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Synonyms: Compound 6412 from US9096541
Compound class: Synthetic organic
Comment: Inhibitor 3 showed potent BACE2 inhibitory activity, ~174,000-fold selectivity over BACE1 and ~15,000-fold selectivity over Cathepsin D . Note the PDB structure 5DQC is a co-crystalisation with comound 2 as PubChem CID 89836206 Inhibitor 3 is described in a patent as example 6412 . Activity data is included for ~30 analogues.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Ghosh AK, Reddy BS, Yen YC, Cardenas E, Rao KV, Downs D, Huang X, Tang J, Mesecar AD. (2016)
Design of Potent and Highly Selective Inhibitors for Human β-Secretase 2 (Memapsin 1), a Target for Type 2 Diabetes.
Chem Sci, 7: 3117-3122. [PMID:27347366]
2. Tang, J et al.. (2015)
Inhibition of memapsin 1 cleavage in the treatment of diabetes.
Patent number: US9096541. Assignee: Oklahoma Medical Research Foundation. Priority date: 03/11/2013. Publication date: 08/04/2015.