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ChEMBL ligand: CHEMBL2347211 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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beta-secretase 1/Beta-secretase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817] | ||||||||
GtoPdb | - | - | 7.74 | pIC50 | 18 | nM | IC50 | Cell Metab (2011) 14: 365-77 [PMID:21907142] |
ChEMBL | Inhibition of recombinant human BACE1 using biotin-XSEVNLDAEFRHDSGC-Eu as substrate after 3 hrs by fluorescence assay | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2033-2045 [PMID:24704031] |
ChEMBL | Inhibition of human BACE1 using MR121-labeled substrate incubated for 4 mins prior to substrate addition measured after 2 mins by spectrophotometric analysis | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2013) 56: 3980-3995 [PMID:23590342] |
ChEMBL | Inhibition of BACE1 (unknown origin) | B | 8.17 | pIC50 | 6.7 | nM | IC50 | J Med Chem (2018) 61: 5122-5137 [PMID:29733614] |
ChEMBL | Inhibition of BACE1 (1 to 454 residues) (unknown origin) using Mca-APP Swedish Lys-Met/Asn-Leu mutant-Dnp quencher as substrate by fluorescence assay | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2019) 62: 5080-5095 [PMID:31021626] |
ChEMBL | Inhibition of human BACE1 in HEK293 cells transfected with wild type APP assessed as reduction of amyloid beta40 level after 18 to 20 hrs by AlphaLISA technique | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2013) 56: 3980-3995 [PMID:23590342] |
ChEMBL | Inhibition of BACE1 in human SKNBE2 cells expressing APP695 assessed as reduction in Abeta42 level measured after 18 hrs by sandwich ELISA | B | 9.03 | pIC50 | 0.93 | nM | IC50 | J Med Chem (2019) 62: 5080-5095 [PMID:31021626] |
ChEMBL | Inhibition of BACE1 (unknown origin) assessed as reduction in amyloid beta production by cell based assay | B | 9.08 | pIC50 | 0.84 | nM | IC50 | J Med Chem (2018) 61: 5122-5137 [PMID:29733614] |
beta-secretase 2/Beta secretase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2525] [GtoPdb: 2331] [UniProtKB: Q9Y5Z0] | ||||||||
ChEMBL | Inhibition of human BACE2 using MR121-labeled substrate incubated for 4 mins prior to substrate addition measured after 2 mins by spectrophotometric analysis | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2013) 56: 3980-3995 [PMID:23590342] |
GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | Cell Metab (2011) 14: 365-77 [PMID:21907142] |
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]