afegostat [Ligand Id: 7410] activity data from GtoPdb and ChEMBL
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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 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] |
| 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 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]
