LY2886721 [Ligand Id: 6475] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2396989 (Ly-2886721, Ly2886721, LY2886721) |
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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] | ||||||||
| ChEMBL | Inhibition of Fc domain of IgG1-fused human BACE1 (1 to 460) expressed in HEK293 cells preincubated for 10 mins followed by enzyme addition measured after 16 to 24 hrs by FRET assay | B | 7.69 | pIC50 | 20.3 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2033-2045 [PMID:24704031] |
| ChEMBL | Inhibition of human BACE1 (1 to 460 residues) expressed in HEK293 cells using mcaFRET peptide as substrate after 20 hrs by FRET assay | B | 7.69 | pIC50 | 20.3 | nM | IC50 | Bioorg Med Chem (2020) 28: 115194-115194 [PMID:31786008] |
| ChEMBL | Inhibition of human recombinant BACE1 by FRET assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5729-5731 [PMID:27816517] |
| GtoPdb | - | - | 7.7 | pIC50 | 20.3 | nM | IC50 | Alzheimers Dement (2012) 8: 95 |
| ChEMBL | Inhibition of BACE1 (unknown origin) | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5729-5731 [PMID:27816517] |
| ChEMBL | Inhibition of recombinant human BACE1 using (MCA)-S-E-V-N-L-D-A-E-F-R-K(dinitrophenol)-R-R-R-R-NH2 as substrate incubated for 8 hrs by FRET assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | J Med Chem (2021) 64: 8076-8100 [PMID:34081466] |
| beta-secretase 1/Beta-secretase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4593] [GtoPdb: 2330] [UniProtKB: P56818] | ||||||||
| ChEMBL | Inhibition of BACE1 in mouse primary cortical neuron assessed as reduction in Amyloid-beta level incubated for 24 hrs by sandwich ELISA assay | B | 7.97 | pIC50 | 10.7 | nM | IC50 | J Med Chem (2021) 64: 8076-8100 [PMID:34081466] |
| beta-secretase 2/Beta secretase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2525] [GtoPdb: 2331] [UniProtKB: Q9Y5Z0] | ||||||||
| ChEMBL | Inhibition of human BACE2 | B | 7.99 | pIC50 | 10.2 | nM | IC50 | Bioorg Med Chem (2020) 28: 115194-115194 [PMID:31786008] |
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]
