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ChEMBL ligand: CHEMBL4277689 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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neuraminidase 1/Sialidase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2726] [GtoPdb: 3214] [UniProtKB: Q99519] | ||||||||
GtoPdb | - | - | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2018) 61: 11261-11279 [PMID:30457869] |
ChEMBL | Inhibition of human His6-tagged NEU1 expressed in HEK293 cells using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2018) 61: 11261-11279 [PMID:30457869] |
ChEMBL | Inhibition of His6-tagged human neuraminidase-1 expressed in HEK293 cells pre-incubated for 15 mins before 4MU-NANA substrate addition and measured after 30 mins by fluorescence based assay | B | 4.85 | pIC50 | 14000 | nM | IC50 | WO-2018213933-A1. Methods of preventing or treating atherosclerosis with inhibitors of specific isoenzymes of human neuraminidase (2018) |
neuraminidase 2/Sialidase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3200] [GtoPdb: 3258] [UniProtKB: Q9Y3R4] | ||||||||
ChEMBL | Competitive inhibition of N-terminal MBP-fused human NEU2 expressed in Escherichia coli using 4MU-NANA as substrate preincubated with substrate for 15 mins and measured every min for 30 mins by Lineweaver-Burk plot analysis | B | 5.89 | pKi | 1300 | nM | Ki | J Med Chem (2018) 61: 11261-11279 [PMID:30457869] |
GtoPdb | - | - | 5.89 | pKi | 1300 | nM | Ki | J Med Chem (2018) 61: 11261-11279 [PMID:30457869] |
ChEMBL | Inhibition of N-terminal MBP-fused human NEU2 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2018) 61: 11261-11279 [PMID:30457869] |
ChEMBL | Inhibition of N-terminal MBP tagged human neuraminidase-2 expressed in Escherichia coli pre-incubated for 15 mins before 4MU-NANA substrate addition and measured after 30 mins by fluorescence based assay | B | 5.68 | pIC50 | 2100 | nM | IC50 | WO-2018213933-A1. Methods of preventing or treating atherosclerosis with inhibitors of specific isoenzymes of human neuraminidase (2018) |
GtoPdb | - | - | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2018) 61: 11261-11279 [PMID:30457869] |
Sialidase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4174] [UniProtKB: Q8WWR8] | ||||||||
ChEMBL | Inhibition of MBP-fused human NEU4 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 4.33 | pIC50 | 47000 | nM | IC50 | J Med Chem (2018) 61: 11261-11279 [PMID:30457869] |
ChEMBL | Inhibition of N-terminal GST tagged human neuraminidase-4 expressed in Escherichia coli pre-incubated for 15 mins before 4MU-NANA substrate addition and measured after 30 mins by fluorescence based assay | B | 4.33 | pIC50 | 47000 | nM | IC50 | WO-2018213933-A1. Methods of preventing or treating atherosclerosis with inhibitors of specific isoenzymes of human neuraminidase (2018) |
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]