AZ-4217 [Ligand Id: 6939] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2152903
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  • beta-secretase 2/Beta secretase 2 in Human [ChEMBL: CHEMBL2525] [GtoPdb: 2331] [UniProtKB: Q9Y5Z0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
beta-secretase 1/Beta-secretase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817]
GtoPdb - - 8.74 pKi 1.8 nM Ki J. Neurosci. (2013) 33: 10075-84 [PMID:23761903]
ChEMBL Inhibition of human recombinant BACE1 using (europium)CEVNLDAEFK(Qsy7) as substrate incubated for 10 mins prior to substrate addition measured after 15 mins by TR-FRET assay B 8.61 pIC50 2.44 nM IC50 J. Med. Chem. (2012) 55: 9346-9361 [PMID:22924815]
ChEMBL Inhibition of BACE1 by diluted TR-FRET assay B 8.7 pIC50 2 nM IC50 ACS Med. Chem. Lett. (2012) 3: 869-870 [PMID:24900394]
ChEMBL Inhibition of BACE1 by secreted AAPbeta release assay B 9.7 pIC50 0.2 nM IC50 ACS Med. Chem. Lett. (2012) 3: 869-870 [PMID:24900394]
ChEMBL Inhibition of BACE1 in human SH-SY5Y cells assessed as inhibition of sAPPbeta release after 16 hrs by immunoassay B 9.8 pIC50 0.16 nM IC50 J. Med. Chem. (2012) 55: 9346-9361 [PMID:22924815]
beta-secretase 1/Beta-secretase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4593] [GtoPdb: 2330] [UniProtKB: P56818]
ChEMBL Inhibition of BACE1-mediated amyloid beta 40 release in C57/BL6 mouse primary cortical neurons after overnight incubation by ELISA B 8.59 pIC50 2.6 nM IC50 J. Med. Chem. (2012) 55: 9346-9361 [PMID:22924815]
beta-secretase 2/Beta secretase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2525] [GtoPdb: 2331] [UniProtKB: Q9Y5Z0]
ChEMBL Inhibition of human recombinant BACE2 using (europium)CEVNLDAEFK(Qsy7) as substrate incubated for 10 mins prior to substrate addition measured after 15 mins by TR-FRET assay B 8.12 pKi 7.5 nM Ki J. Med. Chem. (2012) 55: 9346-9361 [PMID:22924815]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in CHO cells by IonWorks assay B 5.55 pIC50 2800 nM IC50 J. Med. Chem. (2012) 55: 9346-9361 [PMID:22924815]

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]