | IC50 | Medchemcomm (2016) 7: 365-370 |
ChEMBL | Inhibition of GCase in patient derived fibroblast cells using 5'pentafluorobenzoylaminofluorescein-di-beta-D-glucoside as substrate assessed as substrate hydrolysis by FACS analysis | B | 6.39 | pIC50 | 410 | nM | IC50 | Bioorg Med Chem Lett (2023) 81: 129130-129130 [PMID:36640928] |
ChEMBL | Inhibition of recombinant GCase (unknown origin) using 4-methylumbelliferyl-beta-D-glucopyranoside as substrate at pH 4.5 | B | 6.64 | pIC50 | 230 | nM | IC50 | Bioorg Med Chem Lett (2023) 81: 129130-129130 [PMID:36640928] |
ChEMBL | Inhibition of glucocerebrosidase N370S mutant in spleen homogenates of patient with Gaucher disease using resorufin-beta-D-glucopyranoside as substrate after 20 mins fluorescence assay | B | 7.1 | pIC50 | 80 | nM | IC50 | Medchemcomm (2012) 3: 56-60 [PMID:22606365] |
ChEMBL | Inhibition of human lysosome beta-glucosidase assessed as production of 4-methylumbelliferone using 4-methylumbelliferyl beta-D-glucoside as substrate by spectrophotometry | B | 7.2 | pIC50 | 63 | nM | IC50 | Bioorg Med Chem (2011) 19: 3558-3568 [PMID:21546253] |
ChEMBL | Inhibition of human lysosomal beta-glucosidase | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2008) 16: 7330-7336 [PMID:18595718] |
ChEMBL | Inhibition of GCase assessed as 4-methylumbelliferone release assay after 30 mins by fluorimetry | B | 7.23 | pIC50 | 59 | nM | IC50 | Nat Chem Biol (2007) 3: 101-107 [PMID:17187079] |
ChEMBL | Inhibition of human GCase assessed as reduction of 4-methylumbelliferone liberation using 4-methylumbelliferyl-beta-glucopyranoside as substrate preincubated with enzyme for 10 mins followed by substrate addition by fluorescence spectrophotometry | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2022) 238: 114499-114499 [PMID:35675756] |
ChEMBL | Chaperone activity at GCase N370S GBA mutant in patient derived fibroblast cell assessed as GCase level incubated for 5 days by immunocytochemistry assay | B | 6.41 | pEC50 | 390 | nM | EC50 | Bioorg Med Chem Lett (2023) 81: 129130-129130 [PMID:36640928] |
ChEMBL | Chaperone activity at GCase N370S GBA mutant in patient derived fibroblast cell using 4-methylumbelliferyl-beta-D-glucopyranoside as substrate assessed as substrate cleavage by measuring concentration required for maximal response incubated for 5 days by fluorescence based assay | B | 6.52 | pEC50 | 300 | nM | EC50 | Bioorg Med Chem Lett (2023) 81: 129130-129130 [PMID:36640928] |
Beta-glucosidase in Agrobacterium tumefaciens (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4663] [UniProtKB: P27034] | ||||||||
ChEMBL | Inhibition of Agrobacterium sp. beta-glucosidase | B | 8.15 | pKi | 7 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2067-2070 [PMID:16481162] |
Beta-glucosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3761] [UniProtKB: Q9HCG7] | ||||||||
ChEMBL | Inhibition of beta-glucosidase derived from human peripheral blood mononuclear cell lysate using 4-methylumbelliferyl beta-D-glucopyranoside as substrate after 2 hrs by fluorescence analysis | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2018) 26: 5462-5469 [PMID:30270003] |
Glucosylceramidase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1275219] [UniProtKB: Q2KHZ8] | ||||||||
ChEMBL | Inhibition of bovine liver beta-glucosidase assessed as production of 4-methylumbelliferone using 4-methylumbelliferyl beta-D-glucoside as substrate by spectrophotometry | B | 4.51 | pIC50 | 31000 | nM | IC50 | Bioorg Med Chem (2011) 19: 3558-3568 [PMID:21546253] |
Glycogen phosphorylase, muscle form in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4696] [UniProtKB: P00489] | ||||||||
ChEMBL | Inhibition of non-phosphorylated form of rabbit muscle glycogen phosphorylase in presence of phosphate | B | 5.28 | pKi | 5200 | nM | Ki | J Med Chem (2006) 49: 5687-5701 [PMID:16970395] |
ChEMBL | Inhibition of non-phosphorylated form of rabbit muscle glycogen phosphorylase | B | 5.92 | pIC50 | 1210 | nM | IC50 | J Med Chem (2006) 49: 5687-5701 [PMID:16970395] |
ChEMBL | Inhibition of phosphorylated form of rabbit muscle glycogen phosphorylase | B | 6.12 | pIC50 | 760 | nM | IC50 | J Med Chem (2006) 49: 5687-5701 [PMID:16970395] |
Lactase-glycosylceramidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3389] [UniProtKB: Q02401] | ||||||||
ChEMBL | Inhibition of rat intestinal lactase assessed as production of p-nitrophenol by spectrophotometry | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem (2011) 19: 3558-3568 [PMID:21546253] |
Liver glycogen phosphorylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2568] [UniProtKB: P06737] | ||||||||
ChEMBL | Inhibition of liver glycogen phosphorylase A | B | 6.15 | pIC50 | 700 | nM | IC50 | Bioorg Med Chem (2008) 16: 7330-7336 [PMID:18595718] |
ChEMBL | Inhibition of phosphorylated form of pig liver glycogen phosphorylase | B | 6.17 | pIC50 | 670 | nM | IC50 | J Med Chem (2006) 49: 5687-5701 [PMID:16970395] |
Liver glycogen phosphorylase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3239] [UniProtKB: P09811] | ||||||||
ChEMBL | Inhibition of phosphorylated form of rat liver glycogen phosphorylase | B | 6.17 | pIC50 | 680 | nM | IC50 | J Med Chem (2006) 49: 5687-5701 [PMID:16970395] |
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]