AZ-4217 [Ligand Id: 6939] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2152903 |
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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 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]
